%0 Journal Article %1 Swinney2008BindingKineticsDrugDesign %A Swinney, David C. %D 2008 %J Pharmaceutical Medicine %K binding-kinetics drug-design ligand-binding residence-time %N 1 %P 23--34 %R 10.1007/BF03256679 %T Applications of Binding Kinetics to Drug Discovery %U http://dx.doi.org/10.1007/BF03256679 %V 22 %X The therapeutic response of a drug is initiated by binding to a physiological target. The efficacy, tolerability and therapeutic index of the drug will be influenced by how efficiently the binding is coupled to physiology. The influence of coupling efficiency on dose-response relationships is determined by drug binding kinetics and drug-induced conformational changes to the physiological target. Binding kinetics determine the affinity of a drug to its target and can impact the coupling efficiency of the drug by affecting the state of equilibrium. The end result may be greater efficacy (exemplified by the angiotensin II receptor 1 antagonists), longer duration of response (muscarinic receptor antagonists), differentiation of therapeutic indications (NSAIDs and ion channel antagonists) and/or greater tolerability (atypical antipsychotics, N-methyl-D-aspartate NMDA receptor antagonists, NSAIDs and selective estrogen receptor modulators).

@article{Swinney2008BindingKineticsDrugDesign, abstract = {The therapeutic response of a drug is initiated by binding to a physiological target. The efficacy, tolerability and therapeutic index of the drug will be influenced by how efficiently the binding is coupled to physiology. The influence of coupling efficiency on dose-response relationships is determined by drug binding kinetics and drug-induced conformational changes to the physiological target. Binding kinetics determine the affinity of a drug to its target and can impact the coupling efficiency of the drug by affecting the state of equilibrium. The end result may be greater efficacy (exemplified by the angiotensin II receptor 1 antagonists), longer duration of response (muscarinic receptor antagonists), differentiation of therapeutic indications (NSAIDs and ion channel antagonists) and/or greater tolerability (atypical antipsychotics, N-methyl-D-aspartate [NMDA] receptor antagonists, NSAIDs and selective estrogen receptor modulators).}, added-at = {2017-02-27T17:41:09.000+0100}, author = {Swinney, David C.}, biburl = {https://www.bibsonomy.org/bibtex/25669a37240e4ae82e4799b8a8af40758/salotz}, description = {Applications of Binding Kinetics to Drug Discovery | SpringerLink}, doi = {10.1007/BF03256679}, interhash = {74f29d9f4f7ca8f876ff639e0262d591}, intrahash = {5669a37240e4ae82e4799b8a8af40758}, issn = {1179-1993}, journal = {Pharmaceutical Medicine}, keywords = {binding-kinetics drug-design ligand-binding residence-time}, number = 1, pages = {23--34}, timestamp = {2017-02-27T17:41:09.000+0100}, title = {Applications of Binding Kinetics to Drug Discovery}, url = {http://dx.doi.org/10.1007/BF03256679}, volume = 22, year = 2008 }