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Therapeutic role of peroxisome proliferator-activated receptors in obesity, diabetes and inflammation

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Progress in Drug Research

Part of the book series: Progress in Drug Research ((PDR,volume 60))

Summary

Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear receptor family and play a significant role in regulation of lipid metabolism, hepatic peroxisomal enzyme expression, insulin sensitivity and glucose homeostasis. PPARs have been classified into three subtypes encoded by different genes: PPARα (NR1C1), PPARδ (NR1C2), and PPARγ (NR1C3). Each subtype of PPARs appears to be differently expressed in a tissue-specific manner because of their binding to specific consensus DNA sequences, known as PPREs (peroxisome proliferator response elements). Thus, PPARs have emerged as potential molecular targets for the design and synthesis of a different class of compounds, considering the conformation of receptors for the treatment of human metabolic disorders. This review covers the rapid progress made in functional analysis of PPARs and progress made towards the identification of ligands for each subtype receptor.

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Abbreviations

PPARs:

peroxisome proliferator-activated receptors

PPRE:

peroxisome proliferator response element

RXR:

retinoid X-receptor

DBD:

DNA-binding domain

LBD:

ligand-binding domain

LiA:

ligand-independent activation

ATP:

adenosine triphosphate

LDL:

low-density lipoprotein

HDL:

high-density lipoprotein

LPL:

lipoprotein lipase

TNF-α:

tumor necrosis factor-α

SRC:

steroid receptor co-activator

TZD:

thiazolidinedione

NIDDM:

non-insulin-dependent diabetes mellitus

WAT:

white adipose tissue

BAT:

brown adipose tissue

IL-6:

interleukin-6

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  1. Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, 226001, India

    Vishnu Ji Ram

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Ram, V.J. (2003). Therapeutic role of peroxisome proliferator-activated receptors in obesity, diabetes and inflammation. In: Jucker, E. (eds) Progress in Drug Research. Progress in Drug Research, vol 60. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8012-1_3

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