MS105

MS105 is a first-in-class proteolysis-targeting chimera (PROTAC) designed to selectively degrade Protein Tyrosine Kinase 6 (PTK6), also known as Breast Tumor Kinase (Brk). PTK6 is a non-receptor tyrosine kinase that is overexpressed in various cancers, including breast, prostate, and pancreatic cancers, where it serves as an oncogenic driver. Unlike traditional small-molecule inhibitors that only block the catalytic activity of PTK6, MS105 facilitates the recruitment of an E3 ubiquitin ligase to the PTK6 protein, leading to its ubiquitination and subsequent degradation by the proteasome. This approach is particularly advantageous because it eliminates both the kinase-dependent and kinase-independent (scaffolding) functions of PTK6, the latter of which often contribute to drug resistance and tumor progression. Preclinical studies have demonstrated that MS105 potently downregulates PTK6 expression, induces apoptosis, and inhibits the migration of breast cancer cells, including those resistant to standard therapies.

Other names

PTK6 PROTACPTK-6 PROTACPTK 6 PROTACPTK6 degraderPTK-6 degraderPTK 6 degrader