Abstract
Carbohydrates and lipids are two components of the diet that provide the necessary energy to carry out various physiological processes to help maintain homeostasis in the body. However, when the metabolism of both biomolecules is altered, development of various liver diseases takes place; such as metabolic-associated fatty liver diseases (MAFLD), hepatitis B and C virus infections, alcoholic liver disease (ALD), and in more severe cases, hepatocelular carcinoma (HCC). On the other hand, PPARs are a family of ligand-dependent transcription factors with an important role in the regulation of metabolic processes to hepatic level as well as in other organs. After interaction with specific ligands, PPARs are translocated to the nucleus, undergoing structural changes to regulate gene transcription involved in lipid metabolism, adipogenesis, inflammation and metabolic homeostasis. This review aims to provide updated data about PPARs’ critical role in liver metabolic regulation, and their involvement triggering the genesis of several liver diseases. Information is provided about their molecular characteristics, cell signal pathways, and the main pharmacological therapies that modulate their function, currently engaged in the clinic scenario, or in pharmacological development.
Highlights
Accepted: 29 July 2021The liver is the main organ responsible for biochemical metabolism in the human body, compounds absorbed by the intestine such as nutrients or drugs, first pass through the liver, where they are processed into simpler products, maintaining and regulating their levels in the bloodstream [1]
Peroxisome proliferator-activated receptors (PPARs) are a family of ligand-dependent transcription factors that regulate essential metabolic processes in the liver and other organs where they are activated by endogenous ligands such as fatty acids and similar compounds
After interaction with the specific ligands, PPARs are translocated to the nucleus, and heterodimerizes with another nuclear receptor; the retinoid X receptor (RXR), which binds to PPAR through two zinc fingers in the DBD, peroxisome proliferator response elements (PPRE) present in the vicinity of PPAR-responsive genes promoters, subsequently altering co-activator/co-repressor dynamics to modulate transcription [7,8,10]
Summary
The liver is the main organ responsible for biochemical metabolism in the human body, compounds absorbed by the intestine such as nutrients or drugs, first pass through the liver, where they are processed into simpler products, maintaining and regulating their levels in the bloodstream [1]. Carbohydrates and lipids are two components of the diet that are metabolized by the liver to generate the necessary energy, leading to several physiological processes that help maintain body homeostasis [2]. Peroxisome proliferator-activated receptors (PPARs) are a family of ligand-dependent transcription factors that regulate essential metabolic processes in the liver and other organs where they are activated by endogenous ligands such as fatty acids and similar compounds. Three isoforms of PPARs are known: PPARα, PPARβ/δ, and PPARγ, all of them with different distribution, affinity and specificity for their agonists, and the ability to modulate lipid metabolism and energy homeostasis in mammals [4]. We describe the molecular characteristics and functions of each subtype.
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