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BIBO3304 is a highly selective, non-peptide small molecule antagonist of the Neuropeptide Y receptor type 1 (Y1R). Originally developed as a pharmacological tool to investigate the physiological roles of neuropeptide Y (NPY), it has demonstrated significant potential in oncology research, particularly in colorectal cancer (CRC). The drug works by blocking the NPY/Y1R axis, which is often overexpressed in CRC tissues. This inhibition leads to the activation of the AMPK signaling pathway and the subsequent suppression of the mTOR pathway, which induces autophagy in cancer cells. By restoring autophagy-mediated tumor suppression and inhibiting cell proliferation, BIBO3304 limits tumor growth and progression in preclinical models. While primarily used in research settings to study feeding behavior, anxiety, and vascular tension, its role in modulating cancer cell metabolism and survival marks it as a candidate for targeted cancer therapy.
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