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G-8068
- Development stage
- Preclinical
- Lead developer
- Grove Biopharma
- Modality
- Peptides, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- No Publicly Known Route Of Administration Reported
01
Overview
G-8068 is a precision-linked proteomimetic (PLP) molecule designed to target the interaction between WDR5 and the transcription factor Myc. Developed by Grove Biopharma, G-8068 is a multivalent molecule optimized from the MYC-box-IIIb peptide that binds to the WDR5 Myc-binding (WBM) site. In glioblastoma cancer stem cells (CSCs), G-8068 induces the degradation of WDR5 and the subsequent destabilization of Myc, leading to the loss of stem cell markers like SOX2 and the suppression of tumor growth and self-renewal. This approach leverages a non-oncogene addiction to WDR5 function in Myc-driven tumors, offering a novel strategy for indirectly targeting the traditionally "undruggable" Myc protein.
02
Targets
WDR5 (WD repeat-containing protein 5)E3 ligase (E3 ubiquitin ligases)MYC (MYC proto-oncogene protein)
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