Drug intelligence / Profile preview

MP-17

Development stage
Preclinical
Lead developer
West China Hospital of Sichuan University
Modality
MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

MP-17 is an oligonucleotide-based proteolysis-targeting chimera (PROTAC) designed to degrade the c-Myc oncogenic transcription factor. The molecule is created by conjugating VH032 (a VHL ligand) with an optimized DNA sequence that recognizes the c-Myc complex. MP-17 works by forming a ternary complex between VHL (von Hippel-Lindau E3 ubiquitin ligase), the PROTAC molecule, and c-Myc, which then recruits the ubiquitin-proteasome system to induce c-Myc degradation. This approach addresses the challenge of targeting c-Myc, which plays a critical oncogenic role in tumorigenesis but has been difficult to target with conventional therapeutic strategies. The drug was developed by West China Hospital and has demonstrated effectiveness in suppressing cell proliferation in hepatocellular carcinoma cells, showing significant tumor growth inhibition in mouse models with promising drug safety profiles.

02

Targets

MYC (MYC proto-oncogene protein)VHL (Von Hippel–Lindau tumor suppressor protein)

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