G protein-coupled receptors (GPCRs) are involved in the control of every aspect of our behavior and physiology. This is the largest class of receptors, with several hundred GPCRs identified thus far. Examples are receptors for hormones such as calcitonin and luteinizing hormone or neurotransmitters such as serotonin and dopamine. G protein-coupled receptors can be involved in pathological proce...

Recent advances in basic science pointed to a role for proteinases, through the activation of proteinase-activated receptors (PARs) in nociceptive mechanisms. Activation of PAR1, PAR2 and PAR4 either by proteinases or by selective agonists causes inflammation inducing most of the cardinal signs of inflammation: swelling, redness, and pain. Sub-inflammatory doses of PAR2 agonist still induced hy...

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Their discovery in the 1990s provided insights into the cellular mechanisms involved in the control of energy homeostasis; the regulation of cell differentiation, proliferation, and apoptosis; and the modulation of important biological and patholo...

Plasma lipoproteins are responsible for carrying triglycerides and cholesterol in the blood and ensuring their delivery to target organs. Regulation of lipoprotein metabolism takes place at numerous levels including via changes in gene transcription. An important group of transcription factors that mediates the effect of dietary fatty acids and certain drugs on plasma lipoproteins are the perox...

In addition to their role in protein degradation and digestion, proteases can also function as hormone-like signaling molecules that regulate vital patho-physiological processes, including inflammation, hemostasis, pain, and repair mechanisms. Certain proteases can signal to cells by cleaving protease-activated receptors (PARs), a family of four G protein-coupled receptors. PARs are expressed b...

1 Monash Institute of Pharmaceutical Sciences, Parkville, VIC, Australia 2 Department of Pharmacology, University of Melbourne, Melbourne, VIC, Australia *Correspondence: [email protected] Edited by: Michael Weiss, Case Western Reserve University, USA Reviewed by: Charles Roberts, Oregon National Primate Research Center, USA Michael Lawrence, The Walter and Eliza Hall Institute of Medica...

N-methyl-D-aspartate receptors (NMDAR) have a recognized role in neuronal plasticity while their excessive activation results in excitotoxic death. Therefore, NMDAR antagonists are considered for neuroprotective interventions. However, there is also an emerging role of NMDAR in supporting neuronal survival. Thus, during CNS development, basal NMDAR activity suppresses neuronal apoptosis while m...

The PI3K/Akt/mTOR is a key signaling system that binds oncogenes and various receptors to many cell functions, promotes estrogen resistance, the most frequently activated pathway in malignant neoplasm, including breast cancer (BC). About 70 % of BC hormone‑receptor positive endocrine therapy main component treatment for patients. Tamoxifen remains one basic drugs adjuvant estrogen‑positive Howe...

The P2Y receptor family is a class of G protein-coupled receptors activated primarily by adenosine triphosphate (ATP), diphosphate (ADP), uridine (UTP) and (UDP). P2Y12 expressed on platelets which mediates platelet aggregation morphological changes. At the same time, during process vascular remodeling atherosclerosis, ADP can also promote migration proliferation smooth muscle endothelial cells...

Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors of transcription factors composed of three family members: PPARα, PPARβ/δ and PPARγ. This study was aimed to evaluate the role of PPARs in the estradiol production via follicle stimulating hormone (FSH) in the ovine Sertoli cells. At the first step, transcripts of PPARα, PPARβ /δ and PPARγ were evaluated by quantitative r...