Asha Therapeutics presented their novel VHL recruiter technology at Third Annual Ligase Targeting Drug Development conference. Chief Technology Officer and Head of Computational Chemistry Dr. Rainer Metcalf presented “Beyond CRBN: Enrichment of PK Optimized E3 Ligase Recruiters for TPD” as well as participated in a roundtable discussion on “What More Can We Get Out of the Established Ligases, Cereblon, and VHL?” These presentations highlight ASHA-1007, a novel VHL recruiter that can open new tools for protein degradation beyond Cereblon.
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to tackle disease-causing proteins that have historically been highly challenging to target with conventional small molecules. Cereblon (CRBN) was one of the first E3 ligases to be utilized for TPD.
While the E3 ligase VHL has an attractive profile for clinical usage, it has remained relegated to the research usage due exclusively to the lack of clinic ready small molecule recruiters. At Asha, we have solved these issues by making a novel VHL recruiter, ASHA-1007, that can move the TPD field forward beyond Cereblon.
“Cereblon has been the industry standard with good pharmacokinetics,” said Dr. Metcalf. “ASHA-1007 with its drug profile is a potential breakthrough in developing next generation recruiters beyond Cereblon that has implications for the entire targeted protein degradation field.”
Sam Shrivastava, CEO of Asha Therapeutics, engaged with the attendees on a panel discussion at the conference on the future of protein degradation and remarked, “Over 600 E3 ligases exist with only a handful exploited. Asha seeks to remedy this with our innovative PRISM™ platform that can rapidly generate lead candidates and expand the arsenal of E3 ligases by focusing on tissue specific ligases, cell compartment localization, and better selection of E3 ligases capable of mitigating oncogenic resistance. This can fundamentally allow the field to exploit the Achilles heel of cancers in certain situations and expand the reach of the TPD modality into many undruggable targets for many other diseases. This is indeed an early but exciting time for the field of protein degradation and molecular glues”.
About Asha Therapeutics
Asha Therapeutics, an equal-opportunity employer, is a biopharmaceutical and biotechnology company focusing on developing novel therapeutics for diseases with high unmet medical need using its disruptive PRISM™ technology. The PRISM™ Platform is a leading-edge drug design engine that has resulted in a pipeline of assets that treat neurological disease by considering neuronal deterioration and loss from multiple vantage points, promoting cell survival over cell death in a number of neurological conditions. Utilizing its proprietary PRISM™ technology, Asha Therapeutics is designing new medicines for tomorrow’s cures. For more information, please visit www.ashatherapeutics.com.
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