Hot Topics in Pharmacology

Coronavrius Information

We are currently collating information related to SARS-CoV-2 and COVID-19 at a dedicated coronavirus information page. This contains details of ligands and targets relevant to COVID-19 and links to useful resources and publications.

Recent publications of interest recommended by NC-IUPHAR

2022: May | Apr | Mar | Feb | Jan
2021: Dec | Nov | Oct | Sep | Aug | Jul | Jun | May

    May 2022


  • Profiling the Human Phosphoproteome to Estimate the True Extent of Protein Phosphorylation.
    Kalyuzhnyy A, Eyers PA, Eyers CE, Bowler-Barnett E, Martin MJ, Sun Z, Deutsch EW, Jones AR. Profiling the Human Phosphoproteome to Estimate the True Extent of Protein Phosphorylation. (2022)  J Proteome Res, [Epub ahead of print]. [PMID:35532924]

  • Neuroscience-based nomenclature of psychotropics: Progress report.
    Zohar J, Levy DM. Neuroscience-based nomenclature of psychotropics: Progress report. (2022)  Eur Neuropsychopharmacol, 57: 36-38. [PMID:35077943]

  • Mapping cell types across human tissues
    Domínguez Conde C, Xu C, Jarvis LB, Rainbow DB, Wells SB, Gomes T, Howlett SK, Suchanek O, Polanski K, King HW et al.. Cross-tissue immune cell analysis reveals tissue-specific features in humans. (2022)  Science, 376 (6594): eabl5197. [PMID:35549406]
    Liu Z, Zhang Z. Mapping cell types across human tissues. (2022)  Science, 376 (6594): 695-696. [PMID:35549410]
    Tabula Sapiens Consortium*, Jones RC, Karkanias J, Krasnow MA, Pisco AO, Quake SR, Salzman J, Yosef N, Bulthaup B, Brown P et al.. The Tabula Sapiens: A multiple-organ, single-cell transcriptomic atlas of humans. (2022)  Science, 376 (6594): eabl4896. [PMID:35549404]

  • Integrated genomics and chemical biology herald an era of sophisticated antibacterial discovery, from defining essential genes to target elucidation.
    Warrier T, Romano KP, Clatworthy AE, Hung DT. Integrated genomics and chemical biology herald an era of sophisticated antibacterial discovery, from defining essential genes to target elucidation. (2022)  Cell Chem Biol, [Epub ahead of print]. [PMID:35523184]

  • Control of host PTMs by intracellular bacteria: An opportunity toward novel anti-infective agents.
    Stévenin V, Neefjes J. Control of host PTMs by intracellular bacteria: An opportunity toward novel anti-infective agents. (2022)  Cell Chem Biol, [Epub ahead of print]. [PMID:35512694]

  • Gene regulation by gonadal hormone receptors underlies brain sex differences.
    Gegenhuber B, Wu MV, Bronstein R, Tollkuhn J. Gene regulation by gonadal hormone receptors underlies brain sex differences. (2022)  Nature, [Epub ahead of print]. [PMID:35508660]

  • Trends in innovative drug development in China.
    Su X, Wang H, Zhao N, Wang T, Cui Y. Trends in innovative drug development in China. (2022)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:35513561]

  • Endogenous pannexin1 channels form functional intercellular cell-cell channels with characteristic voltage-dependent properties.
    Palacios-Prado N, Soto PA, López X, Choi EJ, Marquez-Miranda V, Rojas M, Duarte Y, Lee J, González-Nilo FD, Sáez JC. Endogenous pannexin1 channels form functional intercellular cell-cell channels with characteristic voltage-dependent properties. (2022)  Proc Natl Acad Sci U S A, 119 (18): e2202104119. [PMID:35486697]

  • TLR7 and Lupus.
    Lowe D. TLR7 and Lupus. 
    Accessed on 16/05/2022. Modified on 16/05/2022. In the Pipeline, https://www.science.org/content/blog-post/tlr7-and-lupus

  • Physicochemical classification of organisms.
    Vallina Estrada E, Oliveberg M. Physicochemical classification of organisms. (2022)  Proc Natl Acad Sci U S A, 119 (19): e2122957119. [PMID:35500111]

  • April 2022


  • The complete sequence of a human genome
    Church DM. A next-generation human genome sequence. (2022)  Science, 376 (6588): 34-35. [PMID:35357937]
    Nurk S, Koren S, Rhie A, Rautiainen M, Bzikadze AV, Mikheenko A, Vollger MR, Altemose N, Uralsky L, Gershman A et al.. The complete sequence of a human genome. (2022)  Science, 376 (6588): 44-53. [PMID:35357919]

  • Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183.
    de Vries LE, Jansen PAM, Barcelo C, Munro J, Verhoef JMJ, Pasaje CFA, Rubiano K, Striepen J, Abla N, Berning L et al.. Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183. (2022)  Nat Commun, 13 (1): 2158. [PMID:35444200]

  • Emergence of new subgenomic mRNAs in SARS-CoV-2.
    Mears HV, Young GR, Sanderson T, Harvey R, Crawford M, Snell DM, Fowler AS, Hussain S, Nicod J, Peacock TP et al.. Emergence of new subgenomic mRNAs in SARS-CoV-2. (2022)  bioRxiv, Preprint. DOI: 10.1101/2022.04.20.488895

  • Novel drug targets in 2021.
    Avram S, Halip L, Curpan R, Oprea TI. Novel drug targets in 2021. (2022)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:35361900]

  • Hot Topics: A new study shows that human ageing is absolutely precise, when disease is eliminated, and accompanied by a disintegration of metabolic efficiency

    Comments by the Guide to Pharmacology Curation Team, University of Edinburgh

    Hot Topics: A new study shows that human ageing is absolutely precise, when disease is eliminated, and accompanied by a disintegration of metabolic efficiency. Read the full article on our blog

  • Hot Topics: Endothelin-1 pathway, a new therapeutic target for COVID-19

    Comments by the Guide to Pharmacology Curation Team, University of Edinburgh

    SARS-CoV-2 gains entry into the body mainly via the lungs. After entering the blood, the virus rapidly multiplies to infect nearby cells. Endothelial cells line every blood vessel and have a surface area similar to a tennis court. These cells are especially vulnerable to virus infection as they express the the virus entry receptor, ACE2. Endothelial cells are also a source of endothelin-1 (ET-1), which is released in response to injury to cause long lasting vasoconstriction, reducing oxygen supply to vital organs. In the lungs, this can cause breathing difficulty, which in severe cases requires patients to be given oxygen and put on a ventilator.. Read the full article on our blog

  • Structural Perspective on the Mechanism of Signal Activation, Ligand Selectivity and Allosteric Modulation in Angiotensin Receptors: IUPHAR Review 34.
    Singh KD, Karnik SS. Structural Perspective on the Mechanism of Signal Activation, Ligand Selectivity and Allosteric Modulation in Angiotensin Receptors: IUPHAR Review 34. (2022)  Br J Pharmacol, [Epub ahead of print]. DOI: 10.1111/bph.15840 [PMID:35318654]

