Enzyme inhibition is typically taught as part of biochemistry courses in undergraduate and professional curricula. This topic is fundamental in its clinical relevance and applicable to pharmacological drug classes, mechanism of action and adverse effects in the health professions curriculum. However inherent concepts are abstract and sometimes difficult for students to grasp. As a result, enzyme inhibition has been the focus of several innovative pedagogical approaches. This study incorporates three-dimensional visualization of therapeutic agents to reinforce lecture concepts of enzyme structure and inhibition, and further relate these concepts to applications for drug action. Investigational and FDA-approved kinase inhibitors developed as anticancer agents were utilized as therapeutically relevant examples of enzyme inhibitors to illustrate enzyme-inhibitor interactions and correlate mechanisms of enzyme inhibition to drug potency, selectivity and resistance. The molecular modeling software, Molecular Operating Environment (MOE) was used for the three-dimensional visualization of enzyme-ligand interactions. Student cohorts were required to answer a series of questions while visualizing the three-dimensional enzyme active site, substrate-bound or inhibitor-bound enzyme complex. Student impressions of the activity based on the survey were positive. Student learning for concepts covered as part of the activity was evaluated using performance on examination questions.

Three-dimensional visualization of kinase inhibitors: Correlating foundational concepts to therapeutic application

2019 Spring National Meeting

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