Dudley Mark W, Peet Norton P, Demeter David A, Weintraub Herschel J R, Ijzerman Ad P, Nordvall Gunnar, van Galen Philip J M, Jacobson Kenneth A
Marion Merrell Dow Research Institute, Cincinnati, Ohio.
Center for Bio-Pharmaceutical Sciences, Leiden, The Netherlands.
Drug Dev Res. 1993 Mar;28(3):237-243. doi: 10.1002/ddr.430280309.
This symposium provided a forum for presentations by the relevant groups on ligand design and ligand binding on the adenosine A, receptor. Agreement appears to exist that the "N-C" model of ligand binding to the receptor is the preferred mode. A consensus has not yet been reached on the actual placement of the ligand in the receptor and the exact amino acids which interact in its binding. Two viable models exist at present. Both can be tested with selective site-directed mutagenic studies on the A receptor as well as with additional designed ligands.
本次研讨会为相关团队提供了一个论坛,用于展示关于腺苷A受体上配体设计和配体结合的研究。似乎大家都认同“N-C”配体与受体结合模型是首选模式。然而,对于配体在受体中的实际位置以及其结合过程中相互作用的具体氨基酸,尚未达成共识。目前存在两种可行的模型。这两种模型都可以通过对A受体进行选择性定点诱变研究以及使用额外设计的配体来进行验证。