Results 81 to 90 of about 31,985 (308)

The Concise Guide to PHARMACOLOGY 2015/16:Ligand-gated ion channels [PDF]

, 2015
The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org),
Aldrich, R, Alexander, SPH, Attali, B, Back, M, Barnes, NM, Bathgate, R, Beart, PM, Becirovic, E, Benson, HE, Biel, M, Birdsall, NJ, Boison, D, Brauner-Osborne, H, Broeer, S, Bryant, C, Burnstock, G, Burris, T, Cain, D, Calo, G, Chan, SL, Chandy, KG, Chiang, N, Christakos, S, Christopoulos, A, Chun, JJ, Chung, J-J, Clapham, DE, Connor, MA, Coons, L, Cox, HM, Dautzenberg, FM, Davies, JA, Dent, G, Douglas, SD, Dubocovich, ML, Edwards, DP, Faccenda, E, Farndale, R, Fong, TM, Forrest, D, Fowler, CJ, Fuller, P, Gainetdinov, RR, Gershengorn, MA, Goldin, A, Goldstein, SAN, Grimm, SL, Grissmer, S, Gundlach, AL, Hagenbuch, B, Hammond, JR, Hancox, JC, Hartig, S, Hauger, RL, Hay, DL, Hebert, T, Hollenberg, AN, Holliday, ND, Hoyer, D, Ijzerman, AP, Inui, KI, Ishii, S, Jacobson, KA, Jan, LY, Jarvis, GE, Jensen, R, Jetten, A, Jockers, R, Kaczmarek, LK, Kanai, Y, Kang, HS, Karnik, S, Kelly, E, Kerr, ID, Korach, KS, Lange, CA, Larhammar, D, Leeb-Lundberg, F, Leurs, R, Lolait, SJ, Macewan, D, Maguire, JJ, Marrion, N, May, JM, Mazella, J, McArdle, CA, McDonnell, DP, Michel, MC, Miller, LJ, Mitolo, V, Monie, T, Monk, PN, Mouillac, B, Murphy, PM, Nahon, J-L, Nerbonne, J, Nichols, CG, Norel, X, Oakley, R, Offermanns, S, Palmer, LG, Panaro, MA, Pawson, AJ, Perez-Reyes, E, Pertwee, RG, Peters, JA, Pike, JW, Pin, JP, Pintor, S, Plant, LD, Poyner, DR, Prossnitz, ER, Pyne, S, Ren, D, Richer, JK, Rondard, P, Ross, RA, Sackin, H, Safi, R, Sanguinetti, MC, Sartorius, CA, Segaloff, DL, Sharman, JL, Sladek, FM, Southan, C, Stewart, G, Stoddart, LA, Striessnig, J, Summers, RJ, Takeda, Y, Tetel, M, Toll, L, Trimmer, JS, Tsai, M-J, Tsai, SY, Tucker, S, Usdin, TB, Vilargada, J-P, Vore, M, Ward, DT, Waxman, SG, Webb, P, Wei, AD, Weigel, N, Willars, GB, Winrow, C, Wong, SS, Wulff, H, Ye, RD, Young, M, Zajac, J-M   +150 more
core   +5 more sources

Fibrates Inhibit PLTP‐induced M2 Macrophage Infiltration and Increase the Sensitivity of Hepatocellular Carcinoma to ICIs

Advanced Science, EarlyView.
Phospholipid transfer protein(PLTP) plays a critical role in forming a complex with kinase A (AURKA) and P65. This interaction facilitates phosphorylation of P65 at Ser536, leading to the activation of the NF‐κB signaling pathway. Ultimately, this leads to the upregulation of downstream cytokines, including IL‐6, IL‐8, and CSF‐1, which promotes M2 ...
Xinyue Liang, Yaning Li, Jianxun Cai, Lisi Luo, Pengfei Yang, Yutong Chen, Jiancong Zhou, Yan Zeng, Jiaping Yu, Weiyu Zhang, Wenzheng Pang, Yufang Li, Chunhua Wen, Jian Li, Linjuan Zeng   +14 more
wiley   +1 more source

In Vivo Non-radioactive Assessment of mGlu5 Receptor-Activated Polyphosphoinositide Hydrolysis in Response to Systemic Administration of a Positive Allosteric Modulator

Frontiers in Pharmacology, 2018
mGlu5 receptor-mediated polyphosphoinositide (PI) hydrolysis is classically measured by determining the amount of radioactivity incorporated in inositolmonophosphate (InsP) after labeling of membrane phospholipids with radioactive inositol. Although this
Anna R. Zuena, Luisa Iacovelli, