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针对肥胖症的潜在抗肥胖/炎症黄酮类生物分子,通过靶向 DNA 结合蛋白抑制剂 ID-1 来预防 WAT 分化。

Potential anti-obesity/inflammatory flavonoid-derived biomolecules against Obesity to prevent WAT differentiation by targeting a DNA-binding protein inhibitor, ID-1.

作者信息

Alanazi Jowaher S, Unnisa Aziz, Alanazi Muteb S, Alharby Tareq N, Patel Rama Devi, Itumalla Ramaiah, Younes Kareem M, Abouzied Amr S, Lakshmi K N V C

机构信息

Department of Pharmacology and Toxicology, College of Pharmacy, University of Hail, Hail, KSA.

Department of Pharmaceutical Chemistry, College of Pharmacy, University of Ha'il, Ha'il, 81442, Saudi Arabia.

出版信息

Cell Mol Biol (Noisy-le-grand). 2023 May 31;69(5):150-155. doi: 10.14715/cmb/2023.69.5.23.

Abstract

A concoction of unhealthy eating, inactivity, and the adverse effects of specific drugs brings on obesity. The primary cause of Obesity is the storage of too much energy and triglycerides in adipocytes, particularly white adipose tissue (WAT). In addition to modifying one's lifestyle, anti-obesity medicines are increasingly used as adjuvant therapy. Flavonoids are the major class of compounds having significant biological impacts and health-improving properties. To find novel flavonoid compounds that fight obesity using computational drug design techniques. This work targets 1DI protein to predict new flavonoid compounds that fight obesity. The study uses computational approaches to anticipate potential anti-obesity/inflammatory flavonoid compounds against obesity to prevent WAT differentiation by targeting ID-1, a DNA-binding protein inhibitor. Our study led to the identification of the protein target inhibitor lead CID: 5280443, which was found to be a potent inhibitor of the receptor. According to the findings of this study, this bio-active molecule may be used as a lead for the development of drugs that preferentially fight obesity without interfering with the functions of the human proteasome. The scientific community will benefit from these discoveries, which could aid in the creation of new medications that treat obesity more successfully.

摘要

不健康的饮食、缺乏运动和特定药物的不良反应会导致肥胖。肥胖的主要原因是脂肪细胞(尤其是白色脂肪组织)中储存了过多的能量和甘油三酯。除了改变生活方式外,抗肥胖药物也越来越多地被用作辅助治疗。类黄酮是具有重要生物学影响和改善健康特性的主要化合物类。使用计算药物设计技术寻找新的具有抗肥胖作用的类黄酮化合物。这项工作以 1DI 蛋白为靶点,预测新的具有抗肥胖作用的类黄酮化合物。该研究使用计算方法预测潜在的抗肥胖/抗炎类黄酮化合物,以防止通过靶向 ID-1(一种 DNA 结合蛋白抑制剂)来阻止白色脂肪组织分化。我们的研究确定了蛋白质靶标抑制剂先导物 CID:5280443,它被发现是该受体的有效抑制剂。根据这项研究的结果,这种具有生物活性的分子可用作开发药物的先导物,这些药物可以优先治疗肥胖症,而不会干扰人类蛋白酶体的功能。科学界将受益于这些发现,这可能有助于开发更成功治疗肥胖症的新药。

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