Book:Drug-Acceptor Interactions

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Bibliographical Data

Title:Drug-Acceptor Interactions: modeling theoretical tools to test and evaluate experimental equilibrium effects
Author:Niels Bindslev
Key words:natural drugs, industrial drugs, ligand receptor interactions, synergy, pharmacodynamics, combinatorial drug therapy, toxicology, physiological processes, enzymology, molecular biology, plant biology, systems biology, synthetic biology, biological regulation, network analysis, epigenetics, dose-response, allosteric, homotropic, heterotropic, theoretical modeling, one-state models, two-state models, equilibrium, steady-state, dose-response curves, reaction schemes, co-operativity, auto-modulation, auto-inhibition, auto-intervention, receptors, channels, co-transporters, pumps, G protein-coupled receptors (GPCRs), carriers, bell-shaped synagics
Education Level:Higher Education
License:CC Attribution-Non Commercial (by-nc)
Description:Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state.

The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze ones own data.

The author suggests that: - a sharp distinction be observed for models between ligand-binding and functional experiments, - an insightful and erudite selection be made between one-state intervention and two-state allosteric models, thus separating the ternary-complex model from genuine allosteric models, - a serious consideration of the allosteric two-state model by Hall be tested when applying two drugs simultaneously, - an application of the homotropic two-state models be tried when auto-inhibitory responses show up, - classical methods such as the Lineweaver-Burk plot be abandoned and non-linear fits used instead, - the use of Hill’s modified equation be revised, - the Schild plot be dropped and replaced with an inhibition curve approach, - new ways to evaluate synergy effects be implemented, i.e. the synergy effect of more than one drug in for instance pain relief, cancer cure, or asthma treatment, and that - a paradigm surrounding the functional form of the Monod-Wyman-Changeux formulation be altered.


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