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2
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Purine derivatives as ligands for A3 adenosine receptors.作为A3腺苷受体配体的嘌呤衍生物
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Recent Developments in Selective Agonists and Antagonists Acting at Purine and Pyrimidine Receptors.作用于嘌呤和嘧啶受体的选择性激动剂和拮抗剂的最新进展。
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Engineering of A Adenosine and P2Y Nucleotide Receptors and Their Ligands.腺苷和P2Y核苷酸受体及其配体的工程研究
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A Adenosine Receptors: Protective vs. Damaging Effects Identified Using Novel Agonists and Antagonists.A 腺苷受体：使用新型激动剂和拮抗剂确定的保护作用与损伤作用
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Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position.2位取代的腺嘌呤核苷中腺苷受体亲和力和内在活性的调节。
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Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety.A3 腺苷受体效能的结构决定因素：核糖部分的修饰
Biochem Pharmacol. 2004 Mar 1;67(5):893-901. doi: 10.1016/j.bcp.2003.10.006.
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Demystifying the three dimensional structure of G protein-coupled receptors (GPCRs) with the aid of molecular modeling.借助分子建模揭开G蛋白偶联受体（GPCRs）的三维结构之谜。
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Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.腺苷受体建模：A2A激动剂与拮抗剂结合域的比较
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Design and synthesis of A3 adenosine receptor ligands, 2'-fluoro analogues of Cl-IB-MECA.A3腺苷受体配体（Cl-IB-MECA的2'-氟类似物）的设计与合成
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G protein-coupled receptor drug discovery: implications from the crystal structure of rhodopsin.G蛋白偶联受体药物研发：视紫红质晶体结构带来的启示
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探索人类腺苷A3受体对在核糖和嘌呤部分修饰的腺苷类似物的互补性和活性。

Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety.

作者信息

Van Rompaey Philippe, Jacobson Kenneth A, Gross Ariel S, Gao Zhan-Guo, Van Calenbergh Serge

机构信息

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences (FFW), Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.

出版信息

Bioorg Med Chem. 2005 Feb 15;13(4):973-83. doi: 10.1016/j.bmc.2004.11.044.

DOI:10.1016/j.bmc.2004.11.044
PMID:15670905
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3460517/
Abstract

In this paper we investigated the influence on affinity, selectivity and intrinsic activity upon modification of the adenosine agonist scaffold at the 3'- and 5'-positions of the ribofuranosyl moiety and the 2- and N6-positions of the purine base. This resulted in the synthesis of various analogues, that is, 3-12 and 24-33, with good hA3AR selectivity and moderate-to-high affinities (as in 32, Ki=27 nM). Interesting was the ability to tune the intrinsic activity depending on the substituent introduced at the 3'-position.

摘要

在本文中，我们研究了对呋喃核糖部分的3'-和5'-位以及嘌呤碱基的2-和N6-位进行腺苷激动剂支架修饰时，对亲和力、选择性和内在活性的影响。这导致合成了各种类似物，即3-12和24-33，它们具有良好的人A3腺苷受体（hA3AR）选择性和中等到高的亲和力（如32的Ki = 27 nM）。有趣的是，可以根据在3'-位引入的取代基来调节内在活性。