Drug intelligence / Profile preview

ZMYND8-targeting peptide PROTAC

Development stage
Preclinical
Modality
Peptides, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

ZMYND8-targeting peptide PROTAC is a peptide-based proteolysis-targeting chimera (PROTAC) designed to induce the degradation of the chromatin reader protein ZMYND8. This drug leverages the cell's natural ubiquitin-proteasome system by simultaneously binding to ZMYND8 and the E3 ubiquitin ligase MDM2, thereby facilitating the ubiquitination and subsequent proteasomal degradation of ZMYND8. Developed using AI-assisted protein structure prediction and macromolecular drug design, this PROTAC has demonstrated significant anti-acute myeloid leukemia (AML) activity in both in vitro and in vivo models. Its mechanism involves degrading ZMYND8, inhibiting cell proliferation, inducing apoptosis, and reducing c-Myc transcription. The drug also utilizes a nano-selenium delivery system to enhance its stability and membrane permeability.

Other names
ZMYND8 PROTAC drugZMYND-8 PROTAC drugZMYND 8 PROTAC drug
02

Targets

ZMYND8 (Zinc finger MYND-type containing 8)MDM2 (Mouse double minute 2 homolog)

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