The Daily Bulletin Archive

Please join the Chemistry and Physics departments for the seminar "Chemoenzymatic Strategies for Expediting Molecular Discovery," presented by Rudi Fasan, professor of chemistry at the University of Rochester, on Thursday, February 6, from 12:15 to 1:30 p.m. in Science and Mathematics Complex 176.

Abstract
Our research group is interested in merging chemical and biological tools for developing general platforms for streamlining the discovery of biologically active molecules. Using these methodologies, we aim to discover and develop novel chemical agents useful for probing cell signalling pathways and modulating protein-protein interactions implicated in cancer and other diseases. A first part of the seminar will describe our work on the development of chemoenzymatic strategies for late-stage C—H bond functionalization. The selective functionalization of aliphatic C—H bonds represents a most valuable but also one of the most challenging transformations in organic chemistry. Our group is investigating the use of engineered cytochrome P450s and P450-mediated chemoenzymatic synthesis as a strategy for rapidly diversifying complex molecules such as natural products and streamlining the discovery of natural product analogs with improved pharmacological properties and as probes for investigating diseases. The second part of the talk will provide an overview of methodologies developed by our group for the construction and screening of combinatorial libraries of "natural product-like" macrocyclic peptides. Macrocyclic peptides constitute attractive molecular scaffolds for modulating protein complexes, including "undruggable" protein-protein interactions. We will discuss representative examples in which these methodologies are leveraged toward developing macrocyclic peptides capable of targeting and disrupting protein-protein interactions implicated in cancer development and progression.