Talks & Lectures
9 Sep 2022
Edwin A. Stevens Hall 330

Enzymology for KIF18A Inhibitor Discovery

Department of Chemistry and Chemical Biology

Rumin Zhang

Speaker: Dr. Rumin Zhang, VP, Head of Biochemistry, Volastra Therapeutics, New York, NY

Abstract

Chromosome instability (CIN) is a well-known hallmark of many cancer cells, with little attention paid to it by biopharma industry until recently. We at NYC-based Volastra Therapeutics are leveraging our understanding of CIN biology in designing a new generation of anticancer agents. One of the targets is KIF18A, a kinesin empowered by ATP hydrolysis in its motor domain to translocate along mitotic spindles, modulate microtubule dynamics and assist in chromosome alignment and congression during mitosis. KIF18A is substantially more essential for many CIN-high cancer cells than normal euploid cells. As a result, its functional inactivation is synthetically lethal to those CIN-high cells. This talk highlights how enzymology plays a key role in our discovery of novel, KIF18A-selective, ATP/microtubule-uncompetitive, safe, efficacious and orally bioavailable inhibitors with sub-nM potency and long drug-target residence time.

Biography

Rumin Zhang is a veteran drug hunter since 1990. He is Vice President, Head of Biochemistry at Volastra Therapeutics since September 2020. Previously, he held positions of increasing responsibilities at Schering-Plough, Merck, Eternity Bioscience and Rafael Pharmaceuticals. He graduated from Wuhan University, came to USA as a CUSBEA (China-United States Biochemistry Examination and Application) predoctoral fellow and completed his PhD study at the State University of New York at Buffalo.

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