Journal
FEBS LETTERS
Volume 581, Issue 17, Pages 3247-3252Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.febslet.2007.05.080
Keywords
type 2 diabetes mellitus; drug discovery; membrane protein
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The mitochondrial membrane-associated carnitine palmitoyltransferase system is a validated target for the treatment of type 2 diabetes mellitus. To further facilitate structure-based drug discovery, we determined the crystal structure of rat CPT-2 (rCPT-2) in complex with the substrate analogue palmitoyl-aminocarnitine at 1.8 A resolution. Biochemical analyses revealed a strong effect of this compound on rCPT-2 activity and stability. Using a computational approach we examined the membrane association of rCPT-2. The protein interacts with the membrane as a functional monomer and the calculations confirm the presence of a membrane association domain that consists of layers of hydrophobic and positively charged residues. (C) 2007 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
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