Reversible covalent inhibition of a phenol sulfotransferase by coenzyme A

2007 ◽  
Vol 457 (2) ◽  
pp. 197-204 ◽  
Author(s):  
Sundari Chodavarapu ◽  
Heather Hertema ◽  
Tien Huynh ◽  
Jessica Odette ◽  
Rachel Miller ◽  
...  
Keyword(s):  
Coenzyme A ◽  
Covalent Inhibition ◽  
Phenol Sulfotransferase ◽  
Reversible Covalent

scholarly journals Reversible Covalent Inhibition of eEF-2K by Carbonitriles

ChemBioChem ◽  
2014 ◽  
Vol 15 (16) ◽  
pp. 2435-2442 ◽  
Author(s):  
Ashwini K. Devkota ◽  
Ramakrishna Edupuganti ◽  
Chunli Yan ◽  
Yue Shi ◽  
Jiney Jose ◽  
...  
Keyword(s):  
Covalent Inhibition ◽  
Reversible Covalent

scholarly journals The Meisenheimer Complex as a Paradigm in Drug Discovery: Reversible Covalent Inhibition through C67 of the ATP Binding Site of PLK1

2018 ◽  
Vol 25 (9) ◽  
pp. 1107-1116.e4 ◽  
Author(s):  
Russell J. Pearson ◽  
David G. Blake ◽  
Mokdad Mezna ◽  
Peter M. Fischer ◽  
Nicholas J. Westwood ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Binding Site ◽  
Atp Binding ◽  
Atp Binding Site ◽  
Covalent Inhibition ◽  
Reversible Covalent

Reversible Covalent Inhibition of a Protein Target

2012 ◽  
Vol 51 (35) ◽  
pp. 8699-8700 ◽  
Author(s):  
Chang-Uk Lee ◽  
Tom N. Grossmann
Keyword(s):  
Protein Target ◽  
Covalent Inhibition ◽  
Reversible Covalent

ONIOM calculations on serotonin degradation by monoamine oxidase B: insight into the oxidation mechanism and covalent reversible inhibition

2016 ◽  
Vol 14 (39) ◽  
pp. 9239-9252 ◽  
Author(s):  
Kubra Cakir ◽  
Safiye Sag Erdem ◽  
Vildan Enisoglu Atalay
Keyword(s):  
Monoamine Oxidase ◽  
Oxidation Mechanism ◽  
Monoamine Oxidase B ◽  
Reversible Inhibition ◽  
Covalent Inhibition ◽  
Hybrid Mechanism ◽  
Reversible Covalent ◽  
Insight Into ◽  
Oniom Calculations

We propose a hybrid mechanism for MAO where the formation of FAD-N5-ylide causes a reversible covalent inhibition, which can be modulated for designing superior therapeutics.

Inhibition and Binding Studies of Coenzyme A and Bovine Phenol Sulfotransferase

1999 ◽  
Vol 261 (3) ◽  
pp. 815-819 ◽  
Author(s):  
Michael Leach ◽  
Emily Cameron ◽  
Nathan Fite ◽  
Jerry Stassinopoulos ◽  
Neal Palmreuter ◽  
...  
Keyword(s):  
Coenzyme A ◽  
Binding Studies ◽  
Phenol Sulfotransferase

ChemInform Abstract: Reversible Covalent Inhibition of a Protein Target

ChemInform ◽  
2012 ◽  
Vol 43 (49) ◽  
pp. no-no
Author(s):  
Chang-Uk Lee ◽  
Tom N. Grossmann
Keyword(s):  
Protein Target ◽  
Covalent Inhibition ◽  
Reversible Covalent

scholarly journals Covalent Aurora A regulation by the metabolic integrator coenzyme A

2018 ◽  
Author(s):  
Yugo Tsuchiya ◽  
Dominic P Byrne ◽  
Selena G Burgess ◽  
Jenny Bormann ◽  
Jovana Bakovic ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Coenzyme A ◽  
Covalent Bond ◽  
Aurora A ◽  
Cell Cycle Protein ◽  
Covalent Interaction ◽  
Oxidative Stresses ◽  
Cellular Analysis ◽  
Activation Segment ◽  
Reversible Covalent

SummaryAurora A is a cell cycle protein kinase implicated in multiple human cancers, and several Aurora A-specific kinase inhibitors have progressed into clinical trials. In this study, we report structural and cellular analysis of a novel biochemical mode of Aurora A inhibition, which occurs through reversible covalent interaction with the universal metabolic integrator coenzyme A (CoA). Mechanistically, the CoA 3’-phospho ADP moiety interacts with Thr 217, an Aurora A selectivity filter, which permits the formation of an unprecedented covalent bond with Cys 290 in the kinase activation segment, lying some 15 Å away. CoA modification (CoAlation) of endogenous Aurora A is rapidly induced by oxidative stresses at Cys 290 in human cells, and microinjection of CoA into mouse embryos perturbs meitoic spindle formation and chromosome alignment. Aurora A regulation by CoA reveals how targeting of Aurora A might be accomplished in the future by development of a ‘double-anchored’ covalent inhibitor.

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