  • Eicosanoid signaling blockade protects middle-aged mice from severe COVID-19.
    Wong LR, Zheng J, Wilhelmsen K, Li K, Ortiz ME, Schnicker NJ, Thurman A, Pezzulo AA, Szachowicz PJ, Li P et al.. Eicosanoid signaling blockade protects middle-aged mice from severe COVID-19. (2022)  Nature, [Epub ahead of print]. DOI: 10.1038/s41586-022-04630-3 [PMID:35314834]

  • A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic
    Guide to Pharmacology Curation Team. Database Release 2022.1.  guidetopharmacology blog, https://blog.guidetopharmacology.org/2022/03/31/database-release-2022-1/#N-0385
    Shapira T, Monreal IA, Dion SP, Buchholz DW, Imbiakha B, Olmstead AD, Jager M, Désilets A, Gao G, Martins M et al.. A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic. (2022)  Nature, [Epub ahead of print]. DOI: 10.1038/s41586-022-04661-w [PMID:35344983]

  • March 2022


  • Protein tyrosine phosphatase receptor δ serves as the orexigenic asprosin receptor.
    Mishra I, Xie WR, Bournat JC, He Y, Wang C, Silva ES, Liu H, Ku Z, Chen Y, Erokwu BO et al.. Protein tyrosine phosphatase receptor δ serves as the orexigenic asprosin receptor. (2022)  Cell Metab, [Epub ahead of print]. [PMID:35298903]

  • International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update.
    IJzerman AP, Jacobson KA, Müller CE, Cronstein BN, Cunha RA. International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update. (2022)  Pharmacol Rev, 74 (2): 340-372. [PMID:35302044]

  • Common coupling map advances GPCR-G protein selectivity.
    Hauser AS, Avet C, Normand C, Mancini A, Inoue A, Bouvier M, Gloriam DE. Common coupling map advances GPCR-G protein selectivity. (2022)  Elife, 11 [Epub ahead of print]. [PMID:35302494]

  • Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs.
    Avet C, Mancini A, Breton B, Le Gouill C, Hauser AS, Normand C, Kobayashi H, Gross F, Hogue M, Lukasheva V et al.. Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs. (2022)  Elife, 11 [Epub ahead of print]. [PMID:35302493]

  • Homotypic fibrillization of TMEM106B across diverse neurodegenerative diseases.
    Chang A, Xiang X, Wang J, Lee C, Arakhamia T, Simjanoska M, Wang C, Carlomagno Y, Zhang G, Dhingra S et al.. Homotypic fibrillization of TMEM106B across diverse neurodegenerative diseases. (2022)  Cell, [Epub ahead of print]. [PMID:35247328]

  • Structural insights into ligand recognition, activation, and signaling of the α2A adrenergic receptor.
    Xu J, Cao S, Hübner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y. Structural insights into ligand recognition, activation, and signaling of the α2A adrenergic receptor. (2022)  Sci Adv, 8 (9): eabj5347. [PMID:35245122]

  • Mammalian monocarboxylate transporter 7 (MCT7/Slc16a6) is a novel facilitative taurine transporter.
    Higuchi K, Sugiyama K, Tomabechi R, Kishimoto H, Inoue K. Mammalian monocarboxylate transporter 7 (MCT7/Slc16a6) is a novel facilitative taurine transporter. (2022)  J Biol Chem,: 101800 [Epub ahead of print]. [PMID:35257743]

  • Targeting solute carriers to modulate receptor-ligand interactions.
    Sijben HJ, Superti-Furga G, IJzerman AP, Heitman LH. Targeting solute carriers to modulate receptor-ligand interactions. (2022)  Trends Pharmacol Sci, [Epub ahead of print]. [PMID:35232590]

  • High-throughput metabolomics predicts drug-target relationships for eukaryotic proteins.
    Holbrook-Smith D, Durot S, Sauer U. High-throughput metabolomics predicts drug-target relationships for eukaryotic proteins. (2022)  Mol Syst Biol, 18 (2): e10767. [PMID:35194925]

  • Systematic illumination of druggable genes in cancer genomes.
    Jiang J, Yuan J, Hu Z, Zhang Y, Zhang T, Xu M, Long M, Fan Y, Tanyi JL, Montone KT et al.. Systematic illumination of druggable genes in cancer genomes. (2022)  Cell Rep, 38 (8): 110400. [PMID:35196490]

  • Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.
    Chen LH, Zhang Q, Xiao YF, Fang YC, Xie X, Nan FJ. Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis. (2022)  J Med Chem, [Epub ahead of print]. [PMID:35195005]

  • Conserved hydrogen-bond motifs of membrane transporters and receptors.
    Lazaratos M, Siemers M, Brown LS, Bondar AN. Conserved hydrogen-bond motifs of membrane transporters and receptors. (2022)  Biochim Biophys Acta Biomembr, 1864 (6): 183896 [Epub ahead of print]. [PMID:35217000]

  • February 2022


  • Structure, mechanism and lipid-mediated remodeling of the mammalian Na+/H+ exchanger NHA2.
    Matsuoka R, Fudim R, Jung S, Zhang C, Bazzone A, Chatzikyriakidou Y, Robinson CV, Nomura N, Iwata S, Landreh M et al.. Structure, mechanism and lipid-mediated remodeling of the mammalian Na+/H+ exchanger NHA2. (2022)  Nat Struct Mol Biol, 29 (2): 108-120. [PMID:35173351]

  • Pharmaceutical pollution of the world's rivers.
    Wilkinson JL, Boxall ABA, Kolpin DW, Leung KMY, Lai RWS, Galbán-Malagón C, Adell AD, Mondon J, Metian M, Marchant RA et al.. Pharmaceutical pollution of the world's rivers. (2022)  Proc Natl Acad Sci U S A, 119 (8). [PMID:35165193]

  • Structural Insights into Molecular Recognition by Human Chemokine CCL19.
    Lewandowski EM, Kroeck KG, Jacobs LMC, Fenske TG, Witt RN, Hintz AM, Ramsden ER, Zhang X, Peterson F, Volkman BF et al.. Structural Insights into Molecular Recognition by Human Chemokine CCL19. (2022)  Biochemistry, [Epub ahead of print]. [PMID:35156805]

  • Spatial transcriptomics of dorsal root ganglia identifies molecular signatures of human nociceptors.
    Tavares-Ferreira D, Shiers S, Ray PR, Wangzhou A, Jeevakumar V, Sankaranarayanan I, Cervantes AM, Reese JC, Chamessian A, Copits BA et al.. Spatial transcriptomics of dorsal root ganglia identifies molecular signatures of human nociceptors. (2022)  Sci Transl Med, 14 (632): eabj8186. [PMID:35171654]

  • Hot Topics: SARS-CoV-2 and the truncated ACE-2 variant

    Comments by Christopher Southan, Data Science, Medicines Discovery Catapult and Honorary Fellow, University of Edinburgh.

