Quantitative analysis of receptor allosterism and its implication for drug discovery

Published on December 31, 2015   57 min
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Hi, this is Rumin Zhang, a Research Scientist with Merck. Today, I'll be giving a lecture on the quantitative analysis of receptor allosterism and its implication for drug discovery. This lecture is based on the review paper we recently wrote and published in the expert opinion on drug discovery.
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In this lecture, we will cover six aspects. First, I'll go over, with you, the operational model for receptor allosterism. And then I'll provide a high level classification of receptor modulators. Thirdly, I'll go over, with you, the optimal screening conditions for modulators. And fourth, we'll talk about a phenomena we termed as beta supremacy in allosterism. And fifth, we will cover the optimal assay design and data analysis by global curve fitting analysis. Lastly, address the impact of maximum system response, Emax, on the parameterization of receptor allosterism and this lack of impact on the structure-activity relationship, or SAR ranking.
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Quantitative analysis of receptor allosterism and its implication for drug discovery

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