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MIA-610 is a **synthetic antagonist** of human growth hormone-releasing hormone (GHRH), belonging to the Miami (MIA) series of GHRH analogs. It demonstrates greatly increased binding affinity to GHRH receptors (48-fold greater than native GHRH (1-29) NH2), and shows potent anticancer activity in vitro and in vivo. MIA-610 inhibits tumor cell proliferation across several human cancer cell lines, notably endometrial adenocarcinoma, colorectal adenocarcinoma, prostate carcinoma, ovarian carcinoma, and renal cell carcinoma. Its antitumor effects are primarily driven by antagonism of GHRH receptor signaling, leading to suppression of tumor growth through downregulation of GHRH receptor levels. In contrast, MIA-610 has only weak endocrine growth hormone inhibitory activity. This agent’s mechanism includes direct action on both pituitary and splice variant type 1 (SV1) GHRH receptors, which are highly expressed in various cancer cells[1][5].
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