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GS-701644

Development stage: Preclinical
Lead developer: Gilead Sciences
Modality: Small Molecules

Overview

GS-701644 is a small molecule inhibitor of KDM5 histone demethylases (including KDM5A, KDM5B, and KDM5C) originally developed by Gilead Sciences. It acts as an epigenetic modulator by preventing the demethylation of lysine residues on histone proteins, thereby regulating DNA transcription and chromatin structure. Preclinical studies have demonstrated that GS-701644 has potent anti-proliferative activity in breast cancer cell lines, with HER2-positive and estrogen receptor-positive (ER+) subtypes showing particular sensitivity. It has also shown synergistic effects when combined with HER2-targeted therapies such as trastuzumab and lapatinib, as well as single-agent activity in HER2-positive breast cancer xenograft models.

Targets

KDM5A (Lysine-specific demethylase 5A)KDM5B (Lysine-specific demethylase 5B)

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