An allosteric mechanism for potent inhibition of human ATP-citrate lyase

  title={An allosteric mechanism for potent inhibition of human ATP-citrate lyase},
  author={Jia Wei and S. Leit and Jun Kuai and Eric Therrien and Salma Rafi and H. J. Harwood and B. DeLaBarre and L. Tong},
  • Jia Wei, S. Leit, +5 authors L. Tong
  • Published 2019
  • Chemistry, Medicine
  • Nature
  • ATP-citrate lyase (ACLY) is a central metabolic enzyme and catalyses the ATP-dependent conversion of citrate and coenzyme A (CoA) to oxaloacetate and acetyl-CoA1–5. The acetyl-CoA product is crucial for the metabolism of fatty acids6,7, the biosynthesis of cholesterol8, and the acetylation and prenylation of proteins9,10. There has been considerable interest in ACLY as a target for anti-cancer drugs, because many cancer cells depend on its activity for proliferation2,5,11. ACLY is also a target… CONTINUE READING
    29 Citations
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