Application of G-protein-coupled receptor antagonist in preparing medicine for treating glutamate receptor high-expression tumor

Abstract

The invention provides application of a G-protein-coupled receptor antagonist in preparing a medicine for treating glutamate receptor high-expression tumor. The G-protein-coupled receptor antagonist is aripiprazole, Aptiganel or carvedilol. The technical effect of the application provided by the invention is as follows: experiments prove that the aripiprazole, Aptiganel or carvedilol in the G-protein-coupled receptor antagonist can show better anti-tumor activity than Riluzole in the glutamate receptor high-expression human tumor cells.

Description

technical field [0001] The invention relates to the use of a G protein-coupled receptor antagonist in the preparation of drugs for treating tumors with high expression of glutamate receptors, and belongs to the technical field of biomedicine. Background technique [0002] G protein-coupled receptors (GPCRs) are a superfamily of cell surface signaling proteins, the largest family of cell surface proteins, and play an important role in the transduction of extracellular signals into the cell, regulating cell movement , growth, and gene transcription—three critical factors in cancer biology. GPCRs contain seven transmembrane α-helices (TMs) composed of alternately connected extracellular loops (Els) and intracellular loops (ILs), as well as an N-terminal extracellular segment and a C-terminal intracellular segment. Over the past decade, GPCRs-mediated signaling pathways have been shown to be key regulators of proto-oncogene signaling. The unique structural features of GPCRs an...

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However, in a subsequent phase II clinical trial, 5 out of 12 patients whose tumors did not continue to progress or worsen after taking riluzole, but none of the patients had tumor shrinkage or disappearance (J.M.Mehnert, Y. Wen, J.H. Lee, et al. JClinOncol29:2011; supplements; abstract8557)

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