October 1, 2018 at 6:45 pm

Chemistry Colloquium | Cell permeability and Phenotypic diversity in Unnatural Cyclic Peptides, Oct. 22

Scott Lokey, portrait

Dr. Scott Lokey

Ohio University’s Chemistry & Biochemistry Colloquium Series presents Dr. Scott Lokey on “Cell permeability and Phenotypic diversity in Unnatural Cyclic Peptides” Monday, Oct. 22, from 4:10 to 5 p.m. in Clippinger 194.

Lokey is Professor with the Department of Chemistry and Biochemistry at the University of California, Santa Cruz.

Abstract:  Cyclic peptides can achieve exquisite biochemical potency and specificity against challenging targets such as protein-protein interactions (PPIs). Most cyclic peptides fail to meet the classical criteria for predicting “drug-likeness”; however, there is a growing number of cyclic peptides that show very drug-like behavior, exhibiting excellent cell permeability and, in some cases, oral bioavailability. These exceptional cases, which include natural products such as cyclosporine A (CSA) as well as a variety of model systems described by our group, have generated enthusiasm for the idea that macrocycles may provide a “middle way” between small molecules and biologics in the pursuit of challenging intracellular targets. We have developed a deep understanding of the factors that govern permeability in this exciting class of molecules. But outside the realm of natural products, the question remains: To what extent can cell permeable cyclic peptides be discovered with novel biological targets and/or mechanisms of action? I will show new data that suggests a vast, untapped chemical space of highly diverse, unnatural cyclic peptides that display both excellent permeability as well as novel biological activity. Our results indicate a path toward discovery that is akin to natural products research, but is not constrained by natural selection to the small set of targets relevant to survival in the natural world

The host is Dr. Justin Holub, Assistant Professor of Chemistry & Biochemistry at Ohio University.

Colloquia are Mondays from 4:10 to 5 p.m. in Clippinger 194.

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