The potential for targeting estrogen receptor (ER)-β in various cancer models has been gaining considerable attention in recent years. In this issue of the journal, Chaudhary and colleagues demonstrate markedly decreased ultraviolet B (UVB)-induced skin cancer in a mouse model using a highly specific ER-β agonist, ERB-041. The mechanisms that underlie this strong inhibitory effect are mediated ...

The mechanism of agonist-induced GABA(B) receptor (GABA(B) R) internalization is not well understood. To investigate this process, we focused on the interaction of GABA(B) R with β-arrestins, which are key proteins in the internalization of most of the G protein-coupled receptors, and the agonist-induced GABA(B) R internalization and the interaction of GABA(B) R with β-arrestin1 and β-arrestin2...

the effect of epinephrine on phosphatidate phosphohydrolase (pap) activity of isolated human hepatocytes was studied. epineprine inhibited the enzyme activity progressively at concentrations above 0.1 µm, reaching a maximum inhibition of 64.5% at 100 µm concentration. inclusion of alprenolol, a β-receptor blocker, in the incubation mixture abolished the inhibitory effect of epinephrine on pap, ...

CRTH2: Chemoattractant Receptor-Homologous Molecule Expressed On Th2 Cells; COPD: Chronic Obstructive Pulmonary Disease; WHO: World Health Organization; SIT: Allergen-Specific Immunotherapy; ICS: Inhaled Corticosteroids; LABA: LongActing-Β-Agonist; SABA: Short-Acting-Β-Agonist; MDI: Metered Dose Inhaler; 5-LO: 5-Lipoxygenase; FLAP: 5-LipoxygenaseActivating Protein; 5-Oxo-ETE: 5-Oxo-6,8,11,14-Ei...

background and purpose: the clinical outcome of intrauterine insemination (iui) treatment cycles employing a gonadotrophin-releasing hormone agonist [superfact)] or human chorionic gonadotrophin (hcg) for ovulation induction was compared. materials and methods: a group of 100 patients presenting with amenorrhoea, oligomenorrhoea or unexplained infertility were all treated with clomiphene 100 mg...

α1a Adrenergic receptors (α1aARs) are the predominant AR subtype in human vascular smooth muscle cells (SMCs). α1aARs in resistance vessels are crucial in the control of blood pressure, yet the impact of naturally occurring human α1aAR genetic variants in cardiovascular disorders remains poorly understood. To this end, we present novel findings demonstrating that 3D cultures of vascular SMCs ex...

The effect of epinephrine on phosphatidate phosphohydrolase (PAP) activity of isolated human hepatocytes was studied. Epineprine inhibited the enzyme activity progressively at concentrations above 0.1 µM, reaching a maximum inhibition of 64.5% at 100 µM concentration. Inclusion of alprenolol, a β-receptor blocker, in the incubation mixture abolished the inhibitory effect of epinephrine on P...

Sustained activation of G protein-coupled receptors can lead to a rapid decline in signaling through acute receptor desensitization. In the case of the μ-opioid receptor (MOPr), this desensitization may play a role in the development of analgesic tolerance. It is understood that phosphorylation of MOPr promotes association with β-arrestin proteins, which then facilitates desensitization and rec...

The internal mammary artery (IMA) is currently the preferred conduit for myocardial revascularization. However, pre-operative vasospasm and a hypoperfusion state during maximal exercise may limit its use as a bypass graft. The mechanism of spasm has not been clearly defined. Since β-adrenoceptor activation plays a major role in vasorelaxation, the present study was carried out to investigate th...

The insulin-like growth factor type 1 receptor (IGF-1R) plays an essential role in the development of numerous cancers. Figitumumab (CP) is not only a monoclonal antibody, it also has agonist activity on IGF-1R. The antitumor activity of CP in esophageal squamous cell carcinoma (ESCC) is still unclear. In our study, we identified IGF-1R as an independent prognostic factor in ESCC patients, and ...