Providing a molecular mechanism for P-glycoprotein; Why would i bother?

作者: Richard Callaghan

DOI: 10.1042/BST20150131

关键词: Cell biologyTransport proteinCancer cellBiologyP-glycoproteinGlycoproteinPlasma protein bindingEffluxFunction (biology)Membrane transport

摘要: It is almost 40 years since the drug efflux pump P-glycoprotein (permeability glycoprotein or P-gp) was shown to confer multi-drug resistance in cancer cells. This protein has been one of most extensively investigated transport proteins due its intriguing mechanism and affect oncology. P-gp known interact with over 300 compounds ability achieve this not yet revealed. Following binding substrate nucleotide, a complex series conformational changes membrane cytosolic domains translocates across membrane. Despite 30 years biochemical investigation, availability structural data plethora chemical tools modulate function, molecular remains mystery. In addition, overcoming activity resistant cells achieved clinic, thereby garnering some degree pessimism field. review highlights progress that understanding value undertaking studies.

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