Results 91 to 100 of about 25,601 (192)

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

N‐Palmitoylglycine and other N‐acylamides activate the lipid receptor G2A/GPR132 [PDF]

, 2019
The G‐protein‐coupled receptor GPR132, also known as G2A, is activated by 9‐hydroxyoctadecadienoic acid (9‐HODE) and other oxidized fatty acids. Other suggested GPR132 agonists including lysophosphatidylcholine (LPC) have not been readily reproduced ...
Brown, Andrew J., Chen, Mao Xiang, Dowell, Simon J., Foster, James, Harvey, Jenni, Irving, Andrew J., Ueno, Shohta   +6 more
core   +1 more source

PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes

British Journal of Pharmacology, EarlyView.
Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier, David Spähn, David Arturo Juarez Lopez, Judith L. Nono, Judith Seigner, Lisa Jacob, Siegfried Ussar, Robert Lukowski, Andreas L. Birkenfeld, Gencer Sancar   +9 more
wiley   +1 more source

β-Arrestin Based Receptor Signaling Paradigms: Potential Therapeutic Targets for Complex Age-Related Disorders

Frontiers in Pharmacology, 2018
G protein coupled receptors (GPCRs) were first characterized as signal transducers that elicit downstream effects through modulation of guanine (G) nucleotide-binding proteins. The pharmacotherapeutic exploitation of this signaling paradigm has created a
Jaana van Gastel, Jaana van Gastel, Jhana O. Hendrickx, Jhana O. Hendrickx, Hanne Leysen, Hanne Leysen, Paula Santos-Otte, Louis M. Luttrell, Bronwen Martin, Stuart Maudsley, Stuart Maudsley   +10 more
doaj   +1 more source

Identification of chemokine receptors as potential modulators of endocrine resistance in oestrogen receptor–positive breast cancers [PDF]

, 2014
Introduction Endocrine therapies target oestrogenic stimulation of breast cancer (BC) growth, but resistance remains problematic. Our aims in this study were (1) to identify genes most strongly associated with resistance to endocrine therapy by ...
A Boudot, A Levoye, AE Gururaj, AH Evans, AK Dunbier, Anita Dunbier, Aradhana Rani, AS Coutts, B Györffy, BC Nair, CA Moore, CM Chan, DG Duda, EA Musgrove, F Andre, GJ Sabnis, H Shankar, H Zheng, J Kang, J Xu, JM Burns, K Hattermann, K Sauvé, KE Luker, LA Martin, LA Martin, LA Martin, Lesley-Ann Martin, LV Rhodes, M Dowsett, Mitch Dowsett, MJ Ellis, MR Hara, MT Weigel, N Lapteva, OE Hawkins, Qiong Gao, R Santen, RD Berahovich, Ricardo Ribas, RK Singh, S Ali, S Masamura, S Masri, S Rajagopal, SE Ghayad, SM DeWire, Sunil Pancholi, TJ Frederick, TN Hartmann, V Lakshmikanthan, Y Shi, YC Su, Z Liang, Zara Ghazoui   +54 more
core   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Hydrogen Sulphide Induces μ Opioid Receptor-Dependent Analgesia in a Rodent Model of Visceral Pain [PDF]

, 2010
Background Hydrogen sulphide (H2S) is a gaseous neuro-mediator that exerts analgesic effects in rodent models of visceral pain by activating KATP channels. A body of evidence support the notion that KATP channels interact with endogenous opioids. Whether
Eleonora Distrutti, Sabrina Cipriani, Barbara Renga, Andrea Mencarelli, Marco Migliorati, Stefano Cianetti, Stefano Fiorucci   +6 more
core   +2 more sources

Divergence in μ and δ opioid receptor pharmacology in neurons and antinociceptive efficacy in neuropathic pain: Insights from MP135 and CYM51010

British Journal of Pharmacology, EarlyView.
Background and purpose Opioids targeting the μ opioid receptor remain largely ineffective in neuropathic pain conditions, emphasizing the need for novel therapeutic strategies. MP135 was reported to reduce thermal nociception in naive animals by activating μ‐δ opioid receptor heteromers.
Perrine Inquimbert, Chantal Fitterer, Sylvain Hugel, Mila Jesic, Yannick Goumon, Virgine Andry, Severine Schneider, Francois Daubeuf, Abdelfattah Faouzi, Stephane Doridot, Susruta Majumdar, Frederic Bihel, Martine Schmitt, Dominique Massotte   +13 more
wiley   +1 more source

Concepts of GPCR-controlled navigation in the immune system

, 2019
G-protein-coupled receptor (GPCR) signaling is essential for the spatiotemporal control of leukocyte dynamics during immune responses. For efficient navigation through mammalian tissues, most leukocyte types express more than one GPCR on their surface ...
Boneschansker L, Brandt SL, Chan EC, Filippo K, Freedman NJ, Hjorto GM, Hons M, Katakai T, Kitayama J, Lemos C, Ley K, Miyabe Y, Moussavi‐Harami SF, Proudfoot AEI, Purvanov V, Rot A, Scheiermann C, Schwarz J, Sokol CL, Sotsios Y, Steury MD, Takeda A, Thiriot A, Tomhave ED, Wang Y, Yanagihara S, Zhang Y   +26 more
core   +1 more source

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors [PDF]

, 2018
Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia.
Andrew B. Tobin, Arthur Christopoulos, Arthur Spathis, Ben Capuano, Celine Valant, Davoren, Ehlert, Ehlert, Elham Khajehali, Emma T. van der Westhuizen, Furchgott, Manuela Jörg, Mistry, Patrick M. Sexton, Peter J. Scammells, Shailesh N. Mistry   +15 more
core   +2 more sources