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  • Title: Adenophostin-medicated quantal Ca2+ release in the purified and reconstituted inositol 1,4,5-trisphosphate receptor type 1.
    Author: Hirota J, Michikawa T, Miyawaki A, Takahashi M, Tanzawa K, Okura I, Furuichi T, Mikoshiba K.
    Journal: FEBS Lett; 1995 Jul 17; 368(2):248-52. PubMed ID: 7628615.
    Abstract:
    Kinetics of Ca2+ release by adenophostin, a novel agonist of inositol 1,4,5-trisphosphate (IP3) receptor, in the purified and reconstituted IP3 receptor type 1 (IP3R1) was investigated using the fluorescent Ca2+ indicator fluo-3. Submaximal concentrations of adenophostin caused quantal Ca2+ release from the purified IP3R1 as IP3 did. Adenophostin-induced Ca2+ release by the purified IP3R1 exhibited a high positive cooperativity (nH = 3.9 +/- 0.2, EC50 = 11 nM), whereas the IP3-induced Ca2+ release exhibited a moderate one (nH = 1.8 +/- 0.1, EC50 = 100 nM). Inhibition of [3H]IP3 binding to the purified IP3R1 by adenophostin exhibited a positive cooperativity (nH = 1.9, Ki = 10 nM), whereas IP3 did not (nH = 1.1, Ki = 41 nM).
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