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renin

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Target not currently curated in GtoImmuPdb

Target id: 2413

Nomenclature: renin

Family: A1: Pepsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 406 1q32.1 REN renin
Mouse - 402 1 57.91 cM Ren1 renin 1 structural
Rat - 402 13q13 Ren renin
Previous and Unofficial Names Click here for help
angiotensinogenase | aspartyl-protease | kidney renin | Ren1 | Ren-A | RENAA | renin b | Rnr
Database Links Click here for help
Specialist databases
MEROPS A01.007 (Hs)
Other databases
Alphafold P00797 (Hs), P06281 (Mm), P08424 (Rn)
BRENDA 3.4.23.15
CATH/Gene3D 2.40.70.10
ChEMBL Target CHEMBL286 (Hs), CHEMBL2615 (Mm), CHEMBL2322 (Rn)
DrugBank Target P00797 (Hs)
Ensembl Gene ENSG00000143839 (Hs), ENSMUSG00000070645 (Mm), ENSRNOG00000002937 (Rn)
Entrez Gene 5972 (Hs), 19701 (Mm), 24715 (Rn)
Human Protein Atlas ENSG00000143839 (Hs)
KEGG Enzyme 3.4.23.15
KEGG Gene hsa:5972 (Hs), mmu:19701 (Mm), rno:24715 (Rn)
OMIM 179820 (Hs)
Orphanet ORPHA138530 (Hs)
Pharos P00797 (Hs)
RefSeq Nucleotide NM_000537 (Hs), NM_031192 (Mm), NM_012642 (Rn)
RefSeq Protein NP_000528 (Hs), NP_112469 (Mm), NP_036774 (Rn)
SynPHARM 78508 (in complex with aliskiren)
UniProtKB P00797 (Hs), P06281 (Mm), P08424 (Rn)
Wikipedia REN (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.23.15

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
sitokiren Small molecule or natural product Hs Inhibition 9.4 pIC50 1
⤷ pIC50 9.4 (IC50 4x10-10 M) [1]
Description: Inhibition of recombinant human renin in vitro
aliskiren Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.2 pIC50 2
⤷ pIC50 9.2 (IC50 6x10-10 M) [2]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Hyperuricemic nephropathy, familial juvenile 2; HNFJ2
Synonyms: Familial juvenile hyperuricemic nephropathy [Disease Ontology: DOID:0060062]
Hyperuricemia - anemia - renal failure [Orphanet: ORPHA217330]
Disease Ontology: DOID:0060062
OMIM: 613092
Orphanet: ORPHA217330
Disease:  Renal tubular dysgenesis
OMIM: 267430
Orphanet: ORPHA97369
General Comments
Cleaves the precursor angiotensinogen to generate angiotensin I.

References

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1. Iijima D, Sugama H, Takahashi Y, Hirai M, Togashi Y, Xie J, Shen J, Ke Y, Akatsuka H, Kawaguchi T et al.. (2022) Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor. J Med Chem, 65 (16): 10882-10897. [PMID:35939295]

2. Wuerzner G, Azizi M. (2008) Renin inhibition with aliskiren. Clin Exp Pharmacol Physiol, 35 (4): 426-30. [PMID:18307734]

How to cite this page

A1: Pepsin: renin. Last modified on 27/09/2022. Accessed on 25/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2413.