gramine-Pt(IV)

Gramine-Pt(IV) is a platinum(IV) prodrug developed as a novel anticancer agent designed to enhance the efficacy of chemotherapy and immunotherapy. Its structure features axial ligands that facilitate strong, non-covalent binding to human serum albumin (HSA), improving stability in the bloodstream and tumor accumulation. Upon reduction inside cells, gramine-Pt(IV) is converted to active platinum(II) species (such as cisplatin), which damage DNA and induce apoptosis in cancer cells. Beyond DNA damage, gramine-Pt(IV) enhances chemoimmunotherapy by activating the cGAS-STING pathway and modulating the TGF-β-MHC-I axis, contributing to both direct cytotoxicity and immune activation against tumors. The compound demonstrates improved pharmacokinetic stability and superior blood stability compared to classical platinum-based chemotherapeutics[2][4].