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calpain 1

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Target not currently curated in GtoImmuPdb

Target id: 2336

Nomenclature: calpain 1

Family: C2: Calpain

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 714 11q13.1 CAPN1 calpain 1
Mouse - 713 19 4.34 cM Capn1 calpain 1
Rat - 713 1q43 Capn1 calpain 1
Previous and Unofficial Names Click here for help
calcium-activated neutral proteinase 1 | calpain mu-type | calpain-1 catalytic subunit | CANP | CANP 1 | Capa1 | micromolar-calpain | mu-calpain | muCANP | calpain 1, (mu/I) large subunit
Database Links Click here for help
Specialist databases
MEROPS C02.001 (Hs)
Other databases
Alphafold P07384 (Hs), O35350 (Mm), P97571 (Rn)
BRENDA 3.4.22.52
ChEMBL Target CHEMBL3891 (Hs), CHEMBL3747 (Rn)
Ensembl Gene ENSG00000014216 (Hs), ENSMUSG00000024942 (Mm), ENSRNOG00000020935 (Rn)
Entrez Gene 823 (Hs), 12333 (Mm), 29153 (Rn)
Human Protein Atlas ENSG00000014216 (Hs)
KEGG Enzyme 3.4.22.52
KEGG Gene hsa:823 (Hs), mmu:12333 (Mm), rno:29153 (Rn)
OMIM 114220 (Hs)
Pharos P07384 (Hs)
RefSeq Nucleotide NM_001198868 (Hs), NM_001198869 (Hs), NM_005186 (Hs), NM_001110504 (Mm), NM_007600 (Mm), NM_019152 (Rn)
RefSeq Protein NP_001185798 (Hs), NP_005177 (Hs), NP_001185797 (Hs), NP_031626 (Mm), NP_001103974 (Mm), NP_062025 (Rn)
UniProtKB P07384 (Hs), O35350 (Mm), P97571 (Rn)
Wikipedia CAPN1 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.22.52

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
compound 4b [PMID: 20690647] Small molecule or natural product Pig Inhibition 7.6 pKi 3
⤷ pKi 7.6 (Ki 2.3x10-8 M) [3]
calpeptin Peptide Click here for species-specific activity table Hs Inhibition 8.3 pIC50 2
⤷ pIC50 8.3 (IC50 5x10-9 M) [2]
Description: Inhibition of recombinant human calpain 1
mercaptoacrylate inhibitor of calpain 1 Small molecule or natural product Pig Inhibition 8.2 pIC50 1
⤷ pIC50 8.2 (IC50 6x10-9 M) [1]
GC-376 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 4
⤷ pIC50 7.1 (IC50 7.4x10-8 M) [4]
UAWJ9-36-3 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition <4.7 pIC50 4
⤷ pIC50 <4.7 (IC50 >2x10-5 M) [4]
Description: inactive
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0043312 neutrophil degranulation TAS
GO:1903238 positive regulation of leukocyte tethering or rolling ISO
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:1903238 positive regulation of leukocyte tethering or rolling ISO
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:1903238 positive regulation of leukocyte tethering or rolling ISO

References

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1. Adams SE, Parr C, Miller DJ, Allemann RK, Hallett MB. (2012) Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates. Medchemcomm, 3: 566 (Concise Article). DOI: 10.1039/C2MD00280A

2. Iqbal M, Messina PA, Freed B, Das M, Chatterjee S, Tripathy R, Ming Tao, Josef KA, Dembofsky B, Dunn D et al.. (1997) Subsite requirements for peptide aldehyde inhibitors of human calpain I. Bioorg Med Chem Lett, 7: 539-544. DOI: 10.1016/S0960-894X(97)00063-2

3. Ovat A, Li ZZ, Hampton CY, Asress SA, Fernández FM, Glass JD, Powers JC. (2010) Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. J Med Chem, 53 (17): 6326-36. [PMID:20690647]

4. Xia Z, Sacco M, Hu Y, Ma C, Meng X, Zhang F, Szeto T, Xiang Y, Chen Y, Wang J. (2021) Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir. ACS Pharmacol Transl Sci, 4 (4): 1408-1421. [PMID:34414360]

How to cite this page

C2: Calpain: calpain 1. Last modified on 26/08/2021. Accessed on 05/07/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2336.