Dessauer C W, Tesmer J J, Sprang S R, Gilman A G
Department of Integrative Biology, Pharmacology and Physiology, University of Texas Health Science Center at Houston, Houston, TX, USA.
Trends Pharmacol Sci. 1999 May;20(5):205-10. doi: 10.1016/s0165-6147(99)01310-3.
Recent kinetic, binding and crystallographic studies using P-site inhibitors of mammalian adenylate bases provide new insights into the catalytic mechanism of these highly regulated enzymes. Here, Carmen Dessauer and colleagues discuss the conformational states of adenylate cyclase, the structural determinants of inhibitor binding and the potential uses of these inhibitors as pharmacological agents.
最近利用哺乳动物腺苷酸碱基的P位点抑制剂进行的动力学、结合和晶体学研究,为这些高度调控的酶的催化机制提供了新的见解。在此,卡门·德绍尔及其同事讨论了腺苷酸环化酶的构象状态、抑制剂结合的结构决定因素以及这些抑制剂作为药物制剂的潜在用途。