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Gain Therapeutics is developing an undisclosed small molecule targeting Discoidin Domain Receptor 2 (DDR2) for the treatment of solid tumors. Discovered using the company's proprietary SEE-Tx™ (Site-Directed Enzyme Enhancement Therapy) platform, these compounds are designed as allosteric regulators (STARs) to inhibit DDR2 signaling. DDR2 is a collagen-activated receptor tyrosine kinase that plays a critical role in cell adhesion, proliferation, and extracellular matrix remodeling. Its dysregulation is associated with tumor progression, epithelial-mesenchymal transition (EMT), and metastasis in various malignancies, including squamous cell lung cancer. By targeting allosteric sites rather than the highly conserved ATP-binding pocket, Gain Therapeutics aims to achieve superior selectivity and potency compared to traditional kinase inhibitors.
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