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The GtoMPdb contains data detailing the parasitic lifecycle activity for antimalarial ligands and their target interactions. Top-level Plasmodium lifecycle stages (collective categories for one or more developmental forms of the parasite) have been defined by GtoMPdb against which interactions in the database have been annotated.
Each individual Parasite Lifecycle Stage page provides a detailed description of the stage and a table displaying all interactions (contained in the database) associated with it.
✖Stage ID: | 4 | |
Name: | Plasmodium sexual blood stage (gametocyte) | |
Associated with: | 8 targets | |
18 ligands |
Description |
The lifecycle stage during which a small percentage of merozoites commit to a cycle of sexual reproduction and differentiate into male or female gametocytes. It is this form of the parasite that is ingested in the vector's blood meal, leading to transmission back to the mosquito from the human host. The sexual blood stage can be further subdivided into stages I-V within the human host, with mature stage V gametocytes infective to the mosquito. Blocking development of the parasite during this stage prevents transmission from human to mosquito. |
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1. Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C et al.. (2019) Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci USA, 116 (14): 7015-7020. [PMID:30894487]
2. Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT et al.. (2018) UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria. Antimicrob Agents Chemother, 62 (9). [PMID:29941635]
3. Huang G, Murillo Solano C, Melendez J, Shaw J, Collins J, Banks R, Arshadi AK, Boonhok R, Min H, Miao J et al.. (2020) Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines. J Med Chem, 63 (20): 11756-11785. [PMID:32959656]
4. Huang Z, Li R, Tang T, Ling D, Wang M, Xu D, Sun M, Zheng L, Zhu F, Min H et al.. (2020) A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1. Cell Discov, 6 (1): 93. [PMID:33311461]
5. Jennison C, Lucantoni L, O'Neill MT, McConville R, Erickson SM, Cowman AF, Sleebs BE, Avery VM, Boddey JA. (2019) Inhibition of Plasmepsin V Activity Blocks Plasmodium falciparum Gametocytogenesis and Transmission to Mosquitoes. Cell Rep, 29 (12): 3796-3806.e4. [PMID:31851913]
6. Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V et al.. (2016) Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature, 538 (7625): 344-349. [PMID:27602946]
7. Krishnan K, Ziniel P, Li H, Huang X, Hupalo D, Gombakomba N, Guerrero SM, Dotrang T, Lu X, Caridha D et al.. (2020) Torin 2 Derivative, NCATS-SM3710, Has Potent Multistage Antimalarial Activity through Inhibition of P. falciparum Phosphatidylinositol 4-Kinase (Pf PI4KIIIβ). ACS Pharmacol Transl Sci, 3 (5): 948-964. [PMID:33073193]
8. Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A et al.. (2014) KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother, 58 (9): 5060-7. [PMID:24913172]
9. Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ et al.. (2016) Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med, 13 (10): e1002138. [PMID:27701420]
10. McNamara CW, Lee MC, Lim CS, Lim SH, Roland J, Simon O, Yeung BK, Chatterjee AK, McCormack SL, Manary MJ et al.. (2013) Targeting Plasmodium PI(4)K to eliminate malaria. Nature, 504 (7479): 248-253. [PMID:24284631]
11. Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE et al.. (2013) Quinolone-3-diarylethers: a new class of antimalarial drug. Sci Transl Med, 5 (177): 177ra37. [PMID:23515079]
12. Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ et al.. (2017) Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Sci Transl Med, 9 (387). [PMID:28446690]
13. Potluri V, Shandil RK, Gavara R, Sambasivam G, Campo B, Wittlin S, Narayanan S. (2020) Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J, 19 (1): 365. [PMID:33046062]
14. Schalkwijk J, Hermkens PHH, Dechering KJ, Bonnert RV. (2020) Pantothenamide analogues. Patent number: WO2020141155A1. Assignee: Medicines for Malaria Venture (MMV). Priority date: 31/12/2018. Publication date: 09/07/2020.
15. Sun W, Tanaka TQ, Magle CT, Huang W, Southall N, Huang R, Dehdashti SJ, McKew JC, Williamson KC, Zheng W. (2014) Chemical signatures and new drug targets for gametocytocidal drug development. Sci Rep, 4: 3743. [PMID:24434750]
16. Vaidya AB, Morrisey JM, Zhang Z, Das S, Daly TM, Otto TD, Spillman NJ, Wyvratt M, Siegl P, Marfurt J et al.. (2014) Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum. Nat Commun, 5: 5521. [PMID:25422853]
17. van Pelt-Koops JC, Pett HE, Graumans W, van der Vegte-Bolmer M, van Gemert GJ, Rottmann M, Yeung BK, Diagana TT, Sauerwein RW. (2012) The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector. Antimicrob Agents Chemother, 56 (7): 3544-8. [PMID:22508309]
18. Wang M, Tang T, Li R, Huang Z, Ling D, Zheng L, Ding Y, Liu T, Xu W, Zhu F et al.. (2022) Drug Repurposing of Quisinostat to Discover Novel Plasmodium falciparum HDAC1 Inhibitors with Enhanced Triple-Stage Antimalarial Activity and Improved Safety. J Med Chem, 65 (5): 4156-4181. [PMID:35175762]