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Literature summary for 3.4.21.109 extracted from

  • Colombo, E.; Désilets, A.; Duchêne, D.; Chagnon, F.; Najmanovich, R.; Leduc, R.; Marsault E.
    Design and synthesis of potent, selective inhibitors of matriptase (2012), ACS Med. Chem. Lett., 3, 530-534.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.109

Inhibitors

Inhibitors Comment Organism Structure
1-[(4S)-4-amino-5-(1,3-benzothiazol-2-yl)-5-oxopentyl]guanidine
-
 Homo sapiens
2-(L-alanyl-L-arginyl)-1,3-benzothiazole
-
 Homo sapiens
L-arginyl-L-glutaminyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-hydroxypentan-2-yl]-L-alaninamide
-
 Homo sapiens
L-arginyl-N1-[(2S)-1-[[(2R)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
-
 Homo sapiens
L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide docking of the inhibitor in the active site of matriptase, structure, overview Homo sapiens
L-arginyl-N1-[(2S)-1-[[(2S)-6-amino-1-(1,3-benzothiazol-2-yl)-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
-
 Homo sapiens
additional information design and synthesis of potent, selective inhibitors of matriptase, overview. Design of a class of potent and selective peptidomimetic inhibitors of matriptase based on the P4-P1 (Arg-Gln-Ala-Arg) portion of the activation peptide of matriptase, to which is linked a C-terminal serine trap in the form of a ketobenzothiazole group. The ketobenzothiazole serine trap is selected to form a covalent and reversible bond with the catalytic serine residue of the enzyme. Importance of stereochemistry at the P1 position for inhibitory potency Homo sapiens
N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8IU80 matriptase and matriptase-2
-

Synonyms

Synonyms Comment Organism
matriptase-2
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000011
-
 L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide matriptase, pH and temperature not specified in the publication Homo sapiens
0.000000088
-
 N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide matriptase, pH and temperature not specified in the publication Homo sapiens
0.0000014
-
 2-(L-alanyl-L-arginyl)-1,3-benzothiazole matriptase, pH and temperature not specified in the publication Homo sapiens
0.0000033
-
 L-arginyl-N1-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide matriptase-2, pH and temperature not specified in the publication Homo sapiens
0.0000046
-
 L-arginyl-N1-[(2S)-1-[[(2R)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide matriptase, pH and temperature not specified in the publication Homo sapiens
0.0000095
-
 L-arginyl-N1-[(2S)-1-[[(2S)-6-amino-1-(1,3-benzothiazol-2-yl)-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]-L-glutamamide matriptase, pH and temperature not specified in the publication Homo sapiens
0.000457
-
 1-[(4S)-4-amino-5-(1,3-benzothiazol-2-yl)-5-oxopentyl]guanidine matriptase, pH and temperature not specified in the publication Homo sapiens
0.0061
-
 L-arginyl-L-glutaminyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-hydroxypentan-2-yl]-L-alaninamide matriptase, pH and temperature not specified in the publication Homo sapiens