EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
2.3.2.23 | 3-(2-hydroxyphenyl)pyridin-2(1H)-one | - |
Homo sapiens | |
2.3.2.23 | 5,6-dibenzo[c,e][1,2]thiazine-5,5(6H)-dione | - |
Homo sapiens | |
2.3.2.23 | 5-chloro-1,3-benzoxazole-2-thiol | - |
Homo sapiens | |
2.3.2.23 | 6-chloro-1,3-benzoxazole-2-thiol | - |
Homo sapiens | |
2.3.2.23 | ethyl 3-(2,2'-dihydroxy[1,1'-biphenyl]-4-yl)propanoate | - |
Homo sapiens | |
2.3.2.23 | additional information | 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 | Homo sapiens | |
2.3.2.23 | [1,1'-biphenyl]-2,2'-diol | - |
Homo sapiens | |
2.3.2.23 | [1,1'-biphenyl]-2-ol | - |
Homo sapiens | |
2.3.2.23 | [1,1'-biphenyl]-2-sulfonamide | - |
Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
2.3.2.23 | S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine + [E2 ubiquitin-conjugating enzyme]-L-cysteine | Homo sapiens | - |
[E1 ubiquitin-activating enzyme]-L-cysteine + S-ubiquitinyl-[E2 ubiquitin-conjugating enzyme]-L-cysteine | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
2.3.2.23 | Homo sapiens | P63279 | - |
- |
EC Number | Posttranslational Modification | Comment | Organism |
---|---|---|---|
2.3.2.23 | sumoylation | conjugation of the small ubiquitin-like modifier (SUMO) to protein substrates is an important disease-associated posttranslational modification. The E2 enzyme Ubc9 is sumoylated | Homo sapiens |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
2.3.2.23 | S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine + [E2 ubiquitin-conjugating enzyme]-L-cysteine | - |
Homo sapiens | [E1 ubiquitin-activating enzyme]-L-cysteine + S-ubiquitinyl-[E2 ubiquitin-conjugating enzyme]-L-cysteine | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
2.3.2.23 | E2 enzyme | - |
Homo sapiens |
2.3.2.23 | SUMO E2 enzyme | - |
Homo sapiens |
2.3.2.23 | Ubc9 | - |
Homo sapiens |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
2.3.2.23 | 1.9 | - |
pH and temperature not specified in the publication | Homo sapiens | [1,1'-biphenyl]-2-ol | |
2.3.2.23 | 3 | - |
pH and temperature not specified in the publication | Homo sapiens | ethyl 3-(2,2'-dihydroxy[1,1'-biphenyl]-4-yl)propanoate | |
2.3.2.23 | 3 | - |
above, pH and temperature not specified in the publication | Homo sapiens | 6-chloro-1,3-benzoxazole-2-thiol | |
2.3.2.23 | 3 | - |
above, pH and temperature not specified in the publication | Homo sapiens | 5,6-dibenzo[c,e][1,2]thiazine-5,5(6H)-dione | |
2.3.2.23 | 3.1 | - |
pH and temperature not specified in the publication | Homo sapiens | [1,1'-biphenyl]-2-sulfonamide | |
2.3.2.23 | 5.8 | - |
pH and temperature not specified in the publication | Homo sapiens | [1,1'-biphenyl]-2,2'-diol | |
2.3.2.23 | 20 | - |
above, pH and temperature not specified in the publication | Homo sapiens | 3-(2-hydroxyphenyl)pyridin-2(1H)-one |
EC Number | General Information | Comment | Organism |
---|---|---|---|
2.3.2.23 | additional information | molecular dynamics simulations of Ubc9 | Homo sapiens |