    ACE2 normally functions as an enzyme metabolising peptides that regulate the cardiovascular system but also acts as a receptor for SARS-CoV-2. This study compared the distribution in human tissue of ACE2 versus deltaACE2, a recently discovered truncated isoform that has lost the spike binding sites for SARS-CoV-2, and is predicted to confer reduced susceptibility to viral infection. ACE2 was highly expressed in human lung, kidney, heart, liver and vasculature. However, deltaACE2 was the predominant isoform in lung airway and liver bile duct epithelia, which may be a contributing factor to variation in response to the virus.. Read the full article on our blog

  • Mechanism of CFTR correction by type I folding correctors.
    Fiedorczuk K, Chen J. Mechanism of CFTR correction by type I folding correctors. (2022)  Cell, 185 (1): 158-168.e11. [PMID:34995514]

  • P2X4 and P2X7 are essential players in basal T cell activity and Ca2+ signaling milliseconds after T cell activation.
    Brock VJ, Wolf IMA, Er-Lukowiak M, Lory N, Stähler T, Woelk LM, Mittrücker HW, Müller CE, Koch-Nolte F, Rissiek B et al.. P2X4 and P2X7 are essential players in basal T cell activity and Ca2+ signaling milliseconds after T cell activation. (2022)  Sci Adv, 8 (5): eabl9770. [PMID:35119925]

  • Community Guidelines for GPCR Ligand Bias: IUPHAR Review 32.
    Kolb P, Kenakin T, Alexander SPH, Bermudez M, Bohn LM, Breinholt CS, Bouvier M, Hill SJ, Kostenis E, Martemyanov K et al.. Community Guidelines for GPCR Ligand Bias: IUPHAR Review 32. (2022)  Br J Pharmacol, [Epub ahead of print]. [PMID:35106752]

  • Structure of the NLRP3 decamer bound to the cytokine release inhibitor CRID3.
    Hochheiser IV, Pilsl M, Hagelueken G, Moecking J, Marleaux M, Brinkschulte R, Latz E, Engel C, Geyer M. Structure of the NLRP3 decamer bound to the cytokine release inhibitor CRID3. (2022)  Nature, [Epub ahead of print]. [PMID:35114687]

  • January 2022


  • Structure and transport mechanism of the human cholesterol transporter ABCG1.
    Xu D, Li Y, Yang F, Sun CR, Pan J, Wang L, Chen ZP, Fang SC, Yao X, Hou WT et al.. Structure and transport mechanism of the human cholesterol transporter ABCG1. (2022)  Cell Rep, 38 (4): 110298. [PMID:35081353]

  • Rearrangement of a unique Kv1.3 selectivity filter conformation upon binding of a drug.
    Tyagi A, Ahmed T, Jian S, Bajaj S, Ong ST, Goay SSM, Zhao Y, Vorobyov I, Tian C, Chandy KG et al.. Rearrangement of a unique Kv1.3 selectivity filter conformation upon binding of a drug. (2022)  Proc Natl Acad Sci U S A, 119 (5). [PMID:35091471]

  • Inhibition of sphingolipid de novo synthesis counteracts muscular dystrophy.
    Laurila PP, Luan P, Wohlwend M, Zanou N, Crisol B, Imamura de Lima T, Goeminne LJE, Gallart-Ayala H, Shong M, Ivanisevic J et al.. Inhibition of sphingolipid de novo synthesis counteracts muscular dystrophy. (2022)  Sci Adv, 8 (4): eabh4423. [PMID:35089797]

  • The cGAS-STING pathway drives type I IFN immunopathology in COVID-19.
    Di Domizio J, Gulen MF, Saidoune F, Thacker VV, Yatim A, Sharma K, Nass T, Guenova E, Schaller M, Conrad C et al.. The cGAS-STING pathway drives type I IFN immunopathology in COVID-19. (2022)  Nature, [Epub ahead of print]. DOI: 10.1038/s41586-022-04421-w [PMID:35045565]

  • AI in health and medicine.
    Rajpurkar P, Chen E, Banerjee O, Topol EJ. AI in health and medicine. (2022)  Nat Med, [Epub ahead of print]. [PMID:35058619]

  • Structural mechanism of human TRPC3 and TRPC6 channel regulation by their intracellular calcium-binding sites.
    Guo W, Tang Q, Wei M, Kang Y, Wu JX, Chen L. Structural mechanism of human TRPC3 and TRPC6 channel regulation by their intracellular calcium-binding sites. (2022)  Neuron, [Epub ahead of print]. [PMID:35051376]

  • NO rapidly mobilizes cellular heme to trigger assembly of its own receptor.
    Dai Y, Faul EM, Ghosh A, Stuehr DJ. NO rapidly mobilizes cellular heme to trigger assembly of its own receptor. (2022)  Proc Natl Acad Sci U S A, 119 (4). [PMID:35046034]

  • A guide to immunotherapy for COVID-19.
    van de Veerdonk FL, Giamarellos-Bourboulis E, Pickkers P, Derde L, Leavis H, van Crevel R, Engel JJ, Wiersinga WJ, Vlaar APJ, Shankar-Hari M et al.. A guide to immunotherapy for COVID-19. (2022)  Nat Med, [Epub ahead of print]. [PMID:35064248]

  • Longitudinal analysis reveals high prevalence of Epstein-Barr virus associated with multiple sclerosis.
    Bjornevik K, Cortese M, Healy BC, Kuhle J, Mina MJ, Leng Y, Elledge SJ, Niebuhr DW, Scher AI, Munger KL et al.. Longitudinal analysis reveals high prevalence of Epstein-Barr virus associated with multiple sclerosis. (2022)  Science, [Epub ahead of print]. [PMID:35025605]

  • December 2021


  • Synthon-based ligand discovery in virtual libraries of over 11 billion compounds.
    Sadybekov AA, Sadybekov AV, Liu Y, Iliopoulos-Tsoutsouvas C, Huang XP, Pickett J, Houser B, Patel N, Tran NK, Tong F et al.. Synthon-based ligand discovery in virtual libraries of over 11 billion compounds. (2021)  Nature, [Epub ahead of print]. [PMID:34912117]

  • Macrophages transfer mitochondria to sensory neurons to resolve inflammatory pain.
    van der Vlist M, Raoof R, Willemen HLDM, Prado J, Versteeg S, Martin Gil C, Vos M, Lokhorst RE, Pasterkamp RJ, Kojima T et al.. Macrophages transfer mitochondria to sensory neurons to resolve inflammatory pain. (2021)  Neuron, [Epub ahead of print]. [PMID:34921782]

