Small-molecule, targeted protein degraders (TPD) are an emerging class of drugs which capitalizes on the body’s natural system for clearing damaged or unwanted proteins. TPD eliminate versus inhibit proteins. In addition, TPD do not require a binding site for activity. As such, targeted protein degradation expands the proteome of potential therapeutic opportunities previously considered undruggable. f5 Therapeutics understands that not all undruggable targets provide drugs.
We assess targeted degradation in therapeutically relevant screening conditions (phenotypic screening). Combining protein degradation and phenotypic screening truly differentiates f5 Therapeutics in our ability to identify and prosecute on undruggable, clinical viable targets.
Our Differentiated Approach
f5 Therapeutics' platform is expanding the scope of degradable targets in the Targeted Protein Degradation space. Our methods allow access to the abundance of undiscovered neosubstrates available for degradation with potential in multiple indications. We identify these new targets in context with cellular assays allowing us to fully realize the wide class of neosubstrates afforded by cereblon. Multiple new targets we have discovered are currently not being pursued by other degrader companies. NExMods™ have demonstrated in vitro POC across five therapeutic areas (immuno-oncology, Wnt-driven cancers, auto-immune disease, NASH, liver fibrosis) and demonstrated 100X cereblon binding potency versus known clinical IMiDs.
11 Novel Putative Neosubstrates Discovered
We have validated our platform hypothesis to utilize phenotypic screening (function first) to tap into the 4500+ substrates available for Cereblon-mediated degradation. This separates us from other protein degrader companies that are pursuing the same 5-6 targets. We have discovered 11 novel putative neosubstrates from our proteomics experiments. From what we see in the public domain, these targets are NOT being pursued by other degrader companies which allows us to state with confidence that we have the potential for “first in class” therapeutics.