pantetheine has been researched along with diphosphoric-acid* in 1 studies
1 other study(ies) available for pantetheine and diphosphoric-acid
| Article | Year |
|---|---|
Design and synthesis of Coenzyme A analogues as Aurora kinase A inhibitors: An exploration of the roles of the pyrophosphate and pantetheine moieties.
Coenzyme A (CoA) is a highly selective inhibitor of the mitotic regulatory enzyme Aurora A kinase, with a novel mode of action. Herein we report the design and synthesis of analogues of CoA as inhibitors of Aurora A kinase. We have designed and synthesised modified CoA structures as potential inhibitors, combining dicarbonyl mimics of the pyrophosphate group with a conserved adenosine headgroup and different length pantetheine-based tail groups. An analogue with a -SH group at the end of the pantotheinate tail showed the best IC50, probably due to the formation of a covalent bond with Aurora A kinase Cys290. Topics: Aurora Kinase A; Coenzyme A; Diphosphates; Dose-Response Relationship, Drug; Drug Design; Humans; Models, Molecular; Molecular Structure; Pantetheine; Protein Kinase Inhibitors; Structure-Activity Relationship | 2020 |