Chandra Avik, Kaur Paranjeet, Sahu Sanjeev Kumar, Mittal Amit
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.
Chem Biol Drug Des. 2022 Dec;100(6):947-967. doi: 10.1111/cbdd.14020. Epub 2022 Jan 17.
PPARs stand for 'peroxisome proliferator-activated receptors' and are ligand-activated transcription factors of nuclear hormone receptor superfamily. A list of the most commonly used single receptor PPAR agonists, that is α (alpha) PPAR agonists, β/δ(beta/delta) PPAR agonists, γ(gamma) PPAR agonists, along with pan PPAR agents, that are being researched on, are marketed, are in clinical trials or are being studied for further derivative findings, has been listed. Type 2 diabetes constitutes about 90% of total diabetes cases. Pan PPAR ligands could very well pave the foundation for a new class of agents, that can act on all 3 PPAR receptors, and produce better effects in general, than the individual receptor-acting ligands or dual combination ligands (α/ γ). In this review paper, we have detailed various pan PPAR agonists that can be used to treat type 2 diabetes, which can generate potential derivatives as well.
PPARs代表“过氧化物酶体增殖物激活受体”,是核激素受体超家族的配体激活转录因子。已列出了一系列正在研究、已上市、处于临床试验阶段或正在进行进一步衍生研究的最常用的单受体PPAR激动剂,即α(阿尔法)PPAR激动剂、β/δ(贝塔/德尔塔)PPAR激动剂、γ(伽马)PPAR激动剂以及泛PPAR药物。2型糖尿病约占糖尿病病例总数的90%。泛PPAR配体很可能为一类新型药物奠定基础,这类药物可作用于所有三种PPAR受体,总体上比作用于单个受体的配体或双重组合配体(α/γ)产生更好的效果。在这篇综述论文中,我们详细介绍了可用于治疗2型糖尿病的各种泛PPAR激动剂,它们也可产生潜在的衍生物。