Allostery and cooperativity in the interaction of drugs with ionic channel receptors.
Allostery is an essential property of many physiological mechanisms. Cooperativity together with allostery is observed in the behavior of multisubunit receptors. Here we summarize and compare several approaches to the description and analysis of allosteric phenomena with emphasis on the receptors connected to ionic channels as a model. Several simplified methods are discussed in comparison with the microscopic kinetic scheme, affinity-efficacy separation and a thermodynamic approach.
Krůsek
J
J
Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic. krusek@biomed.cas.cz
D000818:Animals; D001665:Binding Sites; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects / Q000502:physiology*; D007473:Ion Channels / Q000737:chemistry / Q000378:metabolism*; D007700:Kinetics; D008954:Models, Biological; D008956:Models, Chemical; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D011956:Receptors, Cell Surface / Q000737:chemistry* / Q000187:drug effects / Q000378:metabolism
D007473:Ion Channels; D004364:Pharmaceutical Preparations; D011956:Receptors, Cell Surface