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Literature summary extracted from

  • Qin, Z.; Cui, B.; Jin, J.; Song, M.; Zhou, B.; Guo, H.; Qian, D.; He, Y.; Huang, L.
    The ubiquitin-activating enzyme E1 as a novel therapeutic target for the treatment of restenosis (2016), Atherosclerosis, 247, 142-153 .
    View publication on PubMed

Application

EC Number Application Comment Organism
6.2.1.45 drug development the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis Homo sapiens
6.2.1.45 medicine the ubiquitin-activating enzyme E1 is a therapeutic target for the treatment of restenosis Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.2.1.45 PYR-41 an Uba1 inhibitor Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
6.2.1.45 Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine Homo sapiens
-
 AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.2.1.45 Homo sapiens P22314
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.2.1.45 ATP + ubiquitin + [E1 ubiquitin-activating enzyme]-L-cysteine
-
 Homo sapiens AMP + diphosphate + S-ubiquitinyl-[E1 ubiquitin-activating enzyme]-L-cysteine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.2.1.45 E1
-
 Homo sapiens
6.2.1.45 Uba1
-
 Homo sapiens
6.2.1.45 ubiquitin-activating enzyme E1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
6.2.1.45 ATP
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
6.2.1.45 malfunction local delivery of potent chemical UBA1 inhibitor PYR-41 and UBA1 shRNA lentivirus both result in a substantial decrease in intimal hyperplasia at 2 weeks and 4 weeks after balloon injury. UBA1 inhibition also reduces Ki-67 positive cell percentage and inflammatory response in the carotid artery wall. In vitro UBA1 inhibition is able to ameliorate TNF-alpha-induced nuclear factor-kappa B (NF-kappaB) activation by reducing IkappaB degradation in vascular smooth muscle cells (VSMCs). UBA1 inhibition also leads to the accumulation of short-lived proteins such as p53, p21 and c-jun, which may account for the UBA1 inhibition-induced cell cycle delay. Thus, VSMCs proliferation is blocked. UBA1 inhibition effectively suppresses neointimal thickening through its anti-proliferative and anti-inflammatory effects Homo sapiens
6.2.1.45 metabolism the ubiquitin-activating enzyme E1 (UBA1, E1) is the apex of the ubiquitin proteasome pathway Homo sapiens
6.2.1.45 physiological function the ubiquitin-activating enzyme E1 (UBA1) plays a critical role in protein degradation and in pathological processes. UBA1 participates the development of vascular restenosis Homo sapiens