腺苷酸激酶
膦酸盐
化学
激酶
立体化学
腺苷
生物化学
基质(水族馆)
转移酶
腺嘌呤核苷酸
核苷
核苷酸
酶
组合化学
生物
基因
生态学
作者
Malika Kaci,Jean‐Pierre Uttaro,Valérie Lefort,Christophe Mathé,Chahrazade El Amri,Christian Périgaud
标识
DOI:10.1016/j.bmcl.2014.07.036
摘要
AMP mimics constitute an important class of therapeutic derivatives to treat diseases where the pool of ATP is involved. A new phosphonate derivative of 9-(5-hydroxymethylfuran-2-yl)adenine was synthesized in a multi-step sequence from commercially available adenosine. Its ability to behave as a substrate of human adenylate kinases 1 and 2 was assessed. The phosphonate was shown to be a moderate but selective substrate of the mitochondrial human AK2, better than well-known antiviral acyclic phosphonates 9-(2-phosphonomethoxyethyl)adenine (PMEA, Adefovir) and (R)-9-(2-phosphonomethoxypropyl)adenine (PMPA, Tenofovir). Putative binding mode within adenylate kinase NMP site revealed by molecular docking in comparison to AMP native substrate allowed to illustrate this selective behavior.
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