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GS-1206 is an orally bioavailable small molecule inhibitor of Casitas B-lineage lymphoma proto-oncogene B (CBL-B), an E3 ubiquitin ligase that serves as a critical intracellular negative regulator of T cell and natural killer (NK) cell activation. By inhibiting CBL-B, GS-1206 is designed to enhance the immune system's ability to recognize and attack cancer cells by lowering the threshold for T cell receptor signaling and preventing the induction of T cell exhaustion or anergy. Developed by Gilead Sciences, the compound is currently undergoing Phase 1 clinical evaluation to assess its safety, tolerability, and antitumor activity as a monotherapy in patients with advanced or metastatic solid tumors.
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