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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 638 | 4q35.2 | KLKB1 | kallikrein B1 | |
Mouse | - | 638 | 8 25.17 cM | Klkb1 | kallikrein B, plasma 1 | |
Rat | - | 638 | 16q11 | Klkb1 | kallikrein B1 |
Database Links | |
Specialist databases | |
MEROPS | S01.212 (Hs) |
Other databases | |
Alphafold | P03952 (Hs), P26262 (Mm), P14272 (Rn) |
BRENDA | 3.4.21.34 |
ChEMBL Target | CHEMBL2000 (Hs), CHEMBL1250359 (Mm), CHEMBL4105792 (Rn) |
Ensembl Gene | ENSG00000164344 (Hs), ENSMUSG00000109764 (Mm), ENSRNOG00000014118 (Rn) |
Entrez Gene | 3818 (Hs), 16621 (Mm), 25048 (Rn) |
Human Protein Atlas | ENSG00000164344 (Hs) |
KEGG Enzyme | 3.4.21.34 |
KEGG Gene | hsa:3818 (Hs), mmu:16621 (Mm), rno:25048 (Rn) |
OMIM | 229000 (Hs) |
Orphanet | ORPHA122872 (Hs) |
Pharos | P03952 (Hs) |
RefSeq Nucleotide | NM_000892 (Hs), NM_008455 (Mm), NM_012725 (Rn) |
RefSeq Protein | NP_000883 (Hs), NP_032481 (Mm), NP_036857 (Rn) |
UniProtKB | P03952 (Hs), P26262 (Mm), P14272 (Rn) |
Wikipedia | KLKB1 (Hs) |
Enzyme Reaction | ||||
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Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Antibodies | |||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
Kallikrein is a therapeutic target for the treament of the inflammatory attacks that cause vascular and organ damage in hereditary angioedema (HAE) [4]. The small molecule inhibitor berotralstat and the monoclonal lanadelumab are already used clinically for this indication. A CRISPR-Cas9 KLKB1 gene-disrupting therapeutic is in develoment [4]. |
Immuno Process Associations | ||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||
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1. Davie RL, Edwards HJ, Evans DM, Hodgson ST, Stocks MJ, Smith AJ, Rushbrooke LJ, Pethen SJ, Roe MB, Clark DE et al.. (2022) Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema. J Med Chem, 65 (20): 13629-13644. [PMID:36251573]
2. Dilger AK, Pabbisetty KB, Corte JR, De Lucca I, Fang T, Yang W, Pinto DJP, Wang Y, Zhu Y, Mathur A et al.. (2022) Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy. J Med Chem, 65 (3): 1770-1785. [PMID:34494428]
3. Kotian PL, Babu YS, Wu M, Chintareddy VR, Kumar VS, Zhang W. (2015) Human plasma kallikrein inhibitors. Patent number: WO2015134998A1. Assignee: Biocryst Pharmaceuticals. Priority date: 07/03/2014. Publication date: 11/09/2015.
4. Longhurst HJ, Lindsay K, Petersen RS, Fijen LM, Gurugama P, Maag D, Butler JS, Shah MY, Golden A, Xu Y et al.. (2024) CRISPR-Cas9 In Vivo Gene Editing of KLKB1 for Hereditary Angioedema. N Engl J Med, 390 (5): 432-441. [PMID:38294975]
5. Partridge JR, Choy RM, Silva-Garcia A, Yu C, Li Z, Sham H, Metcalf B. (2019) Structures of full-length plasma kallikrein bound to highly specific inhibitors describe a new mode of targeted inhibition. J Struct Biol, 206 (2): 170-182. [PMID:30876891]
6. Sexton DJ, Viswanathan M. (2014) Plasma kallikrein binding proteins. Patent number: US8816055 B2. Assignee: Dyax Corp.. Priority date: 06/01/2011. Publication date: 26/08/2014.
7. Young WB, Rai R, Shrader WD, Burgess-Henry J, Hu H, Elrod KC, Sprengeler PA, Katz BA, Sukbuntherng J, Mordenti J. (2006) Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett, 16 (7): 2034-6. [PMID:16413183]
S1: Chymotrypsin: kallikrein B1. Last modified on 06/02/2024. Accessed on 04/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2379.