P-糖蛋白（P-gp）是一種跨膜轉(zhuǎn)運(yùn)蛋白，屬于三磷酸腺苷結(jié)合盒式結(jié)構(gòu)轉(zhuǎn)運(yùn)蛋白超家族成員，其主要分布于肝臟、腎臟、胃腸道和血腦屏障等組織。一方面，P-gp在細(xì)胞營養(yǎng)的攝取、代謝物的排泄、能量的產(chǎn)生和細(xì)胞信號的傳導(dǎo)等正常細(xì)胞生理學(xué)功能方面起到了至關(guān)重要的作用；另一方面，P-gp的過度表達(dá)也是造成腫瘤細(xì)胞多藥耐藥（MDR）的主要機(jī)制。介紹P-糖蛋白的分子結(jié)構(gòu)和轉(zhuǎn)運(yùn)機(jī)制的相關(guān)研究進(jìn)展，為其進(jìn)一步研究提供參考。

P-glycoprotein(P-gp) is one kind of membrane proteins which belongs to sub-family B of the ATP-binding cassette transporter superfamily. P-gp is mainly localized in the liver, kidney, gastrointestinal tract and blood brain barrier. On one hand, P-gp plays an important part in transporting ligands across cellular lipid membranes, which is critical for most aspects of cell physiology, including the uptake of nutrients and elimination of waste products, energy generation, and cell signaling. On the other hand, there is a greater likelihood of treatment failure if P-gp expression increases after therapy. One of the best-understood MDR involved mechanisms is the over-expression of P-gp. In the present review, we will provide the latest advances in the studies of the molecular structure basis and the mechanism of P-glycoprotein functions.

國家自然科學(xué)基金項目（81473280，81502992）