A prolyl endopeptidase FAP that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q12884]
EC 3.4.21.26; This protein enables 10 target(s): This protein is located in 11 target(s): This protein is active in 1 target(s): This protein is part of 1 target(s): This protein is involved in 14 target(s):
170 kDa melanoma membrane-bound gelatinase;
Dipeptidyl peptidase FAP;
3.4.14.5;
Fibroblast activation protein alpha;
FAPalpha;
Gelatine degradation protease FAP;
3.4.21.-;
Integral membrane serine protease;Research
Bioassay Publications (23)
Timeframe Studies on this Protein(%) All Drugs % pre-1990 0 (0.00) 18.7374 1990's 0 (0.00) 18.2507 2000's 6 (26.09) 29.6817 2010's 13 (56.52) 24.3611 2020's 4 (17.39) 2.80 Compounds (11)
Drugs with Inhibition Measurements
Drug Taxonomy Measurement Average (mM) Bioassay(s) Publication(s) sitagliptin Homo sapiens (human) IC50 52.6136 11 14 vildagliptin Homo sapiens (human) IC50 36.1225 8 12 talabostat Homo sapiens (human) IC50 0.0792 5 5 talabostat Homo sapiens (human) Ki 0.0355 2 2 linagliptin Homo sapiens (human) IC50 0.0799 2 2 kyp 2047 Homo sapiens (human) IC50 0.1000 1 1 bms 477118 Homo sapiens (human) IC50 860.5000 2 2 alogliptin Homo sapiens (human) IC50 556.6667 3 3 gosogliptin Homo sapiens (human) IC50 10.3000 1 1 anagliptin Homo sapiens (human) IC50 72.7000 1 1 mk-3102 Homo sapiens (human) IC50 67.0000 1 1 Drugs with Other Measurements
Drug Taxonomy Measurement Average (mM) Bioassay(s) Publication(s) n-carbobenzoxyglycyl-prolyl-4-methylcoumarinyl amide Homo sapiens (human) Km 103.0000 1 1 Enables
Target Category Definition protease binding molecular function Binding to a protease or a peptidase. [GOC:hjd] endopeptidase activity molecular function Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain. [http://merops.sanger.ac.uk/about/glossary.htm#ENDOPEPTIDASE] serine-type endopeptidase activity molecular function Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] integrin binding molecular function Binding to an integrin. [GOC:ceb] protein binding molecular function Binding to a protein. [GOC:go_curators] peptidase activity molecular function Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181] serine-type peptidase activity molecular function Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] dipeptidyl-peptidase activity molecular function Catalysis of the hydrolysis of N-terminal dipeptides from a polypeptide chain. [GOC:mb, https://www.ebi.ac.uk/merops/about/glossary.shtml#DIPEPTIDYL-PEPTIDASE] identical protein binding molecular function Binding to an identical protein or proteins. [GOC:jl] protein homodimerization activity molecular function Binding to an identical protein to form a homodimer. [GOC:jl] Located In
Target Category Definition extracellular space cellular component That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] cytoplasm cellular component The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] plasma membrane cellular component The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] focal adhesion cellular component A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] cell surface cellular component The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] membrane cellular component A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] lamellipodium cellular component A thin sheetlike process extended by the leading edge of a migrating cell or extending cell process; contains a dense meshwork of actin filaments. [ISBN:0815316194] lamellipodium membrane cellular component The portion of the plasma membrane surrounding a lamellipodium. [GOC:mah] ruffle membrane cellular component The portion of the plasma membrane surrounding a ruffle. [GOC:mah] apical part of cell cellular component The region of a polarized cell that forms a tip or is distal to a base. For example, in a polarized epithelial cell, the apical region has an exposed surface and lies opposite to the basal lamina that separates the epithelium from other tissue. [GOC:mah, ISBN:0815316194] basal part of cell cellular component The region of a cell situated near the base. For example, in a polarized epithelial cell, the basal surface rests on the basal lamina that separates the epithelium from other tissue. [GOC:mah, ISBN:0815316194] Active In
Target Category Definition plasma membrane cellular component The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] Part Of
Target Category Definition peptidase complex cellular component A protein complex which is capable of peptidase activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:1689240] Involved In
Target Category Definition angiogenesis biological process Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] proteolysis biological process The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] cell adhesion biological process The attachment of a cell, either to another cell or to an underlying substrate such as the extracellular matrix, via cell adhesion molecules. [GOC:hb, GOC:pf] regulation of collagen catabolic process biological process Any process that modulates the rate, frequency or extent of collagen catabolism. Collagen catabolism is the proteolytic chemical reactions and pathways resulting in the breakdown of collagen in the extracellular matrix. [GOC:BHF, GOC:dph, GOC:tb] negative regulation of extracellular matrix disassembly biological process Any process that decreases the rate, frequency or extent of extracellular matrix disassembly. Extracellular matrix disassembly is a process that results in the breakdown of the extracellular matrix. [GOC:BHF, GOC:dph, GOC:tb] endothelial cell migration biological process The orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:go_curators] proteolysis involved in protein catabolic process biological process The hydrolysis of a peptide bond or bonds within a protein as part of the chemical reactions and pathways resulting in the breakdown of a protein by individual cells. [GOC:ai, GOC:dph, GOC:tb] regulation of cell cycle biological process Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] regulation of fibrinolysis biological process Any process that modulates the frequency, rate or extent of fibrinolysis, an ongoing process that solubilizes fibrin, resulting in the removal of small blood clots. [GOC:ai] negative regulation of cell proliferation involved in contact inhibition biological process Any process that stops, prevents or reduces the rate or extent of cell proliferation in response to cell density. [GOC:dph] melanocyte proliferation biological process The multiplication or reproduction of melanocytes, resulting in the expansion of a cell population. A melanocyte is a pigment cell derived from the neural crest. It contains melanin-filled pigment granules, which give a brown to black appearance. [CL:0000148, GOC:uh, PMID:22637532] positive regulation of execution phase of apoptosis biological process Any process that activates or increases the frequency, rate or extent of execution phase of apoptosis. [GOC:mtg_apoptosis, GOC:TermGenie] melanocyte apoptotic process biological process Any apoptotic process in a melanocyte, the main structural component of the epidermis. [GOC:ic, GOC:TermGenie, PMID:20530876] negative regulation of extracellular matrix organization biological process Any process that stops, prevents or reduces the frequency, rate or extent of extracellular matrix organization. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:22357537]