Literature summary for 3.4.21.109 extracted from

Uhland, K.; Siphos, B.; Arkona, C.; Schuster, M.; Petri, B.; Steinmetzer, P.; Mueller, F.; Schweinitz, A.; Steinmetzer, T.; Van De Locht, A.
Use of IHC and newly designed matriptase inhibitors to elucidate the role of matriptase in pancreatic ductal adenocarcinoma (2009), Int. J. Oncol., 35, 347-357.

Search for more literature for 3.4.21.109

Inhibitors

Inhibitors	Comment	Organism	Structure
3-(3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl)benzenecarboximidamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
4-(1-[3-carbamimidoyl-N-[(4'-ethylbiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
4-([1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[(4-cyclohexylphenyl)sulfonyl]amino]propanoyl]piperidin-4-yl]carbonyl)piperidine-1-carboximidamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitor reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
benzyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
N-(3-[[(2S)-1-[4-(2-aminoethyl)piperidin-1-yl]-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl]sulfamoyl]phenyl)-beta-alaninamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens
N-(3-[[(2S)-3-(3-carbamimidoylphenyl)-1-oxo-1-(piperazin-1-yl)propan-2-yl]sulfamoyl]phenyl)-beta-alaninamide	inhibitor completely prevents matriptase zymogen activation in human adenocarcinoma cell lines AsPC-1 and BxPC-3. Pro-urokinase-type plasminogen activator activation is completely abolished by matriptase inhibition. Matriptase inhibitors reduce the phosphorylation of the HGF receptor/cMet and the overall cellular invasiveness of the human pancreatic adenocarcinoma cell line AsPC-1	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
pancreatic duct	-	Homo sapiens	-
pancreatic ductal adenocarcinoma cell	using immunohistochemistry a significant overexpression of matriptase is shown in pancreatic carcinoma compared to normal pancreatic ducts	Homo sapiens	-
PC-1 cell	-	Homo sapiens	-
PC-3 cell	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
matriptase	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000001	-	3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-([[3-(6-amino-2,3,4,5-tetrahydropyridin-3-yl)phenyl]sulfonyl]amino)-3-oxopropyl]benzenecarboximidamide	-	Homo sapiens
0.0000025	-	3-(3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[(4'-ethylbiphenyl-3-yl)sulfonyl]amino]-3-oxopropyl)benzenecarboximidamide	-	Homo sapiens
0.0000038	-	N-(3-[[(2S)-1-[4-(2-aminoethyl)piperidin-1-yl]-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl]sulfamoyl]phenyl)-beta-alaninamide	-	Homo sapiens
0.0000061	-	benzyl 4-(N-[[3-(beta-alanylamino)phenyl]sulfonyl]-3-carbamimidoyl-L-phenylalanyl)piperazine-1-carboxylate	-	Homo sapiens
0.0000245	-	4-(1-[3-carbamimidoyl-N-[(4'-ethylbiphenyl-3-yl)sulfonyl]-L-phenylalanyl]piperidin-4-yl)-N-methylbutanamide	-	Homo sapiens
0.000026	-	4-([1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[(4-cyclohexylphenyl)sulfonyl]amino]propanoyl]piperidin-4-yl]carbonyl)piperidine-1-carboximidamide	-	Homo sapiens
0.000036	-	N-(3-[[(2S)-3-(3-carbamimidoylphenyl)-1-oxo-1-(piperazin-1-yl)propan-2-yl]sulfamoyl]phenyl)-beta-alaninamide	-	Homo sapiens

Expression

Organism	Comment	Expression
Homo sapiens	using immunohistochemistry a significant overexpression of matriptase is shown in pancreatic carcinoma compared to normal pancreatic ducts	up

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Release 2023.1 (January 2023)