Results 101 to 110 of about 25,601 (192)

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

Pepducin-mediated cardioprotection via β-arrestin-biased β2-adrenergic receptor-specific signaling [PDF]

, 2018
Reperfusion as a therapeutic intervention for acute myocardial infarction-induced cardiac injury itself induces further cardiomyocyte death. β-arrestin (βarr)-biased β-adrenergic receptor (βAR) activation promotes survival signaling responses in vitro ...
Benovic, Jeffrey L., Carter, Rhonda L., de Lucia, Claudio, Gao, Erhe, Grisanti, Laurel A., Koch, Walter J., Thomas, Toby P., Tilley, Douglas G.   +7 more
core   +1 more source

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity [PDF]

, 2016
The free fatty acid receptor 4 (FFA4 or GPR120) has appeared as an interesting potential target for the treatment of metabolic disorders. At present, most FFA4 ligands are carboxylic acids that are assumed to mimic the endogenous long-chain fatty acid ...
Azevedo, Carlos, Christiansen, Elisabeth, Dunlop, Julia, Hansen, Steffen, Hudson, Brian, Kępczyńska, Malgorzata A., Milligan, Graeme, Shumpukade, Bharat, Stocker, Claire J., Ulven, Trond, Wargent, Edward T., Watterson, Kenneth   +11 more
core   +3 more sources

The relationship between the cannabinoids and cardiac remodelling: A comprehensive review of pivotal mechanisms and emerging evidence

British Journal of Pharmacology, EarlyView.
Cardiac remodelling and fibrosis after myocardial infarction or during chronic diseases, such as arterial and pulmonary hypertension or diabetes mellitus, continue to be the more important prognostic factors in determining survival, and so the search for effective anti‐fibrotic interventions is an important target for research and therapy in cardiology.
Anna Krzyżewska, Marta Baranowska‐Kuczko, Hanna Kozłowska   +2 more
wiley   +1 more source

Troglitazone stimulates beta-arrestin-dependent cardiomyocyte contractility via the angiotensin II type 1A receptor. [PDF]

, 2010
Peroxisome proliferator-activated receptor gamma (PPAR gamma) agonists are commonly used to treat cardiovascular diseases, and are reported to have several effects on cardiovascular function that may be due to PPAR gamma-independent signaling events ...
Nguyen, Anny D., Rockman, Howard A., Tilley, Douglas G G.   +2 more
core   +1 more source

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source

Altered agonist sensitivity of a mutant V2 receptor suggests a novel therapeutic strategy for nephrogenic diabetes insipidus. [PDF]

, 2014
Loss of function mutations of the type 2 vasopressin receptor (V2R) in kidney can lead to nephrogenic diabetes insipidus (NDI). We studied a previously described, but uncharacterized mutation of V2R (N321K missense mutation) of an NDI patient.
Balla, András, Erdélyi, László Sándor, Hunyady, László, Patócs, Attila, Tóth, Miklós, Várnai, Péter   +5 more
core   +1 more source

Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation

The FEBS Journal, EarlyView.
Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev, Tomas Obsil, Veronika Obsilova   +2 more
wiley   +1 more source

Spatiotemporal dynamics of β‐arrestin‐mediated Src activation in 5‐HT7 receptor signaling pathway

The FEBS Journal, EarlyView.
GPCRs induce distinct cellular responses via G protein‐ or β‐arrestin‐mediated signaling pathways. This study revealed that β‐arrestin‐biased 5‐HT7R ligand induces slow, sustained Src activation, contrasting with transient G protein‐mediated activation.
Hyunbin Kim, Yong Woo Lee, Huimin Lee, Eunseo Park, Jieon Lee, Hae Nim Lee, Kyeong‐Man Kim, Hyunah Choo, Jihye Seong   +8 more
wiley   +1 more source

Peri-operative opioid analgesia - when is enough too much? A review of opioid-induced tolerance and hyperalgesia [PDF]

, 2019
Opioids are a mainstay of acute pain management but can have many adverse effects, contributing to problematic long-term use. Opioid tolerance (increased dose needed for analgesia) and opioid-induced hyperalgesia (paradoxical increase in pain with opioid
Bull, Fiona, Colvin, Lesley, Hales, Tim
core   +2 more sources