  • Structure-Based Virtual Screening for Ligands of G Protein-Coupled Receptors: What Can Molecular Docking Do for You?.
    Ballante F, Kooistra AJ, Kampen S, de Graaf C, Carlsson J. Structure-Based Virtual Screening for Ligands of G Protein-Coupled Receptors: What Can Molecular Docking Do for You?. (2021)  Pharmacol Rev, 73 (4): 527-565. [PMID:34907092]

  • Aprepitant is a novel, selective activator of the K2P channel TRAAK.
    McCoull D, Veale EL, Walsh Y, Byrom L, Avkiran T, Large JM, Vaitone E, Gaffey F, Jerman J, Mathie A, Wright PD. Aprepitant is a novel, selective activator of the K2P channel TRAAK. (2022)  BBRC, 588: 41-46 [Epub ahead of print]. DOI: 10.1016/j.bbrc.2021.12.031

  • Structures of the σ2 receptor enable docking for bioactive ligand discovery.
    Alon A, Lyu J, Braz JM, Tummino TA, Craik V, O'Meara MJ, Webb CM, Radchenko DS, Moroz YS, Huang XP et al.. Structures of the σ2 receptor enable docking for bioactive ligand discovery. (2021)  Nature, [Epub ahead of print]. [PMID:34880501]

  • Structure and mechanism of the SGLT family of glucose transporters.
    Han L, Qu Q, Aydin D, Panova O, Robertson MJ, Xu Y, Dror RO, Skiniotis G, Feng L. Structure and mechanism of the SGLT family of glucose transporters. (2021)  Nature, [Epub ahead of print]. [PMID:34880492]

  • Key cancer results failed to be reproduced.
    Kaiser J. Key cancer results failed to be reproduced. (2021)  Science, 374 (6573): 1311. [PMID:34882444]

  • Structural basis of inhibition of the human SGLT2-MAP17 glucose transporter.
    Niu Y, Liu R, Guan C, Zhang Y, Chen Z, Hoerer S, Nar H, Chen L. Structural basis of inhibition of the human SGLT2-MAP17 glucose transporter. (2021)  Nature, [Epub ahead of print]. [PMID:34880493]

  • A hormone complex of FABP4 and nucleoside kinases regulates islet function.
    Prentice KJ, Saksi J, Robertson LT, Lee GY, Inouye KE, Eguchi K, Lee A, Cakici O, Otterbeck E, Cedillo P et al.. A hormone complex of FABP4 and nucleoside kinases regulates islet function. (2021)  Nature, [Epub ahead of print]. [PMID:34880500]

  • From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
    Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD et al.. From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. (2021)  Cell, 184 (24): 5886-5901.e22. [PMID:34822784]

  • November 2021


  • GPCR activation mechanisms across classes and macro/microscales.
    Hauser AS, Kooistra AJ, Munk C, Heydenreich FM, Veprintsev DB, Bouvier M, Babu MM, Gloriam DE. GPCR activation mechanisms across classes and macro/microscales. (2021)  Nat Struct Mol Biol, 28 (11): 879-888. [PMID:34759375]

  • Toxoplasma gondii serine hydrolases regulate parasite lipid mobilization during growth and replication within the host.
    Onguka O, Babin BM, Lakemeyer M, Foe IT, Amara N, Terrell SM, Lum KM, Cieplak P, Niphakis MJ, Long JZ et al.. Toxoplasma gondii serine hydrolases regulate parasite lipid mobilization during growth and replication within the host. (2021)  Cell Chem Biol, 28 (10): 1501-1513.e5. [PMID:34043961]

  • AdipoAtlas: A reference lipidome for human white adipose tissue.
    Lange M, Angelidou G, Ni Z, Criscuolo A, Schiller J, Blüher M, Fedorova M. AdipoAtlas: A reference lipidome for human white adipose tissue. (2021)  Cell Rep Med, 2 (10): 100407. [PMID:34755127]

  • Morphology and gene expression profiling provide complementary information for mapping cell state.
    Way GP, Natoli T, Adeboye A, Litichevskiy L, Yang A, Lu X, Caicedo JC, Cimini BA, Karhohs K, Logan DJ et al.. Morphology and gene expression profiling provide complementary information for mapping cell state. (2021)  bioRxiv, Preprint. DOI: 10.1101/2021.10.21.465335

  • Pfizer's Good News Is the World's Good News.
    Lowe D. Pfizer's Good News Is the World's Good News. 
    Accessed on 10/11/2021. Modified on 10/11/2021. In the Pipeline, https://www.science.org/content/blog-post/pfizer-s-good-news-world-s-good-news

  • Mechanistic insights into COVID-19 by global analysis of the SARS-CoV-2 3CLpro substrate degradome.
    Pablos I, Machado Y, de Jesus HCR, Mohamud Y, Kappelhoff R, Lindskog C, Vlok M, Bell PA, Butler GS, Grin PM et al.. Mechanistic insights into COVID-19 by global analysis of the SARS-CoV-2 3CLpro substrate degradome. (2021)  Cell Rep, 37 (4): 109892. [PMID:34672947]

  • Every gene can (and possibly will) be associated with cancer.
    João Pedro de Magalhães. Every gene can (and possibly will) be associated with cancer. (2021)  Trends in Genetics,. DOI: 10.1016/j.tig.2021.09.005

  • October 2021


  • COVID19 Disease Map, a computational knowledge repository of virus-host interaction mechanisms
    Ostaszewski M, Niarakis A, Mazein A, Kuperstein I, Phair R, Orta-Resendiz A, Singh V, Aghamiri SS, Acencio ML, Glaab E et al.. COVID19 Disease Map, a computational knowledge repository of virus-host interaction mechanisms. (2021)  Mol Syst Biol, 17 (10): e10387. [PMID:34664389]
    COVID-19 Disease Map.  https://covid.pages.uni.lu/

  • The risks of using unapproved gene symbols.
    Braschi B, Seal RL, Tweedie S, Jones TEM, Bruford EA. The risks of using unapproved gene symbols. (2021)  Am J Hum Genet, 108 (10): 1813-1816. [PMID:34626580]

  • Inositol serves as a natural inhibitor of mitochondrial fission by directly targeting AMPK.
    Hsu CC, Zhang X, Wang G, Zhang W, Cai Z, Pan BS, Gu H, Xu C, Jin G, Xu X et al.. Inositol serves as a natural inhibitor of mitochondrial fission by directly targeting AMPK. (2021)  Mol Cell, 81 (18): 3803-3819.e7. [PMID:34547240]

  • Association of physical activity intensity and bout length with mortality: An observational study of 79,503 UK Biobank participants.
    Millard LAC, Tilling K, Gaunt TR, Carslake D, Lawlor DA. Association of physical activity intensity and bout length with mortality: An observational study of 79,503 UK Biobank participants. (2021)  PLoS Med, 18 (9): e1003757. [PMID:34525088]

