骆驼 FGF21 蛋白增强 FGF21 信号转导及其靶向化合物筛选

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Yuan Gao, Fang Yong, Wangye Ji, Lili Zhang, Jibao Hou, Ruilin Ma, Shuqin Zhao, Huizhen Ge, Xiaoyu Wu
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引用次数: 0

摘要

简介成纤维细胞生长因子 21 (FGF21) 作为一种新型葡萄糖和脂质代谢调节剂,已成为治疗代谢性疾病的一个很有前景的靶点。骆驼是适应干旱和半干旱沙漠气候的特有物种,在调节脂质储备和利用方面表现出卓越的能力:方法:本研究通过序列分析和 FGF21 信号下游标记物的检测发现,与人和小鼠相比,骆驼 FGF21 对下游信号转导具有更强的调控作用。利用 CavityPlus 在线平台预测发现,FGF21 蛋白有一个潜在的药物结合口袋。利用加州大学旧金山分校的 DOCK6 程序进行分子对接,筛选出了四种靶向 FGF21 蛋白的小化合物:间苯二酚单乙酸酯、托吡司琼、尼利德林和斯奇潘托:结果:四种小化合物的抑制浓度 50%(IC50)值由 MTT 试验测定,并通过 GraphPad Prism 软件进行模拟。生物效应测试表明,这四种化合物参与了 FGF21 信号通路的调控,是 FGF21 信号转导的激动剂。而化合物与蛋白质共处理的阻断实验表明,这四种小化合物并不能抑制 FGF21 诱导的通路激活。甚至,间苯二酚单乙酸酯和斯奇潘托还能协同激活 FGF21 蛋白的下游信号通路:本研究为开发基于 FGF21 蛋白修饰的治疗策略提供了新思路,并探索了基于化合物-蛋白组合的新型疾病治疗策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Withdrawn: Camel FGF21 Protein Enhances FGF21 Signaling and its Targeted Compounds Screening

The article has been withdrawn at the request of the author.

Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.

The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php

Bentham science disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

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来源期刊
CiteScore
6.30
自引率
0.00%
发文量
302
审稿时长
2 months
期刊介绍: Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field. Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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