First Reported E3 Ligase Beyond Cereblon and VHL Shown to Support Broad Targeted Protein Degradation of Multiple Targets In Vivo
SAN DIEGO, May 15, 2020 /PRNewswire/ — Vividion Therapeutics, a biotechnology company discovering and developing highly selective small molecule medicines that drug traditionally inaccessible targets, today announced data describing the application of Vividion’s screening platform to discover a highly selective and potent covalent engager of a previously undrugged E3 ligase. Data will be presented in a poster during the 2020 American Association for Cancer Research (AACR) Virtual Annual Meeting II, being held from June 22-24, 2020. All poster presentations will be made available online on the first day of the meeting.
“Our proprietary platform allows us to discover highly selective small molecules against previously undruggable targets, exemplified by the data we are presenting at AACR, which shows unparalleled selectivity and potency for a novel E3 ligase,” said Diego Miralles, M.D., Chief Executive Officer of Vividion. “E3 ligases are an important class of proteins responsible for directing target proteins to the proteasome for degradation and have the potential to unlock a wide range of valuable therapeutic applications. To the best of our knowledge, our program represents the first E3 ligase outside of Cereblon and VHL that has been reported in a bifunctional construct to achieve in vivo degradation of multiple targets. In addition to data described in our abstract, we have additional evidence that by leveraging covalent binding, we can achieve differentiated pharmacology with profound and long lasting-protein degradation, which may enable us to offer an improved treatment compared to existing approaches.”
When Vividion’s ligands were used to build bispecific degraders, they demonstrated degradation of all targets tested in vitro at concentrations less than 10 nanomolar and achieved near complete degradation of the intended target across multiple tissues in vivo. The constructs were consistently more potent both in vitro and in vivo compared to several published Cereblon- and VHL- based degraders designed to target the same proteins.
Poster Presentation Details:
Abstract # 6411
Title: Discovery of covalent ligands to novel E3 ligases enables bispecific degraders with highly differentiated protein degradation across a broad range of targets
Authors: Kristen Baltgalvis, Shota Kikuchi, Kent Symons, Joe Klebba, Lena Luukkonen, Yuta Naro, Colin Walsh, Joon Chang, Charles Chapman, Ali Tabatabaei, Brian Nordin, Christie Eissler, Joel Chick, Landon Whitby, Jaclyn Brannon, Gabe Simon, Matt Patricelli, Dean Stamos, Larry Burgess, Todd Kinsella
Session Category: Experimental and Molecular Therapeutics
Session Title: Novel Therapeutic Approaches
Vividion Therapeutics, Inc. is a biotechnology company focused on transforming the future of human health through the creation of highly selective small molecule medicines that drug traditionally inaccessible targets. The company is advancing a broad, diversified pipeline of multiple, selective small molecule therapeutics for highly sought-after disease-causing target proteins in oncology and immunology. The company’s cutting-edge platform was spun out of the labs of Vividion’s scientific founders, a team of experts in chemical biology and synthetic chemistry from The Scripps Research Institute in La Jolla, CA. For more information, please visit www.vividion.com.
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SOURCE Vividion Therapeutics