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.”