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嘌呤功能化同系物作为腺苷受体的分子探针

PURINE FUNCTIONALIZED CONGENERS AS MOLECULAR PROBES FOR ADENOSINE RECEPTORS.

作者信息

Jacobson Kenneth A, Daly John W

机构信息

Laboratory of Bioorganic Chemistry, National Inst. of Diabetes, Digestive, and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.

出版信息

Nucleosides Nucleotides. 1991;10(5):1029-1038. doi: 10.1080/07328319108047240.

DOI:10.1080/07328319108047240
PMID:39802924
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11724714/
Abstract

The effects of distal structural changes on biological activity may be studied, using a "functionalized congener" strategy, in which suitably placed chemically reactive chains lead to biologically active conjugates. Probes for photoaffinity labeling, chemical affinity labeling, spectroscopic characterization and affinity chromatography of adenosine receptors have been derived from purine amine congeners (XAC, ADAC for A-receptors and APEC for A-receptors). Also, drug conjugates, including prodrugs and lipids, have been designed as potential pharmacological agents.

摘要

可采用“功能化同系物”策略研究远端结构变化对生物活性的影响，在该策略中，适当放置的化学反应性链会产生生物活性缀合物。腺苷受体的光亲和标记、化学亲和标记、光谱表征及亲和色谱的探针均来源于嘌呤胺同系物（XAC，A受体的ADAC以及A受体的APEC）。此外，包括前药和脂质在内的药物缀合物已被设计为潜在的药理剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/47fe/11724714/a679d9b87fe3/nihms-2044184-f0001.jpg

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本文引用的文献

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Conjugates of catecholamines. 1. N-alkyl-functionalized carboxylic acid congeners and amides related to isoproterenol.儿茶酚胺缀合物。1. N-烷基官能化羧酸同系物及与异丙肾上腺素相关的酰胺。
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N-acyl-gamma-glutamyl derivatives of sulfamethoxazole as models of kidney-selective prodrugs.磺胺甲恶唑的N-酰基-γ-谷氨酰衍生物作为肾选择性前药的模型
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Adenosine analogs with covalently attached lipids have enhanced potency at A1-adenosine receptors.具有共价连接脂质的腺苷类似物在A1-腺苷受体上具有增强的效力。
FEBS Lett. 1987 Dec 10;225(1-2):97-102. doi: 10.1016/0014-5793(87)81138-9.
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A new high affinity, iodinated adenosine receptor antagonist as a radioligand/photoaffinity crosslinking probe.一种新型高亲和力碘化腺苷受体拮抗剂，用作放射性配体/光亲和交联探针。
Mol Pharmacol. 1987 Aug;32(1):184-8.
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High affinity acylating antagonists for the A1 adenosine receptor: identification of binding subunit.A1腺苷受体的高亲和力酰化拮抗剂：结合亚基的鉴定
Mol Pharmacol. 1988 Dec;34(6):724-8.
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A lymphotropic prodrug of L-dopa: synthesis, pharmacological properties, and pharmacokinetic behavior of 1,3-dihexadecanoyl-2-[(S)-2-amino-3-(3,4-dihydroxyphenyl)prop anoyl] propane-1,2,3-triol.
J Med Chem. 1986 May;29(5):687-91. doi: 10.1021/jm00155a018.
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8
High potency congeners of isoproterenol. Binding to beta-adrenergic receptors, activation of adenylate cyclase and stimulation of intracellular cyclic AMP synthesis.异丙肾上腺素的高效同系物。与β-肾上腺素能受体结合，激活腺苷酸环化酶并刺激细胞内环磷酸腺苷的合成。
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