Target Information
| Target General Information | Top | |||||
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| Target ID |
T75772
(Former ID: TTDNR00667)
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| Target Name |
Enteropeptidase (TMPRSS15)
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| Synonyms |
Transmembrane protease serine 15; TMPRSS15; Serine protease 7; Enterokinase
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| Gene Name |
TMPRSS15
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| Target Type |
Patented-recorded target
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[1] | ||||
| Function |
Responsible for initiating activation of pancreatic proteolytic proenzymes (trypsin, chymotrypsin and carboxypeptidase A). It catalyzes the conversion of trypsinogen to trypsin which in turn activates other proenzymes including chymotrypsinogen, procarboxypeptidases, and proelastases.
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| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| EC Number |
EC 3.4.21.9
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| Sequence |
MGSKRGISSRHHSLSSYEIMFAALFAILVVLCAGLIAVSCLTIKESQRGAALGQSHEARA
TFKITSGVTYNPNLQDKLSVDFKVLAFDLQQMIDEIFLSSNLKNEYKNSRVLQFENGSII VVFDLFFAQWVSDENVKEELIQGLEANKSSQLVTFHIDLNSVDILDKLTTTSHLATPGNV SIECLPGSSPCTDALTCIKADLFCDGEVNCPDGSDEDNKMCATVCDGRFLLTGSSGSFQA THYPKPSETSVVCQWIIRVNQGLSIKLSFDDFNTYYTDILDIYEGVGSSKILRASIWETN PGTIRIFSNQVTATFLIESDESDYVGFNATYTAFNSSELNNYEKINCNFEDGFCFWVQDL NDDNEWERIQGSTFSPFTGPNFDHTFGNASGFYISTPTGPGGRQERVGLLSLPLDPTLEP ACLSFWYHMYGENVHKLSINISNDQNMEKTVFQKEGNYGDNWNYGQVTLNETVKFKVAFN AFKNKILSDIALDDISLTYGICNGSLYPEPTLVPTPPPELPTDCGGPFELWEPNTTFSST NFPNSYPNLAFCVWILNAQKGKNIQLHFQEFDLENINDVVEIRDGEEADSLLLAVYTGPG PVKDVFSTTNRMTVLLITNDVLARGGFKANFTTGYHLGIPEPCKADHFQCKNGECVPLVN LCDGHLHCEDGSDEADCVRFFNGTTNNNGLVRFRIQSIWHTACAENWTTQISNDVCQLLG LGSGNSSKPIFPTDGGPFVKLNTAPDGHLILTPSQQCLQDSLIRLQCNHKSCGKKLAAQD ITPKIVGGSNAKEGAWPWVVGLYYGGRLLCGASLVSSDWLVSAAHCVYGRNLEPSKWTAI LGLHMKSNLTSPQTVPRLIDEIVINPHYNRRRKDNDIAMMHLEFKVNYTDYIQPICLPEE NQVFPPGRNCSIAGWGTVVYQGTTANILQEADVPLLSNERCQQQMPEYNITENMICAGYE EGGIDSCQGDSGGPLMCQENNRWFLAGVTSFGYKCALPNRPGVYARVSRFTEWIQSFLH Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: 4-Guanidinobenzoic acid | Ligand Info | |||||
| Structure Description | ENTEROPEPTIDASE IN COMPLEX WITH COMPOUND 6 | PDB:6ZOV | ||||
| Method | X-ray diffraction | Resolution | 2.19 Å | Mutation | Yes | [7] |
| PDB Sequence |
IVGGSDAKEG
10 AWPWVVGLYY20 DDRLLCGASL30 VSSDWLVSAA40 HCVYGRNLEP50 SKWTAILGLH 60 MKSNLTSPQT70 VPRLIDEIVI80 NPHYNRRRKD90 NDIAMMHLEF100 KVNYTDYIQP 110 ISLPEENQVF120 PPGRNCSIAG130 WGTVVYQGTT140 ADILQEADVP150 LLSNERCQQQ 160 MPEYNITENM170 ICAGYEEGGI180 DSCQGDSGGP190 LMCQENNRWF200 LAGVTSFGYE 210 CALPNRPGVY220 ARVSRFTEWI230 QSFL
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HIS41
4.244
ASP181
3.125
SER182
3.484
CYS183
3.695
GLN184
3.388
GLY185
3.660
ASP186
4.403
SER187
1.457
THR205
3.736
SER206
3.892
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| T-cell differentiation antigen CD6 (TP120) | 32.000 (16/50) | 1.00E-03 |
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| References | Top | |||||
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| REF 1 | Enteropeptidase: a gene associated with a starvation human phenotype and a novel target for obesity treatment. PLoS One. 2012;7(11):e49612. | |||||
| REF 2 | Heteroarylcarboxylic acid ester derivative. US8609715. | |||||
| REF 3 | Heteroarylcarboxylic acid ester derivative. US9227949. | |||||
| REF 4 | Heteroarylcarboxylic acid ester derivative. US9655879. | |||||
| REF 5 | Heteroarylcarboxylic acid ester derivative. US9024044. | |||||
| REF 6 | Heterocyclic carboxylic acid ester derivative. US9346821. | |||||
| REF 7 | Targeting Enteropeptidase with Reversible Covalent Inhibitors To Achieve Metabolic Benefits. J Pharmacol Exp Ther. 2020 Dec;375(3):510-521. | |||||
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