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Join this ACS Publications webinar to learn about the creation of novel 'bi-steric inhibitors' of mTORC1 and RAS(ON) G12D-Selective inhibitors and their journey into clinical trials, as well as innovative kinase inhibitors developed through the combination of medicinal chemistry and structural biology. Hear from Prof. David Heppner and Dr. Leslie Burnett, winners of the 2025 Philip S. Portoghese Journal of Medicinal Chemistry/ACS Medicinal Chemistry Letters/Division of Medicinal Chemistry Joint Lectureship Awards.

Speakers

• Prof. David Heppner, J. Solo Assistant Professor, State University of New York at Buffalo, United States, David Heppner is the J. Solo Assistant Professor of Medicinal Chemistry in the Department of Chemistry at The State University of New York at Buffalo. He obtained his B.S. in Chemistry from the University of Minnesota and Ph.D. in Chemistry with Edward I. Solomon from Stanford University. He acquired training in biomedical research as an NIH postdoctoral fellow at the University of Vermont and subsequently in medicinal chemistry, cancer biology, and structural biology at the Dana-Farber Cancer Institute and Harvard Medical School. The Heppner Lab applies a structural perspective to drug discovery and focuses on developing novel small molecules relevant to several diseases.

• Dr. Leslie Burnett, Director of Medicinal Chemistry, Revolutionary Medicines, United States, Les Burnett has served in roles of increasing responsibility during his 8-year tenure at Revolution Medicines and currently serves as Director of Medicinal Chemistry. In this role, he has lead chemistry development for two clinical candidates, including RMC-9805, an oral, RAS(ON) G12D-selective, covalent, tri-complex inhibitor for the treatment of RAS-addicted pancreatic (PDAC), non-small cell lung cancer (NSCLC), and colorectal cancer (CRC) that is currently in Phase I (NCT06040541), and RMC-5552, a potential first-in-class, bi-steric, mTORC1-selective inhibitor in Phase I/IIb (NCT04774952, NCT05557292) as an IV agent to treat tumors with hyperactive mTORC1 signaling. Les currently serves as the project lead for an undisclosed RAS(ON) program and leads the development of a DNA Encoded Library (DEL) platform.

• Prof. Kelly Chibale, Editor-in-Chief, ACS Medicinal Chemistry Letters, Kelly Chibale is a Professor of Organic Chemistry at the University of Cape Town (UCT) where he holds the Neville Isdell Chair in African-centric Drug Discovery & Development. He is also a Schmidt Sciences AI2050 Senior Fellow, Full Member of the UCT Institute of Infectious Disease & Molecular Medicine, founding Director of the South African Medical Research Council Drug Discovery & Development Research unit at UCT, Founder & Director of the UCT Holistic Drug Discovery and Development (H3D) Centre, and Founder & CEO of the H3D Foundation. Kelly obtained his PhD in Synthetic Organic Chemistry from the University of Cambridge. This was followed by postdoctoral stints at the University of Liverpool and at The Scripps Research Institute. He was a Sandler Sabbatical Fellow at the University of California San Francisco, a US Fulbright Senior Research Scholar at the University of Pennsylvania School of Medicine, and a Visiting Professor at Pfizer.