Presented By: Center for the Discovery of New Medicines - CDNM
Drug Discovery Lecture Series — "Adventures in Academic Drug Discovery: from Acid Isosteres to Zebrafish"
Donna Huryn, Ph.D., University of Pittsburgh School of Pharmacy, University of Pennsylvania
The rapidly changing pharmaceutical industry landscape provides unique opportunities for drug discovery scientists working in academia.
By “playing to their strengths” rather than competing with colleagues in commercial enterprises, academic drug discovery scientists and organizations have an opportunity to have significant impact, both directly and indirectly.
Three projects will be described that take advantage of some of the unique characteristics of a university environment.
Huryn and her colleagues developed a novel acid isostere in an effort to improve blood brain barrier penetrance of a series of enzyme inhibitors. Subsequently, they completed a systematic and comprehensive evaluation of pharmaceutical properties of >30 different known acid isosteres to determine logD, permeability, plasma protein binding and solubility measurements of this group of widely incorporated medicinal chemistry scaffolds. Some surprising trends were uncovered.
In a second project, a high content screen identified selective inhibitors of the STAT3 pathway. Medicinal chemistry optimization provided novel analogs that have potential use as anti-cancer agents.
A third project took advantage of highly specialized capabilities in zebrafish screening and validation in animal models to identify lead compounds for treating acute kidney injury.
All three projects took advantage of some of benefits of an academic environment, but also ran into some of the same frustrations that all drug discovery scientists face.
<strong>About the speaker</strong>
Donna Huryn, Ph.D., is an experienced medicinal chemist who worked at Roche and Wyeth for 20 years prior to becoming a research professor at the University of Pittsburgh School of Pharmacy and adjunct professor of chemistry at the University of Pennsylvania. Huryn is also chair of American Chemical Society Division of Organic Chemistry.
By “playing to their strengths” rather than competing with colleagues in commercial enterprises, academic drug discovery scientists and organizations have an opportunity to have significant impact, both directly and indirectly.
Three projects will be described that take advantage of some of the unique characteristics of a university environment.
Huryn and her colleagues developed a novel acid isostere in an effort to improve blood brain barrier penetrance of a series of enzyme inhibitors. Subsequently, they completed a systematic and comprehensive evaluation of pharmaceutical properties of >30 different known acid isosteres to determine logD, permeability, plasma protein binding and solubility measurements of this group of widely incorporated medicinal chemistry scaffolds. Some surprising trends were uncovered.
In a second project, a high content screen identified selective inhibitors of the STAT3 pathway. Medicinal chemistry optimization provided novel analogs that have potential use as anti-cancer agents.
A third project took advantage of highly specialized capabilities in zebrafish screening and validation in animal models to identify lead compounds for treating acute kidney injury.
All three projects took advantage of some of benefits of an academic environment, but also ran into some of the same frustrations that all drug discovery scientists face.
<strong>About the speaker</strong>
Donna Huryn, Ph.D., is an experienced medicinal chemist who worked at Roche and Wyeth for 20 years prior to becoming a research professor at the University of Pittsburgh School of Pharmacy and adjunct professor of chemistry at the University of Pennsylvania. Huryn is also chair of American Chemical Society Division of Organic Chemistry.
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