By György Keserü, David C. Swinney
This useful reference for medicinal and pharmaceutical chemists combines the theoretical history with glossy tools in addition to functions from contemporary lead discovering and optimization initiatives.
Divided into components at the thermodynamics and kinetics of drug-receptor interplay, the textual content presents the conceptual and methodological foundation for characterizing binding mechanisms for medicinal drugs and different bioactive molecules. It covers all at present used tools, from experimental techniques, corresponding to ITC or SPR, correct as much as the most recent computational equipment. Case reports of real-life lead or drug improvement tasks also are integrated so readers can practice the equipment discovered to their very own tasks. ultimately, some great benefits of an intensive binding mode research for any drug improvement undertaking are summarized in an outlook bankruptcy written through the editors.
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Additional info for Thermodynamics and Kinetics of Drug Binding
For this reason, both ΔH and ΔS values are independent of temperature and their standard values can be obtained by linear van’t Hoﬀ plots. At present, only two examples are reported in literature showing non linear van’t Hoﬀ plots and negative ΔC p ∘ values: the thrombin receptor and the cytoplasmic steroid nuclear receptors where there are relevant intramolecular hydrophobic contributions to the binding [26, 32]. Because of the magnitude of this phenomenon, the molecular characteristics of the ligands and the determination of the ΔC p ∘ allow comparative assessment of analogs, which can be structurally rationalized in respect of their ligand-binding behavior .
2009) A thermodynamic approach to the aﬃnity optimization of drug candidates. Chemical Biology and Drug Design, 74, 468–472. 1 Relevance of Thermodynamics to Pharmacology Increasing evidence can be found that describing receptor ligand interactions in terms of a “lock-and-key” model is no longer adequate. Receptors can be regarded as part of a “molecular machinery,” in which ligand binding forms a trigger to activate or deactivate the machinery. According to this view, it is no longer suﬃcient to know how the key ﬁts into the lock, but we should also ﬁnd out the mechanism with which the key opens and closes the lock.
2. 3. 4. 5. 6. 7. and Dalpiaz, A. (2001b) Thermodynamics of adenosine (A1 and A2A ) receptor interactions, in Drug Receptor Thermodynamics: Introduction and Applications (ed. B. , New York. B. I. I. J. J. Kuhar), Raven Press, New York.