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Drugs for Seven Transmembrane Receptors (7TMRs) can have different behaviors in different organs; Pharmacology describes drug behavior in organ systems with system-independent scales (affinity, efficacy) and these can be used to convert descriptive data (what we see in experiments) to predictive data (what the drug will do in therapeutic systems). This conversion is essential in the industrial and academic drug discovery process. My research applies mathematical models of efficacy and receptor allosteric function to characterize drug activity for 7TMRs. Specifically this has produced methods to quantify agonism, biased signaling, allosteric functional effects and quantification of the effects of mutation on receptor function. Currently my efforts are aimed at further incorporating elements of molecular dynamics and new assay technology to 7TMR research to produce scales that can be used to effectively evaluate new drug candidates in drug discovery and development programs.
Drugs for Seven Transmembrane Receptors (7TMRs) can have different behaviors in different organs; Pharmacology describes drug behavior in organ systems with system-independent scales (affinity, efficacy) and these can be used to convert descriptive data (what we see in experiments) to predictive data (what the drug will do in therapeutic systems). This conversion is essential in the industrial and academic drug discovery process. My research applies mathematical models of efficacy and receptor allosteric function to characterize drug activity for 7TMRs. Specifically this has produced methods to quantify agonism, biased signaling, allosteric functional effects and quantification of the effects of mutation on receptor function. Currently my efforts are aimed at further incorporating elements of molecular dynamics and new assay technology to 7TMR research to produce scales that can be used to effectively evaluate new drug candidates in drug discovery and development programs.
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NATURE COMMUNICATIONSno. 1 (2023): 1692-1692
Peter Kolb,Terry Kenakin, Stephen Alexander,Marcel Bermudez,Laura Bohn, Christian Breinholt,Michel Bouvier,Frederick Ehlert,Stephen Hill,Kirill A. Martemyanov, Richard D Neubig,Ongun Onaran,
Authorea (Authorea) (2021)
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