  • Defining variant-resistant epitopes targeted by SARS-CoV-2 antibodies: A global consortium study.
    Hastie KM, Li H, Bedinger D, Schendel SL, Dennison SM, Li K, Rayaprolu V, Yu X, Mann C, Zandonatti M et al.. Defining variant-resistant epitopes targeted by SARS-CoV-2 antibodies: A global consortium study. (2021)  Science,: eabh2315 [Epub ahead of print]. [PMID:34554826]

  • The G protein database, GproteinDb.
    Pándy-Szekeres G, Esguerra M, Hauser AS, Caroli J, Munk C, Pilger S, Keserű GM, Kooistra AJ, Gloriam DE. The G protein database, GproteinDb. (2021)  Nucleic Acids Res, [Epub ahead of print]. [PMID:34570219]

  • The biological and clinical significance of emerging SARS-CoV-2 variants.
    Tao K, Tzou PL, Nouhin J, Gupta RK, de Oliveira T, Kosakovsky Pond SL, Fera D, Shafer RW. The biological and clinical significance of emerging SARS-CoV-2 variants. (2021)  Nat Rev Genet, [Epub ahead of print]. [PMID:34535792]

  • Gut microbiota-mediated secondary bile acids regulate dendritic cells to attenuate autoimmune uveitis through TGR5 signaling.
    Hu J, Wang C, Huang X, Yi S, Pan S, Zhang Y, Yuan G, Cao Q, Ye X, Li H. Gut microbiota-mediated secondary bile acids regulate dendritic cells to attenuate autoimmune uveitis through TGR5 signaling. (2021)  Cell Rep, 36 (12): 109726. [PMID:34551302]

  • Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics.
    Kiss M, Mbasu R, Nicolaï J, Barnouin K, Kotian A, Mooij MG, Kist N, Wijnen RMH, Ungell AL, Cutler P et al.. Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics. (2021)  Drug Metab Dispos, [Epub ahead of print]. [PMID:34548392]

  • Reading ADP-ribosylation signaling using chemical biology and interaction proteomics.
    Kliza KW, Liu Q, Roosenboom LWM, Jansen PWTC, Filippov DV, Vermeulen M. Reading ADP-ribosylation signaling using chemical biology and interaction proteomics. (2021)  Mol Cell, [Epub ahead of print]. [PMID:34551281]

  • Structural basis of gating modulation of Kv4 channel complexes.
    Kise Y, Kasuya G, Okamoto HH, Yamanouchi D, Kobayashi K, Kusakizako T, Nishizawa T, Nakajo K, Nureki O. Structural basis of gating modulation of Kv4 channel complexes. (2021)  Nature, [Epub ahead of print]. [PMID:34552243]

  • The lesson of ivermectin: meta-analyses based on summary data alone are inherently unreliable.
    Lawrence JM, Meyerowitz-Katz G, Heathers JAJ, Brown NJL, Sheldrick KA. The lesson of ivermectin: meta-analyses based on summary data alone are inherently unreliable. (2021)  Nat Med, [Epub ahead of print]. [PMID:34552263]

  • September 2021


  • Insights into the expanding phenotypic spectrum of inherited disorders of biogenic amines.
    Kuseyri Hübschmann O, Horvath G, Cortès-Saladelafont E, Yıldız Y, Mastrangelo M, Pons R, Friedman J, Mercimek-Andrews S, Wong SN, Pearson TS et al.. Insights into the expanding phenotypic spectrum of inherited disorders of biogenic amines. (2021)  Nat Commun, 12 (1): 5529. [PMID:34545092]

  • Drug repurposing: Misconceptions, challenges, and opportunities for academic researchers.
    Begley CG, Ashton M, Baell J, Bettess M, Brown MP, Carter B, Charman WN, Davis C, Fisher S, Frazer I et al.. Drug repurposing: Misconceptions, challenges, and opportunities for academic researchers. (2021)  Sci Transl Med, 13 (612): eabd5524. [PMID:34550729]

  • Structures of the human cholecystokinin receptors bound to agonists and antagonists.
    Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X et al.. Structures of the human cholecystokinin receptors bound to agonists and antagonists. (2021)  Nat Chem Biol, [Epub ahead of print]. [PMID:34556863]

  • Ligand recognition and G-protein coupling selectivity of cholecystokinin A receptor.
    Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C et al.. Ligand recognition and G-protein coupling selectivity of cholecystokinin A receptor. (2021)  Nat Chem Biol, [Epub ahead of print]. [PMID:34556862]

  • Clinical Lipidomics: Realizing the potential of lipid profiling.
    Meikle TG, Huynh K, Giles C, Meikle PJ. Clinical Lipidomics: Realizing the potential of lipid profiling. (2021)  J Lipid Res,: 100127 [Epub ahead of print]. [PMID:34582882]

  • Examining Gender Imbalance in Chemistry Authorship.
    Cotton AD, Seiple IB. Examining Gender Imbalance in Chemistry Authorship. (2021)  ACS Chem Biol, [Epub ahead of print]. [PMID:34523912]

  • Probing the molecular basis for signal transduction through the Zinc-Activated Channel (ZAC).
    Madjroh N, Mellou E, Æbelø L, Davies PA, Söderhielm PC, Jensen AA. Probing the molecular basis for signal transduction through the Zinc-Activated Channel (ZAC). (2021)  Biochem Pharmacol,: 114781 [Epub ahead of print]. [PMID:34560053]

  • Ligandability of E3 Ligases for Targeted Protein Degradation Applications.
    Belcher BP, Ward CC, Nomura DK. Ligandability of E3 Ligases for Targeted Protein Degradation Applications. (2021)  Biochemistry, [Epub ahead of print]. DOI: 10.1021/acs.biochem.1c00464 [PMID:34473924]

  • Cryo-EM and antisense targeting of the 28-kDa frameshift stimulation element from the SARS-CoV-2 RNA genome.
    Zhang K, Zheludev IN, Hagey RJ, Haslecker R, Hou YJ, Kretsch R, Pintilie GD, Rangan R, Kladwang W, Li S et al.. Cryo-EM and antisense targeting of the 28-kDa frameshift stimulation element from the SARS-CoV-2 RNA genome. (2021)  Nat Struct Mol Biol, [Epub ahead of print]. DOI: 10.1038/s41594-021-00653-y [PMID:34426697]

  • SLC-30A9 is required for Zn2+ homeostasis, Zn2+ mobilization, and mitochondrial health.
    Deng H, Qiao X, Xie T, Fu W, Li H, Zhao Y, Guo M, Feng Y, Chen L, Zhao Y et al.. SLC-30A9 is required for Zn2+ homeostasis, Zn2+ mobilization, and mitochondrial health. (2021)  Proc Natl Acad Sci U S A, 118 (35). DOI: 10.1073/pnas.2023909118 [PMID:34433664]

