EC Number   |
Inhibitors |
Structure  |
|---|
   2.3.2.23 | more |
allosteric inhibition of the SUMO E2 enzyme Ubc9. Identification of two distinct small molecule fragments that bind to Ubc9 at a site distal from its catalytic cysteine. These fragments and related compounds inhibit SUMO conjugation to the enzyme with IC50 values of 1.9-5.8 mM. Mechanistic and biophysical analyses, coupled with molecular dynamics simulations, point toward ligand-induced rigidification of Ubc9 as a mechanism of inhibition, overview |
 |
| 2.3.2.23 | more |
backside binding by accessory elements of the RING E3 Rad18 inhibits the intrinsic chain-forming activity of Ube2B; enzyme UBE2E1 performs autoubiquitylation, ubiquitylation results in inhibition of E2 activity; the backside-binding element of the E3 AO7 decreases the processivity of chain building by the E2 Ube2D2 |
|
| 2.3.2.23 | more |
identification of an allosteric pocket on Ube2T through a fragment screening using biophysical methods. Several fragments binding to this site inhibit ubiquitin conjugation in vitro. One-dimensional 1H NMR spectroscopy, binding site identification through protein-observed NMR spectroscopy, and X-ray crystallography, overview. No inhibition by 5-(pyridin-2-yl)thiophene-2-carboxamide (EM29) |
|
| 2.3.2.23 | more |
identification of ubiquitin variants that bind tightly and specifically to Ube2k at a hydrophobic cleft that is distinct from the active site and ubiquitin binding sites. The variants are potent inhibitors of Ube2k and block both ubiquitin charging of the E2 enzyme and E3-catalyzed ubiquitin transfer |
|
| 2.3.2.23 | more |
generation of ubiquitin variants that inhibit the E2 enzyme. The variants inhibit ubiquitin chain building, and bind to UB2D2 with low micromolar affinity and high specificity. The binding site overlaps with E1 binding, and the variants can have an additional binding site that blocks a critical non-covalent ubiquitin-binding site on the E2 enzyme |
|
| 2.3.2.23 | 4-phenyl-1,3-thiazol-2-amine |
i.e. EM17, about 60% inhibition of FANCD2 ubiquination |
  |
| 2.3.2.23 | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
i.e. EM02, almost complete inhibition of FANCD2 ubiquination |
|
| 2.3.2.23 | 1-(1,3-benzothiazol-2-yl)methanamine |
i.e. EM04, about 40% inhibition of FANCD2 ubiquination |
|
| 2.3.2.23 | 2-amino-5-phenylfuran-3-carbonitrile |
i.e. EM11, about 25% inhibition of FANCD2 ubiquination |
|
| 2.3.2.23 | 3-(2-hydroxyphenyl)pyridin-2(1H)-one |
- |
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