Results 71 to 80 of about 11,411 (182)

Protease-activated receptor 2 : are common functions in glial and immune cells linked to inflammation-related CNS disorders? [PDF]

, 2015
Protease-activated receptors (PARs) are a novel family of G-protein coupled receptors (GPCRs) whose activation requires the cleavage of the N-terminus by a serine protease.
Bushell, Trevor J., Cunningham, Margaret R., McIntosh, Kathryn A., Moudio, Serge, Plevin, Robin   +4 more
core   +1 more source

Structural basis for GPR40 allosteric agonism and incretin stimulation

Nature Communications, 2018
GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of human GPR40 with an agonist bound to an allosteric site located near the lipid-rich region ...
Joseph D. Ho, Betty Chau, Logan Rodgers, Frances Lu, Kelly L. Wilbur, Keith A. Otto, Yanyun Chen, Min Song, Jonathan P. Riley, Hsiu-Chiung Yang, Nichole A. Reynolds, Steven D. Kahl, Anjana Patel Lewis, Christopher Groshong, Russell E. Madsen, Kris Conners, Jayana P. Lineswala, Tarun Gheyi, Melbert-Brian Decipulo Saflor, Matthew R. Lee, Jordi Benach, Kenton A. Baker, Chahrzad Montrose-Rafizadeh, Michael J. Genin, Anne R. Miller, Chafiq Hamdouchi   +25 more
doaj   +1 more source

Complex Pharmacology of Free Fatty Acid Receptors [PDF]

, 2017
G protein-coupled receptors (GPCRs) are historically the most successful family of drug targets. In recent times it has become clear that the pharmacology of these receptors is far more complex than previously imagined.
Bharat Shimpukade, Brian D. Hudson, Carpentier Y. A., Graeme Milligan, Kalliomaki M., Liu D., Lutz M., Tazoe H., Trond Ulven, Yousefi S., Zhu Y.   +10 more
core   +3 more sources

An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse effects

Pharmacological Research, 2022
Kappa opioid receptor (κOR) agonists lack the abuse liability and respiratory depression effects of clinically used mu opioid receptor (μOR) analgesics and are hypothesized to be safer alternatives.
Alexander R. French, Richard M. van Rijn
doaj   +1 more source

Editorial: Biased agonism in chemoattractant receptor signaling [PDF]

Journal of Leukocyte Biology, 2010
Abstract Selective induction of neutrophil responses by chemoattractants reflects biased agonistic activities of the ligands and is modulated at several levels in chemoattractant receptor signaling.
openaire   +1 more source

Retrospective analysis reveals significant association of hypoglycemia with tramadol and methadone in contrast to other opioids. [PDF]

, 2019
Tramadol is one of the most commonly used analgesics worldwide, classified as having a low abuse potential by U.S. Drug Enforcement Agency, and often recommended in pain management guidelines.
Abagyan, Ruben, Atayee, Rabia S, Makunts, Tigran, U, Andrew   +3 more
core   +1 more source

Desensitization of cAMP Accumulation via Human β3-Adrenoceptors Expressed in Human Embryonic Kidney Cells by Full, Partial, and Biased Agonists

Frontiers in Pharmacology, 2019
β3-Adrenoceptors couple not only to cAMP formation but, at least in some cell types, also to alternative signaling pathways such as phosphorylation of extracellular signal-regulated kinase (ERK). β3-Adrenoceptor agonists are used in long-term symptomatic
Katerina Okeke, Katerina Okeke, Martina B. Michel-Reher, Stavros Gravas, Martin C. Michel   +4 more
doaj   +1 more source

‘O sibling, where art thou?’ – a review of avian sibling recognition with respect to the mammalian literature [PDF]

, 2004
Avian literature on sibling recognition is rare compared to that developed by mammalian researchers. We compare avian and mammalian research on sibling recognition to identify why avian work is rare, how approaches differ and what avian and mammalian ...
Barnard C. J., Barnard C.J., Barnard C.J., Bateson P., Bateson P., Beecher I. M., Blaustein A. R., Boyse E. A., Brown J. L., Burger J., Byers J. A., Catchpole C. K., Colgan P., Cramp S., Cramp S., Davis L. S., Dawkins R., Dewsbury D. A., Evans R. M., Farabaugh S. M., Ferkin M. H., Fletcher D. J. C., Fletcher D.J. C., Fuller C. A., Gamboa G. J., Gottlieb G., Halpin Z. T., Hamilton W. D., Hare J. F., Hare J. F., Hepper P. G., Hepper P. G., Hepper P. G., Hoglund J., Holmes W. G., Holmes W. G., Holmes W. G., Johnsgard P. A., Johnsgard P. A., Kroodsma D. E., Lenington S., McGregor P. K., McShea W. J., Medvin M. B., Miller D. E., Mock D. W., Murie J. O., Nowak R. M., Palestis B. G., Palestis B. G., Pfennig D. W., Pierotti R., Porter R. H., Porter R. H., Porter R. H., Radesater T., Schimmel L., Schubert C. A., Sherman P. W., Sherman P. W., Shields W. M., Shields W. M., Slater P.J. B., Stacey P. B., Stoddard P. K., Trainer J. M., Waldman B., Wilson E. O., Wilson E. O., Zann R. A.   +69 more
core   +2 more sources

Fulfilling the Promise of "Biased" G Protein–Coupled Receptor Agonism [PDF]

Molecular Pharmacology, 2015
The fact that over 30% of current pharmaceuticals target heptahelical G protein-coupled receptors (GPCRs) attests to their tractability as drug targets. Although GPCR drug development has traditionally focused on conventional agonists and antagonists, the growing appreciation that GPCRs mediate physiologically relevant effects via both G protein and ...
Luttrell, Louis M., Maudsley, Stuart, Bohn, Laura M.   +2 more
openaire   +3 more sources

Cytoprotective Activated Protein C Averts Nlrp3 Inflammasome–Induced Ischemia-Reperfusion Injury Via Mtorc1 Inhibition [PDF]

, 2017
Cytoprotection by activated protein C (aPC) after ischemia-reperfusion injury (IRI) is associated with apoptosis inhibition. However, IRI is hallmarked by inflammation, and hence, cell-death forms disjunct from immunologically silent apoptosis are, in ...
Al-Dabet, Moh\u27d Mohanad, Bock, Fabian, Braun-Dullaeus, Ruediger C., Camerer, Eric, Dockendorff, Chris, Elwakiel, Ahmed, Esmon, Charles T., Gadi, Ihsan, Ghosh, Sanchita, Griffin, John H., Huber, Tobias B., Isermann, Berend, Kohli, Shrey, Manoharan, Jayakumar, Nazir, Sumra, Ranjan, Satish, Shahzad, Khurrum   +16 more
core   +2 more sources