The peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors that regulate the expression of genes. All three PPAR isotypes, PPAR-α, PPAR-β/δ, and PPAR-γ, though expressed in different tissues, play essential roles in the regulation of cellular differentiation, development, metabolism, and tumorigenesis. Many types of medicine exert multiple effects targeted for PPARs in various human diseases, such as thiazolidinediones (TZDs) for restoring insulin sensitivity in type 2 diabetes, and fibrates for reducing cardiovascular events such as coronary heart disease, myocardial infarction, and stroke in type 2 diabetic patients without the use of statins. Given that PPARs are known to play a role in human diseases, the targeted medication of PPARs needs to be developed for appropriate clinical utilisation.

However, adverse effects of current PPAR agonists have been extensively reported. For example, the clinical use of the PPAR-γ agents pioglitazone and rosiglitazone revealed a number of common adverse effects, including weight gain, fluid retention, congestive heart failure, and bone fractures. Thus, the development of tissue-specific agonists may enhance the therapeutic benefits and reduce deleterious effects. Traditional Chinese medicine (TCM) compounds have long been used against metabolic disease and related cardiovascular complications and are an attractive resource in the design of new PPAR agonists to reduce cardiovascular risks.

The aim of this Special Issue is to invite investigators to submit original research articles and review articles that aim to increase the knowledge of PPAR signalling pathways in related diseases and medicines at systematic or tissue levels.

Potential topics include but are not limited to the following:

• The dominant roles played by PPARs in the development of human metabolic-related diseases, including obesity, type 2 diabetes, cardiovascular diseases, or hepatic steatosis
• Medicines targeted for PPARs including inhibitors, agonists, antagonists, activators, and modulators for different human diseases
• Pharmacological and toxicological effects of targeted medicines for PPARs and in-depth exploration of the mechanisms
• Combined drug therapy for PPAR signalling pathways and related drug screening
• Drug screening of PPAR activators/inhibitors as novel targeting agents
• The comparison of PPAR targeted medicines with other targeted drugs
• The broad exploration of PPAR signalling pathways in human diseases and pharmacotherapeutics
• Crosstalk between PPAR signalling and other pathways in human diseases and pharmacotherapeutics