Structural determinants of adenophostin A activity at inositol trisphosphate receptors.

  title={Structural determinants of adenophostin A activity at inositol trisphosphate receptors.},
  author={V. Corr{\^e}a and A. Riley and S. Shuto and G. Horne and E. P. Nerou and R. D. Marwood and B. Potter and C. Taylor},
  journal={Molecular pharmacology},
  volume={59 5},
  • V. Corrêa, A. Riley, +5 authors C. Taylor
  • Published 2001
  • Chemistry, Medicine
  • Molecular pharmacology
  • Adenophostin A is the most potent known agonist of inositol 1,4,5-trisphosphate (InsP(3)) receptors. Ca(2+) release from permeabilized hepatocytes was 9.9 +/- 1.6-fold more sensitive to adenophostin A (EC(50), 14.7 +/- 2.4 nM) than to InsP(3) (145 +/- 10 nM), consistent with the greater affinity of adenophostin A for hepatic InsP(3) receptors (K(d) = 0.48 +/- 0.06 and 3.09 +/- 0.33 nM, respectively). Here, we systematically modify the structures of the glucose, ribose, and adenine moieties of… CONTINUE READING
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