The catalytic cycle of P-glycoprotein
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- 作者：Senior ; Alan E. ; Al-Shawi ; Marwan K. ; Urbatsch ; Ina L.
- 关键词：Multidrug-resistance ; P-glycoprotein ; ATPase catalytic cycle
- 刊名：FEBS Letters
- 出版年：1995
- 出版时间：December 27, 1995
- 年：1995
- 卷：377
- 期：3
- 页码：285-289
- 全文大小：477 K
文摘
P-glycoprotein is a plasma-membrane glycoprotein which confers multidrug-resistance on cells and displays ATP-driven drug-pumping in vitro. It contains two nucleotide-binding domains, and its structure places it in the ‘ABC transporter’ family. We review recent evidence that both nucleotide-sites bind and hydrolyse Mg-ATP. The two catalytic sites interact strongly. A minimal scheme for the MgATP hydrolysis reaction is presented. An alternating catalytic sites scheme is proposed, in which drug transport is coupled to relaxation of a high-energy catalytic site conformation generated by the hydrolysis step. Other ABC transporters may show similar catalytic features.