ROR nuclear receptors: structures, related diseases, and drug discovery

Y Zhang, X Luo, D Wu, Y Xu - Acta Pharmacologica Sinica, 2015 - nature.com
Nuclear receptors (NRs) are ligand-regulated transcription factors that regulate metabolism,
development and immunity. The NR superfamily is one of the major classes of drug targets …

The expansive role of oxylipins on platelet biology

J Yeung, M Hawley, M Holinstat - Journal of molecular medicine, 2017 - Springer
In mammals, three major oxygenases, cyclooxygenases (COXs), lipoxygenases (LOXs), and
cytochrome P450 (CYP450), generate an assortment of unique lipid mediators (oxylipins) …

The mechanistic basis of prostacyclin and its stable analogues in pulmonary arterial hypertension: Role of membrane versus nuclear receptors

LH Clapp, R Gurung - Prostaglandins & other lipid mediators, 2015 - Elsevier
Pulmonary arterial hypertension (PAH) is a progressive disease of distal pulmonary arteries
in which patients suffer from elevated pulmonary arterial pressure, extensive vascular …

[HTML][HTML] Molecular mechanism of peroxisome proliferator-activated receptor α activation by WY14643: a new mode of ligand recognition and receptor stabilization

A Bernardes, PCT Souza, JRC Muniz, CG Ricci… - Journal of molecular …, 2013 - Elsevier
Peroxisome proliferator-activated receptors (PPARs) are members of a superfamily of
nuclear transcription factors. They are involved in mediating numerous physiological effects …

Design, synthesis, and biological evaluation of triazolone derivatives as potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis

Z Feng, J Xiang, H Liu, J Li, X Xu, G Sun… - Journal of Medicinal …, 2022 - ACS Publications
Peroxisome proliferator-activator receptors α/δ (PPARα/δ) are regarded as potential
therapeutic targets for nonalcoholic steatohepatitis (NASH). However, PPARα/δ dual agonist …

Hepatic PPARs: their role in liver physiology, fibrosis and treatment

EM Zardi, L Navarini, G Sambataro… - Current Medicinal …, 2013 - ingentaconnect.com
Complex molecular and cellular mechanisms are involved in the pathway of liver fibrosis.
Activation and transformation of hepatic stellate cells (HSCs) are considered the two main …

[HTML][HTML] Peptides released from bovine α-lactalbumin by simulated digestion alleviated free fatty acids-induced lipid accumulation in HepG2 cells

H Chen, X Qi, K Guan, Y Gu, R Wang, Q Li… - Journal of Functional …, 2021 - Elsevier
Our previous study showed that α-lactalbumin (α-LA) has a regulatory effect on lipid
metabolism in obese mice. In this study, we performed simulated gastrointestinal digestion …

Arjunolic acid, a peroxisome proliferator-activated receptor α agonist, regresses cardiac fibrosis by inhibiting non-canonical TGF-β signaling

T Bansal, E Chatterjee, J Singh, A Ray, B Kundu… - Journal of Biological …, 2017 - ASBMB
Cardiac hypertrophy and associated heart fibrosis remain a major cause of death worldwide.
Phytochemicals have gained attention as alternative therapeutics for managing …

The peroxisomal enzyme L-PBE is required to prevent the dietary toxicity of medium-chain fatty acids

J Ding, U Loizides-Mangold, G Rando, V Zoete… - Cell reports, 2013 - cell.com
Specific metabolic pathways are activated by different nutrients to adapt the organism to
available resources. Although essential, these mechanisms are incompletely defined. Here …

Elucidation of molecular mechanism of a selective PPARα modulator, pemafibrate, through combinational approaches of X-ray crystallography, thermodynamic …

M Kawasaki, A Kambe, Y Yamamoto… - International Journal of …, 2020 - mdpi.com
The selective PPARα modulator (SPPARMα) is expected to medicate dyslipidemia with
minimizing adverse effects. Recently, pemafibrate was screened from the ligand library as …