  • Up-regulation of the manganese transporter SLC30A10 by hypoxia-inducible factors defines a homeostatic response to manganese toxicity.
    Liu C, Jursa T, Aschner M, Smith DR, Mukhopadhyay S. Up-regulation of the manganese transporter SLC30A10 by hypoxia-inducible factors defines a homeostatic response to manganese toxicity. (2021)  Proc Natl Acad Sci U S A, 118 (35). DOI: 10.1073/pnas.2107673118 [PMID:34446561]

  • Neuropeptide S receptor 1 is a nonhormonal treatment target in endometriosis.
    Tapmeier TT, Rahmioglu N, Lin J, De Leo B, Obendorf M, Raveendran M, Fischer OM, Bafligil C, Guo M, Harris RA et al.. Neuropeptide S receptor 1 is a nonhormonal treatment target in endometriosis. (2021)  Sci Transl Med, 13 (608). DOI: 10.1126/scitranslmed.abd6469 [PMID:34433639]

  • Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A3 Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary.
    Lee Y, Hou X, Lee JH, Nayak A, Alexander V, Sharma PK, Chang H, Phan K, Gao ZG, Jacobson KA et al.. Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A3 Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary. (2021)  J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.1c00239 [PMID:34435786]

  • Will the chemical probes please stand up?.
    Škuta C, Southan C, Bartůněk P. Will the chemical probes please stand up?. (2021)  RSC Med Chem, 12 (8): 1428-1441. [PMID:34447939]

  • August 2021


  • Rare variant contribution to human disease in 281,104 UK Biobank exomes.
    Wang Q, Dhindsa RS, Carss K, Harper AR, Nag A, Tachmazidou I, Vitsios D, Deevi SVV, Mackay A, Muthas D et al.. Rare variant contribution to human disease in 281,104 UK Biobank exomes. (2021)  Nature, [Epub ahead of print]. [PMID:34375979]

  • Clinical Features of Vaccine-Induced Immune Thrombocytopenia and Thrombosis.
    Pavord S, Scully M, Hunt BJ, Lester W, Bagot C, Craven B, Rampotas A, Ambler G, Makris M. Clinical Features of Vaccine-Induced Immune Thrombocytopenia and Thrombosis. (2021)  N Engl J Med, [Epub ahead of print]. [PMID:34379914]

  • Leslie Iversen, a friend of friends and an inspiring light in neuropharmacology.
    Cuello AC. Leslie Iversen, a friend of friends and an inspiring light in neuropharmacology. (2021)  Proc Natl Acad Sci U S A, 118 (32). [PMID:34353919]

  • Nicotinic acetylcholine receptor redux: Discovery of accessories opens therapeutic vistas.
    Matta JA, Gu S, Davini WB, Bredt DS. Nicotinic acetylcholine receptor redux: Discovery of accessories opens therapeutic vistas. (2021)  Science, 373 (6556). [PMID:34385370]

  • Anti-Platelet Drugs Block Platelet Activation by Vaccine-Induced Immune Thrombocytopenia and Thrombosis Patient Serum.
    Smith CW, Montague SJ, Kardeby C, DI Y, Lowe GC, Lester WA, Watson SP, Nicolson PLR. Anti-Platelet Drugs Block Platelet Activation by Vaccine-Induced Immune Thrombocytopenia and Thrombosis Patient Serum. (2021)  Blood, [Epub ahead of print]. DOI: 10.1182/blood.2021012277 [PMID:34375398]

  • Amino acid transporter LAT1 (SLC7A5) as a molecular target for cancer diagnosis and therapeutics.
    Kanai Y. Amino acid transporter LAT1 (SLC7A5) as a molecular target for cancer diagnosis and therapeutics. (2021)  Pharmacol Ther,: 107964 [Epub ahead of print]. [PMID:34390745]

  • Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor.
    Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ et al.. Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor. (2021)  ACS Chem Neurosci, [Epub ahead of print]. [PMID:34351123]

  • Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.
    Moehle MS, Bender AM, Dickerson JW, Foster DJ, Qi A, Cho HP, Donsante Y, Peng W, Bryant Z, Stillwell KJ et al.. Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy. (2021)  ACS Pharmacol. Transl. Sci., [Epub ahead of print]. DOI: 10.1021/acsptsci.0c00162

  • The residence of synaptically released dopamine on D2 autoreceptors.
    Condon AF, Robinson BG, Asad N, Dore TM, Tian L, Williams JT. The residence of synaptically released dopamine on D2 autoreceptors. (2021)  Cell Rep, 36 (5): 109465. [PMID:34348146]

  • Antisense oligonucleotide-mediated inhibition of angiopoietin-like protein 3 increases reverse cholesterol transport in mice.
    Bell 3rd TA, Liu M, Donner AJ, Lee RG, Mullick AE, Crooke RM. Antisense oligonucleotide-mediated inhibition of angiopoietin-like protein 3 increases reverse cholesterol transport in mice. (2021)  J Lipid Res,: 100101 [Epub ahead of print]. [PMID:34371033]

  • The structural basis of odorant recognition in insect olfactory receptors.
    Del Mármol J, Yedlin MA, Ruta V. The structural basis of odorant recognition in insect olfactory receptors. (2021)  Nature, [Epub ahead of print]. [PMID:34349260]

  • Cell specific photoswitchable agonist for reversible control of endogenous dopamine receptors.
    Donthamsetti P, Winter N, Hoagland A, Stanley C, Visel M, Lammel S, Trauner D, Isacoff E. Cell specific photoswitchable agonist for reversible control of endogenous dopamine receptors. (2021)  Nat Commun, 12 (1): 4775. [PMID:34362914]

  • Cryo-EM structure of the human MT1-Gi signaling complex.
    Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N et al.. Cryo-EM structure of the human MT1-Gi signaling complex. (2021)  Nat Struct Mol Biol, [Epub ahead of print]. [PMID:34354246]

  • Structural basis for enhanced infectivity and immune evasion of SARS-CoV-2 variants.
    Cai Y, Zhang J, Xiao T, Lavine CL, Rawson S, Peng H, Zhu H, Anand K, Tong P, Gautam A et al.. Structural basis for enhanced infectivity and immune evasion of SARS-CoV-2 variants. (2021)  Science, 373 (6555): 642-648. [PMID:34168070]

  • Effect of natural mutations of SARS-CoV-2 on spike structure, conformation, and antigenicity.
    Gobeil SM, Janowska K, McDowell S, Mansouri K, Parks R, Stalls V, Kopp MF, Manne K, Li D, Wiehe K et al.. Effect of natural mutations of SARS-CoV-2 on spike structure, conformation, and antigenicity. (2021)  Science, 373 (6555). [PMID:34168071]

