Drug intelligence / Profile preview

JMX1123

Development stage
Preclinical
Lead developer
Louisiana State University Health Sciences Center
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Parenteral
01

Overview

JMX1123 is a proteolysis-targeting chimera (PROTAC) protein degrader designed to target and degrade Signal Transducer and Activator of Transcription 3 (STAT3). Developed by researchers at the Louisiana State University Health Sciences Center and the University of Texas Medical Branch, JMX1123 is based on the lead STAT3 inhibitor HJC0152 (an O-alkylamino tethered derivative of niclosamide). JMX1123 functions by recruiting an E3 ubiquitin ligase to STAT3, leading to its ubiquitination and subsequent proteasomal degradation. In preclinical studies, JMX1123 has demonstrated potent antiproliferative and apoptotic activity against breast cancer cell lines, including triple-negative breast cancer (TNBC) and estrogen receptor (ER)-positive breast cancer, by significantly reducing total STAT3 protein levels and inhibiting STAT3 phosphorylation at Tyr705 and Ser727.

02

Targets

CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)STAT3 (Signal Transducer and Activator of Transcription 3)

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