EC Number   |
Inhibitors |
Structure |
|---|
   3.4.21.B10 | 2-benzyl 1-[3-[(benzyloxy)carbonyl]phenyl] (2S,3S)-3-(4-hydroxybenzyl)-4-oxoazetidine-1,2-dicarboxylate |
- |
   |
| 3.4.21.B10 | 2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-3'-carbamoyl-6-hydroxybiphenyl-3-yl]butanedioic acid |
- |
|
| 3.4.21.B10 | 2-[[4-(aminomethyl)phenyl]carbamoyl]-1-[(1-benzyl-1H-imidazol-2-yl)methyl]-3-hydroxypyridinium |
crystal structure analysis of enzyme bound to inhibitor 2-[[4-(aminomethyl)phenyl]carbamoyl]-1-[(1-benzyl-1H-imidazol-2-yl)methyl]-3-hydroxypyridinium, two adjacent beta-barrels connected with several alpha helices and turns, overview |
|
| 3.4.21.B10 | 3-[[N-[[4-(aminomethyl)cyclohexyl]carbonyl]-O-(pyrimidin-2-yl)tyrosyl]amino]benzoic acid |
- |
|
| 3.4.21.B10 | 4,4'-[benzene-1,4-diylbis(methanediyloxy)]bis(3-iodobenzenecarboximidamide) |
- |
|
| 3.4.21.B10 | 4,4'-[pentane-1,5-diylbis(oxy)]bis(3,5-dibromobenzenecarboximidamide) |
- |
|
| 3.4.21.B10 | 4-amino-N-[4-(aminomethyl)phenyl]-2-hydroxybenzamide |
- |
|
| 3.4.21.B10 | Abz-Phe-Arg-Lys-Gln-EDDnp |
- |
|
| 3.4.21.B10 | alpha2-Macroglobulin |
- |
|
| 3.4.21.B10 | amyloid precursor protein Kunitz protease inhibitor domain |
combinatorial approach to engineering KLK6 inhibitors via flow cytometry-based screening of a yeast-displayed mutant library of the human amyloid precursor protein Kunitz protease inhibitor domain (APPI). On the basis of this screening, APPI(M17L/I18F/S19F/F34V) (APPI-4M) is generated, an APPI variant with a KLK6 inhibition constant (Ki) of 160 pM and a turnover time of 10 days. APPI-4M is a potent KLK6 inhibitor, displaying 146fold improved affinity and 13fold improved proteolytic stability compared with wild-type APPI (APPIWT). It is demonstrated that APPI-4M acts as a functional inhibitor in a cell-based model of KLK6-dependent breast cancer invasion |
|
