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首页> 外文期刊>Journal of biochemical and molecular toxicology >Discovery of novel 1,3,5-triazine as adenosine A_2A receptor antagonist for benefit in Parkinson's disease
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Discovery of novel 1,3,5-triazine as adenosine A_2A receptor antagonist for benefit in Parkinson's disease

机译：在帕金森病中发现新型1,3,5-三嗪作为腺苷A_2A受体拮抗剂

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摘要

Parkinson's disease (PD) is a chronic neuro-degenerative ailment characterized by impairment in various motor and nonmotor functions of the body. In the past few years, adenosine A_2A receptor (A_2AR) antagonists have attracted much attention due to significant relief in PD. Therefore, in the current study, we intend to disclose the development of novel 1,3,5-triazines as A_2AR antagonist. The radioligand binding and selectivity of analogs were tested in HEK293 (human embryonic kidney) and the cells were transfected with pcDNA 3.1(+) containing full-length human A_2AR cDNA and pcDNA 3.1(+) containing full-length human A_1R cDNA, where they exhibit selective affinity for A_2AR. Molecular docking analysis was also conducted to rationalize the probable mode of action, binding affinity, and orientation of the most potent molecule (7c) at the active site of A_2AR. It has been shown that compound 7c form numerous nonbonded interactions in the active site of A_2AR by interacting with Ala59, Ala63, Ile80, Val84 Glu169, Phe168, Met270, and Ile274. The study revealed 1,3,5-triazines as a novel class of A_2AR antagonists.
机译：帕金森病（PD）是一种慢性神经退行性疾病，其特征是身体的各种运动和非运动功能受损。在过去的几年里，腺苷A_2A受体（A_2AR）拮抗剂因能显著缓解PD而引起了广泛关注。因此，在目前的研究中，我们打算揭示新型1,3,5-三嗪类药物作为一种受体拮抗剂的发展。在HEK293（人类胚胎肾）中测试类似物的放射配体结合和选择性，并用含有全长人类A_2AR cDNA的pcDNA 3.1（+）和含有全长人类A_1R cDNA的pcDNA 3.1（+）转染细胞，其中它们对A_2AR表现出选择性亲和力。还进行了分子对接分析，以理顺A_2AR活性位点上最有效分子（7c）的可能作用模式、结合亲和力和方向。已经证明，化合物7c通过与Ala59、Ala63、Ile80、Val84 Glu169、Phe168、Met270和Ile274相互作用，在A2ar的活性部位形成许多非键相互作用。研究表明1,3,5-三嗪类药物是一类新的A2AR拮抗剂。

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