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coagulation factor XII

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Target not currently curated in GtoImmuPdb

Target id: 2361

Nomenclature: coagulation factor XII

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 615 5q35.3 F12 coagulation factor XII
Mouse - 597 13 B1 F12 coagulation factor XII (Hageman factor)
Rat - 595 17p14 F12 coagulation factor XII
Previous and Unofficial Names Click here for help
factor XII | FXII | HAF | hageman factor | coagulation factor XII (Hageman factor)
Database Links Click here for help
Specialist databases
MEROPS S01.211 (Hs)
Other databases
Alphafold P00748 (Hs), Q80YC5 (Mm), D3ZTE0 (Rn)
BRENDA 3.4.21.38
CATH/Gene3D 2.10.10.10
ChEMBL Target CHEMBL2821 (Hs)
Ensembl Gene ENSG00000131187 (Hs), ENSMUSG00000021492 (Mm), ENSRNOG00000015139 (Rn)
Entrez Gene 2161 (Hs), 58992 (Mm), 306761 (Rn)
Human Protein Atlas ENSG00000131187 (Hs)
KEGG Enzyme 3.4.21.38
KEGG Gene hsa:2161 (Hs), mmu:58992 (Mm), rno:306761 (Rn)
OMIM 610619 (Hs)
Orphanet ORPHA121663 (Hs)
Pharos P00748 (Hs)
RefSeq Nucleotide NM_000505 (Hs), NM_021489 (Mm), NM_001014006 (Rn)
RefSeq Protein NP_000496 (Hs), NP_067464 (Mm), NP_001014028 (Rn)
UniProtKB P00748 (Hs), Q80YC5 (Mm), D3ZTE0 (Rn)
Wikipedia F12 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.38

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
methyl 5-[(4-tert-butylbenzoyl)amino]-2H-1,2,4-triazole-3-carboxylate Small molecule or natural product Hs Inhibition 8.0 pIC50 1
⤷ pIC50 8.0 (IC50 1.04x10-8 M) [1]
Inhibitor Comments
Factor XIIa blocking antibody 3F7 is an inhibitor of FXIIa.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
garadacimab Peptide Hs Binding 9.8 pKd 2
⤷ pKd 9.8 (Kd 1.5x10-10 M) [2]
Description: Affinity of antibody VR115
anti-FXII nanobody N4-38 Peptide Hs Binding 8.5 pKd 3
⤷ pKd 8.5 (Kd 3.07x10-9 M) [3]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Angioedema, hereditary, type III; HAE3
Synonyms: Hereditary angioedema [Disease Ontology: DOID:14735]
Hereditary angioedema type 3 [Orphanet: ORPHA100054]
Disease Ontology: DOID:14735
OMIM: 610618
Orphanet: ORPHA100054
Disease:  Factor XII deficiency
Disease Ontology: DOID:2231
OMIM: 234000
Orphanet: ORPHA330

References

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1. Diamond SL. Factor XIIa 1536 HTS Dose Response Confirmation - BioAssay Summary. Accessed on 06/09/2013. Modified on 06/09/2013. PubChem, http://pubchem.ncbi.nlm.nih.gov/assay/assay.cgi?aid=852

2. Panousis C, Rayznam V, Nash A, Wilson M, Schmidbauer S, Nolte M. (2018) Nucleic acids encoding inhibitory anti-factor XII/XIIa monoclonal antibodies. Patent number: US9856325B2. Assignee: CSL Ltd, CSL Behring GmbH Deutschland. Priority date: 04/11/2016. Publication date: 04/06/2024.

3. Wang M, Xu P. (2021) Anti-fxii nanobody or antigen binding fragment thereof and use thereof. Patent number: WO2021253662A1. Assignee: Ningbo Kangshan Biotechnology Co., Ltd.. Priority date: 21/09/2020. Publication date: 23/12/2021.

How to cite this page

S1: Chymotrypsin: coagulation factor XII. Last modified on 04/06/2024. Accessed on 04/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2361.