Journal article
Allosteric inhibition explained through conformational ensembles sampling distinct “mixed” states
Abstract
Allosteric modulation provides an effective avenue for selective and potent enzyme inhibition. Here, we summarize and critically discuss recent advances on the mechanisms of allosteric partial agonists for three representative signalling enzymes activated by cyclic nucleotides: the cAMP-dependent protein kinase (PKA), the cGMP-dependent protein kinase (PKG), and the exchange protein activated by cAMP (EPAC). The comparative analysis of partial …
Authors
Byun JA; VanSchouwen B; Akimoto M; Melacini G
Journal
Computational and Structural Biotechnology Journal, Vol. 18, , pp. 3803–3818
Publisher
Elsevier
Publication Date
2020
DOI
10.1016/j.csbj.2020.10.026
ISSN
2001-0370