Article
A short cross-linker activates human P-glycoprotein missing a catalytic carboxylate.
Biochemical pharmacology - 1 Dec 2017
Loo Tip W, Clarke David M
Abstract excerpt
P-glycoprotein (P-gp) is an ATP-dependent drug pump that protects us from toxic agents and confers multidrug resistance. It has a tweezer-like structure with each arm consisting of a transmembrane domain (TMD) and a nucleotide-binding domain (NBD). Drug substrates bind to sites within the TMDs to activate ATPase activity by promoting a tweezer-like closing of the gap between the NBDs. The catalytic carboxylates...
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