Grayson N A, Westkaemper R B
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298.
Life Sci. 1988;43(5):437-44. doi: 10.1016/0024-3205(88)90523-1.
Adenosine 5'-alkylphosphates are potent inhibitors of acetyl- and acyl-CoA synthetase. In each case, the most effective inhibitor in the series is homologous with the tightly bound acyl adenylate intermediate. Adenosine 5'-ethylphosphate (Ki = 33 nM) is 88-fold more potent than adenosine 5'-methylphosphate (Ki = 2900 nM) as a competitive inhibitor of acetyl-CoA synthetase; the contribution of a single carbon to the observed binding energy (-11 kJ/mol) is much larger than is typically observed.
5'-烷基腺苷磷酸酯是乙酰辅酶A合成酶和酰基辅酶A合成酶的强效抑制剂。在每种情况下，该系列中最有效的抑制剂都与紧密结合的酰基腺苷酸中间体同源。5'-乙基腺苷磷酸酯（Ki = 33 nM）作为乙酰辅酶A合成酶的竞争性抑制剂，其效力比5'-甲基腺苷磷酸酯（Ki = 2900 nM）高88倍；单个碳原子对观察到的结合能（-11 kJ/mol）的贡献比通常观察到的要大得多。