  • A high-throughput cell- and virus-free assay shows reduced neutralization of SARS-CoV-2 variants by COVID-19 convalescent plasma.
    Fenwick C, Turelli P, Pellaton C, Farina A, Campos J, Raclot C, Pojer F, Cagno V, Nusslé SG, D'Acremont V et al.. A high-throughput cell- and virus-free assay shows reduced neutralization of SARS-CoV-2 variants by COVID-19 convalescent plasma. (2021)  Sci Transl Med, 13 (605). [PMID:34257144]

  • An Oral SARS-CoV-2 Mpro Inhibitor Clinical Candidate for the Treatment of COVID-19.
    Owen DR, Allerton CMN, Anderson AS, Aschenbrenner L, Avery M, Berritt S, Boras B, Cardin RD, Carlo A, Karen Coffman et al.. An Oral SARS-CoV-2 Mpro Inhibitor Clinical Candidate for the Treatment of COVID-19. (2021)  Science, Epub ahead of print. DOI: 10.1126/science.abl4784

  • Human embryonic stem cell-derived cardiomyocyte platform screens inhibitors of SARS-CoV-2 infection.
    Williams TL, Colzani MT, Macrae RGC, Robinson EL, Bloor S, Greenwood EJD, Zhan JR, Strachan G, Kuc RE, Nyimanu D et al.. Human embryonic stem cell-derived cardiomyocyte platform screens inhibitors of SARS-CoV-2 infection. (2021)  Commun Biol, 4 (1): 926. [PMID:34326460]

  • Discovering and Summarizing Relationships Between Chemicals, Genes, Proteins, and Diseases in PubChem.
    Zaslavsky L, Cheng T, Gindulyte A, He S, Kim S, Li Q, Thiessen P, Yu B, Bolton EE. Discovering and Summarizing Relationships Between Chemicals, Genes, Proteins, and Diseases in PubChem. (2021)  Front Res Metr Anal, 6: 689059. [PMID:34322655]

  • Hot Topics: Trends in kinase drug discovery: twenty years of successfully targeting the kinome

    Comments by Misty Attwood and Helgi Schiöth, University of Uppsala, Uppsala, Sweden.

    The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology area and beyond.. Read the full article on our blog

  • Sphingomyelin synthase related protein is a mammalian phosphatidylethanolamine phospholipase C.
    Chiang YP, Li Z, Chen Y, Cao Y, Jiang XC. Sphingomyelin synthase related protein is a mammalian phosphatidylethanolamine phospholipase C. (2021)  Biochim Biophys Acta Mol Cell Biol Lipids, 1866 (11): 159017 [Epub ahead of print]. [PMID:34332077]

  • Gene name errors: Lessons not learned
    Abeysooriya M, Soria M, Kasu MS, Ziemann M. Gene name errors: Lessons not learned. (2021)  PLoS Comput Biol, 17 (7): e1008984 [Epub ahead of print]. [PMID:34329294]
    Lewis D. Autocorrect errors in Excel still creating genomics headache. (2021)  Nature, [Epub ahead of print]. [PMID:34389840]

  • GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain.
    Leurs U, Klein AB, McSpadden ED, Griem-Krey N, Solbak SMØ, Houlton J, Villumsen IS, Vogensen SB, Hamborg L, Gauger SJ et al.. GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain. (2021)  Proc Natl Acad Sci U S A, 118 (31). [PMID:34330837]

  • Counteracting age-related VEGF signaling insufficiency promotes healthy aging and extends life span.
    Grunewald M, Kumar S, Sharife H, Volinsky E, Gileles-Hillel A, Licht T, Permyakova A, Hinden L, Azar S, Friedmann Y et al.. Counteracting age-related VEGF signaling insufficiency promotes healthy aging and extends life span. (2021)  Science, 373 (6554). [PMID:34326210]

  • Nuclear accumulation of CHMP7 initiates nuclear pore complex injury and subsequent TDP-43 dysfunction in sporadic and familial ALS.
    Coyne AN, Baskerville V, Zaepfel BL, Dickson DW, Rigo F, Bennett F, Lusk CP, Rothstein JD. Nuclear accumulation of CHMP7 initiates nuclear pore complex injury and subsequent TDP-43 dysfunction in sporadic and familial ALS. (2021)  Sci Transl Med, 13 (604). [PMID:34321318]

  • July 2021


  • The PROTACtable genome.
    Schneider M, Radoux CJ, Hercules A, Ochoa D, Dunham I, Zalmas LP, Hessler G, Ruf S, Shanmugasundaram V, Hann MM et al.. The PROTACtable genome. (2021)  Nat Rev Drug Discov, [Epub ahead of print]. [PMID:34285415]

  • Identifying the core concepts of pharmacology education.
    White PJ, Davis EA, Santiago M, Angelo T, Shield A, Babey AM, Kemp-Harper B, Maynard G, Al-Sallami HS, Musgrave IF et al.. Identifying the core concepts of pharmacology education. (2021)  Pharmacol Res Perspect, 9 (4): e00836. [PMID:34288559]

  • Sulfatides are endogenous ligands for the TLR4-MD-2 complex.
    Su L, Athamna M, Wang Y, Wang J, Freudenberg M, Yue T, Wang J, Moresco EMY, He H, Zor T et al.. Sulfatides are endogenous ligands for the TLR4-MD-2 complex. (2021)  Proc Natl Acad Sci U S A, 118 (30). [PMID:34290146]

  • Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2.
    Drayman N, DeMarco JK, Jones KA, Azizi SA, Froggatt HM, Tan K, Maltseva NI, Chen S, Nicolaescu V, Dvorkin S et al.. Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. (2021)  Science, [Epub ahead of print]. [PMID:34285133]

  • Toward predicting CYP2D6-mediated variable drug response from CYP2D6 gene sequencing data.
    van der Lee M, Allard WG, Vossen RHAM, Baak-Pablo RF, Menafra R, Deiman BALM, Deenen MJ, Neven P, Johansson I, Gastaldello S et al.. Toward predicting CYP2D6-mediated variable drug response from CYP2D6 gene sequencing data. (2021)  Sci Transl Med, 13 (603). [PMID:34290055]

  • The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance.
    Murithi JM, Pascal C, Bath J, Boulenc X, Gnädig NF, Pasaje CFA, Rubiano K, Yeo T, Mok S, Klieber S et al.. The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance. (2021)  Sci Transl Med, 13 (603). [PMID:34290058]

  • Molecular topography of an entire nervous system.
    Taylor SR, Santpere G, Weinreb A, Barrett A, Reilly MB, Xu C, Varol E, Oikonomou P, Glenwinkel L, McWhirter R et al.. Molecular topography of an entire nervous system. (2021)  Cell, [Epub ahead of print]. [PMID:34237253]

  • Structure of human Cav2.2 channel blocked by the painkiller ziconotide.
    Gao S, Yao X, Yan N. Structure of human Cav2.2 channel blocked by the painkiller ziconotide. (2021)  Nature, [Epub ahead of print]. [PMID:34234349]

