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ST14 transmembrane serine protease matriptase

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Target id: 2418

Nomenclature: ST14 transmembrane serine protease matriptase

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 855 11q24.3 ST14 ST14 transmembrane serine protease matriptase
Mouse 1 855 9 16.61 cM St14 suppression of tumorigenicity 14 (colon carcinoma)
Rat - 855 8q13 St14 ST14 transmembrane serine protease matriptase
Previous and Unofficial Names Click here for help
epithin | HAI | matriptase/MT-SP1 | membrane-type serine protease | MT-SP1 | protease, serine, 14 (epithin) | Prss14 | serine protease 14 | SNC19 | suppression of tumorigenicity 14 | suppression of tumorigenicity 14 (colon carcinoma) | Tmprss14
Database Links Click here for help
Specialist databases
MEROPS S01.302 (Hs)
Other databases
Alphafold Q9Y5Y6 (Hs), P56677 (Mm)
BRENDA 3.4.21.109
CATH/Gene3D 2.60.120.290, 3.30.70.960
ChEMBL Target CHEMBL3018 (Hs), CHEMBL3745587 (Mm)
Ensembl Gene ENSG00000149418 (Hs), ENSMUSG00000031995 (Mm), ENSRNOG00000005903 (Rn)
Entrez Gene 6768 (Hs), 19143 (Mm), 114093 (Rn)
Human Protein Atlas ENSG00000149418 (Hs)
KEGG Enzyme 3.4.21.109
KEGG Gene hsa:6768 (Hs), mmu:19143 (Mm), rno:114093 (Rn)
OMIM 606797 (Hs)
Orphanet ORPHA179413 (Hs)
Pharos Q9Y5Y6 (Hs)
RefSeq Nucleotide NM_021978 (Hs), NM_011176 (Mm), NM_053635.2 (Rn)
RefSeq Protein NP_068813 (Hs), NP_035306 (Mm), NP_446087 (Rn)
UniProtKB Q9Y5Y6 (Hs), P56677 (Mm)
Wikipedia ST14 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.109

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
inhibitor 1 [Colombo et al., 2012] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 11.0 pKi 2
⤷ pKi 11.0 (Ki 1.1x10-11 M) [2]
I-432 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pKi 3
⤷ pKi 8.7 (Ki 2x10-9 M) [3]
N-0385 Peptide Click here for species-specific activity table Hs Inhibition 8.6 pKi 1
⤷ pKi 8.6 (Ki 2.6x10-9 M) [1]
compound 3 [PMID: 23849879] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 4
⤷ pIC50 6.2 (IC50 5.7x10-7 M) [4]
compound 4d [PMID: 25489658] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pIC50 5
⤷ pIC50 5.8 (IC50 1.42x10-6 M) [5]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Ichthyosis, congenital, autosomal recessive 11; ARCI11
Synonyms: Ichthyosis-hypotrichosis syndrome [Orphanet: ORPHA91132]
OMIM: 602400
Orphanet: ORPHA91132
Drugs:  Tazarotene

References

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1. Boudreault P-L, Colombo E, Leduc R, Marsault E, Plancq B, Richter M. (2019) Matriptase inhibitors and uses thereof. Patent number: US2019337981A1. Assignee: Neomed Institute. Priority date: 23/12/2016. Publication date: 07/11/2019.

2. Colombo E, Désilets A, Duchêne D, Chagnon F, Najmanovich R, Leduc R, Marsault E. (2012) Design and synthesis of potent, selective inhibitors of matriptase. ACS Med Chem Lett, 3 (7): 530-4. [PMID:24900505]

3. Pászti-Gere E, Czimmermann E, Ujhelyi G, Balla P, Maiwald A, Steinmetzer T. (2016) In vitro characterization of TMPRSS2 inhibition in IPEC-J2 cells. J Enzyme Inhib Med Chem, 31 (sup2): 123-129. [PMID:27277342]

4. Tan X, Furio L, Reboud-Ravaux M, Villoutreix BO, Hovnanian A, El Amri C. (2013) 1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases. Bioorg Med Chem Lett, 23 (16): 4547-51. [PMID:23849879]

5. Tan X, Soualmia F, Furio L, Renard JF, Kempen I, Qin L, Pagano M, Pirotte B, El Amri C, Hovnanian A et al.. (2015) Toward the first class of suicide inhibitors of kallikreins involved in skin diseases. J Med Chem, 58 (2): 598-612. [PMID:25489658]

How to cite this page

S1: Chymotrypsin: ST14 transmembrane serine protease matriptase . Last modified on 29/03/2022. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2418.