“Drug Design Strategies – Integrating Chemistry and Biology” 
Abstract: Drug design and development strategies involve application of the principles of chemistry, biochemistry, physiology and related disciplines. Several years ago we initiated a project to design and optimize potential inhibitors of an enzyme implicated in the pathogenesis of chronic diabetes, especially the ocular pathologies. These studies required us understand the biochemistry and physiologic role of the target enzyme, and to be able to isolate the enzyme for biochemical and drug inhibition studies. We had to develop strategies for the initial design of potential enzyme inhibitors and methods for their synthesis and in vitro testing. We also had to apply the tools and methods of analytical chemistry to confirm the structures and configurations of the inhibitor compounds synthesized, as well as assess their purity. Determination of the inhibitory potential of the initial series of compounds in isolated enzyme assays provided basic drug structure-enzyme inhibitory relationships that were exploited for the design of additional drug analogues with even greater inhibitory potential, novel kinetic mechanisms of action and specificity for the target enzyme. Once candidate lead compounds were identified from our initial in vitro enzyme inhibitory and cell culture studies, we began to assess their activity in animal models. We determined their potential to prevent ocular pathologies in diabetes by exploring different routes of drug administration (topical, oral, injection) and measuring drug concentrations in target (ocular) and non-target tissues (brain). We also prepared different dosage forms of the test compounds to optimize drug delivery to eye. Using this integrated approach, applying the foundational principles of chemistry, biochemistry and biology, our team investigated the challenges of designing and delivering potentially effective therapies to treat the ocular complications of diabetes.

 Biography: Jack DeRuiter was born in Holland, Michigan where he earned a bachelor’s degree in Chemistry and Biology from Hope College in 1976. From 1976-1978 he attended the University of Michigan completing a Master’s degree in Medicinal Chemistry where he worked on the design of novel anti-parasitic quinolone drugs. From there Dr. DeRuiter went to the Medical College of Virginia at Virginia Commonwealth University in Richmond where he earned a PhD in 1981 in the area of neuro-medicinal chemistry. His PhD research involved the design and testing of structurally unique adrenergic receptor probes. In 1981 Dr. DeRuiter accepted a post doctoral position at the State University of New York at Buffalo where he investigated the design and synthesis of novel potential anti cancer drugs of the pyrroloquinoline class. In 1983 he joined the faculty at Auburn University’s Harrison College of Pharmacy as an Assistant Professor and member of the Graduate Faculty. He was promoted to Associate professor with tenure in 1988, and to full Professor in 1993. Dr. DeRuiter’s primary responsibilities at Auburn University have been curricular design and development, teaching in the professional and graduate programs and conducting research. In his 30+ years at Auburn Dr. DeRuiter has been engaged in a number of research projects, with a major focus on drug design methods in the areas of diabetes, cancer and novel psychoactive agents. His research team has received over 10 million dollars in federal research funding, and he and his colleagues have published over 200 peer-reviewed research articles, 150 professional articles and book chapters and 20 technical manuals. Dr. DeRuiter and his students also have given more than 150 presentations at scientific meetings across the globe. Dr. DeRuiter was named Hill Crest Endowed Professor in 2019, and Alumni Professor in 2021. He also serves a medical consultant for several law firms throughout the southeast and as an educational consultant focusing on curricular design, development and integration of basic and clinical science content.