KRAS G12D Degrader ARV-806

**Semantic type:** Pharmacologic Substance

**Definition:** A targeted degrader composed of an E3 ubiquitin ligase-binding moiety that is conjugated, via a linker, to the oncogenic KRAS substitution mutation G12D-binding moiety, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon administration of KRAS G12D degrader ARV-806, the KRAS G12D-targeting moiety specifically targets and binds to the KRAS G12D mutated protein and the E3 ligase-binding moiety targets and binds to the E3 ubiquitin ligase, thereby forming a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation of KRAS G12D. This prevents KRAS G12D-mediated signaling and activation of downstream survival pathways. This leads to an inhibition of the growth of tumor cells that overexpress KRAS G12D. KRAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell proliferation, invasion, and metastasis.

**Synonyms:** - ARV 806 - ARV-806 - ARV806 - KRAS G12D PROTAC Degrader ARV-806 - KRAS G12D PROTAC Protein Degrader ARV-806 - KRAS G12D Proteolysis Targeting Chimera Protein Degrader ARV-806