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Literature summary extracted from

  • Morreale, F.E.; Bortoluzzi, A.; Chaugule, V.K.; Arkinson, C.; Walden, H.; Ciulli, A.
    Allosteric targeting of the Fanconi anemia ubiquitin-conjugating enzyme Ube2T by fragment screening (2017), J. Med. Chem., 60, 4093-4098 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.3.2.23 drug development enzyme Ube2T represents an attractive target for the development of inhibitors. Modulation of DNA repair pathways is a strategy for the development of inhibitors of tumor cell growth, as it can either potentiate the effects of radiotherapy and conventional genotoxins or exploit synthetic lethal interactions Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.3.2.23 Ube2T in complex with inhibitor 1-(1,3-benzothiazol-2-yl)methanamine, X-ray diffraction crystal structure analysis, PDB ID 5NGZ Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.23 1-(1,3-benzothiazol-2-yl)methanamine i.e. EM04, about 40% inhibition of FANCD2 ubiquination Homo sapiens
2.3.2.23 2-amino-5-phenylfuran-3-carbonitrile i.e. EM11, about 25% inhibition of FANCD2 ubiquination Homo sapiens
2.3.2.23 3-methyl-3,4-dihydroquinazolin-2(1H)-one i.e. EM09, about 15% inhibition of FANCD2 ubiquination Homo sapiens
2.3.2.23 4-phenyl-1,3-thiazol-2-amine i.e. EM17, about 60% inhibition of FANCD2 ubiquination Homo sapiens
2.3.2.23 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EM02, almost complete inhibition of FANCD2 ubiquination Homo sapiens
2.3.2.23 additional information 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) Homo sapiens

Natural Substrates/ Products (Substrates)

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
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.23 Homo sapiens Q9NPD8
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.2.23 carcinoma cell Ube2T is overexpressed in several cancers Homo sapiens
-

Substrates and Products (Substrate)

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
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.2.23 Ube2J1
-
 Homo sapiens
2.3.2.23 UBE2T
-
 Homo sapiens
2.3.2.23 ubiquitin-conjugating enzyme
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.3.2.23 metabolism Ube2T is the E2 ubiquitin-conjugating enzyme of the Fanconi anemia DNA repair pathway Homo sapiens
2.3.2.23 additional information the catalytic cysteine is C86 Homo sapiens
2.3.2.23 physiological function Ube2T is the E2 ubiquitin-conjugating enzyme of the Fanconi anemia DNA repair pathway. Together with FANCL (the E3 ligase), Ube2T catalyzes the monoubiquitination of the heterodimeric FANCI/FANCD2 complex, which is the key signaling event to activate the FA pathway for DNA repair Homo sapiens