  • Mapping the human genetic architecture of COVID-19.
    COVID-19 Host Genetics Initiative. Mapping the human genetic architecture of COVID-19. (2021)  Nature, [Epub ahead of print]. [PMID:34237774]

  • Structural mechanism of heat-induced opening of a temperature-sensitive TRP channel.
    Nadezhdin KD, Neuberger A, Trofimov YA, Krylov NA, Sinica V, Kupko N, Vlachova V, Zakharian E, Efremov RG, Sobolevsky AI. Structural mechanism of heat-induced opening of a temperature-sensitive TRP channel. (2021)  Nat Struct Mol Biol, 28 (7): 564-572. [PMID:34239124]

  • Heat-dependent opening of TRPV1 in the presence of capsaicin.
    Kwon DH, Zhang F, Suo Y, Bouvette J, Borgnia MJ, Lee SY. Heat-dependent opening of TRPV1 in the presence of capsaicin. (2021)  Nat Struct Mol Biol, 28 (7): 554-563. [PMID:34239123]

  • 2020 in review: FDA approvals of new medicines.
    Kinch MS, Kraft Z, Schwartz T. 2020 in review: FDA approvals of new medicines. (2021)  Drug Discov Today, [Epub ahead of print]. [PMID:34252611]

  • Advancing human genetics research and drug discovery through exome sequencing of the UK Biobank.
    Szustakowski JD, Balasubramanian S, Kvikstad E, Khalid S, Bronson PG, Sasson A, Wong E, Liu D, Wade Davis J, Haefliger C et al.. Advancing human genetics research and drug discovery through exome sequencing of the UK Biobank. (2021)  Nat Genet, 53 (7): 942-948. [PMID:34183854]

  • Identification of new GLUT2-selective inhibitors through in silico ligand screening and validation in eukaryotic expression systems.
    Schmidl S, Ursu O, Iancu CV, Oreb M, Oprea TI, Choe JY. Identification of new GLUT2-selective inhibitors through in silico ligand screening and validation in eukaryotic expression systems. (2021)  Sci Rep, 11 (1): 13751. [PMID:34215797]

  • Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2
    Lowe D. Drug Repurposing for Coronaviruses: Be Careful.  In the Pipeline, https://blogs.sciencemag.org/pipeline/archives/2021/06/25/drug-repurposing-for-coronaviruses-be-careful
    Tummino TA, Rezelj VV, Fischer B, Fischer A, O'Meara MJ, Monel B, Vallet T, White KM, Zhang Z, Alon A et al.. Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2. (2021)  Science, 373 (6554): 541-547. [PMID:34326236]

  • The language of race, ethnicity, and ancestry in human genetic research.
    Birney E, Inouye M, Raff J, Rutherford A, Scally A. The language of race, ethnicity, and ancestry in human genetic research. (2021)  arXiv, Preprint.

  • June 2021


  • Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4.
    Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X et al.. Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4. (2021)  Nature, [Epub ahead of print]. [PMID:34135510]

  • Structures of human mGlu2 and mGlu7 homo- and heterodimers.
    Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T et al.. Structures of human mGlu2 and mGlu7 homo- and heterodimers. (2021)  Nature, [Epub ahead of print]. [PMID:34135509]

  • SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation.
    Sanders DW, Jumper CC, Ackerman PJ, Bracha D, Donlic A, Kim H, Kenney D, Castello-Serrano I, Suzuki S, Tamura T et al.. SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation. (2021)  Elife, 10. [PMID:33890572]

  • Structural basis of omega-3 fatty acid transport across the blood-brain barrier.
    Cater RJ, Chua GL, Erramilli SK, Keener JE, Choy BC, Tokarz P, Chin CF, Quek DQY, Kloss B, Pepe JG et al.. Structural basis of omega-3 fatty acid transport across the blood-brain barrier. (2021)  Nature, [Epub ahead of print]. [PMID:34135507]

  • A Promising Chemical Series of Positive Allosteric Modulators of the μ-Opioid Receptor that Enhance the Antinociceptive Efficacy of Opioids but not their Adverse Effects.
    Pryce KD, Kang HJ, Sakloth F, Liu Y, Khan S, Toth K, Kapoor A, Nicolais A, Che T, Qin L et al.. A Promising Chemical Series of Positive Allosteric Modulators of the μ-Opioid Receptor that Enhance the Antinociceptive Efficacy of Opioids but not their Adverse Effects. (2021)  Neuropharmacology, In Press. DOI: 10.1016/j.neuropharm.2021.108673

  • The Problems of Applying Classical Pharmacology Analysis to Modern In Vitro Drug Discovery Assays: Slow Binding Kinetics and High Target Concentration.
    Hoare SRJ. The Problems of Applying Classical Pharmacology Analysis to Modern In Vitro Drug Discovery Assays: Slow Binding Kinetics and High Target Concentration. (2021)  SLAS Discov,: 24725552211019653 [Epub ahead of print]. [PMID:34112012]

  • Landmark Alzheimer's drug approval confounds research community.
    Mullard A. Landmark Alzheimer's drug approval confounds research community. (2021)  Nature, [Epub ahead of print]. [PMID:34103732]

  • Rationality over fashion and hype in drug design.
    Medina-Franco JL, Martinez-Mayorga K, Fernández-de Gortari E, Kirchmair J, Bajorath J. Rationality over fashion and hype in drug design. (2021)  F1000Res, Preprint. DOI: 10.12688/f1000research.52676.1

  • Spread of a SARS-CoV-2 variant through Europe in the summer of 2020.
    Hodcroft EB, Zuber M, Nadeau S, Vaughan TG, Crawford KHD, Althaus CL, Reichmuth ML, Bowen JE, Walls AC, Corti D et al.. Spread of a SARS-CoV-2 variant through Europe in the summer of 2020. (2021)  Nature, [Epub ahead of print]. [PMID:34098568]

  • Genome-wide analysis in 756,646 individuals provides first genetic evidence that ACE2 expression influences COVID-19 risk and yields genetic risk scores predictive of severe disease.
    Horowitz JE, Kosmicki JA, Damask A, Sharma D, Roberts GHL, Justice AE, Banerjee N, Coignet MV, Yadav A, Leader JB et al.. Genome-wide analysis in 756,646 individuals provides first genetic evidence that ACE2 expression influences COVID-19 risk and yields genetic risk scores predictive of severe disease. (2021)  medrxiv, Preprint. DOI: 10.1101/2020.12.14.20248176

  • May 2021


  • Pharmacogenetics at Scale: An Analysis of the UK Biobank.
    McInnes G, Lavertu A, Sangkuhl K, Klein TE, Whirl-Carrillo M, Altman RB. Pharmacogenetics at Scale: An Analysis of the UK Biobank. (2021)  Clin Pharmacol Ther, 109 (6): 1528-1537. [PMID:33237584]

  • Assessing the functional relevance of splice isoforms.
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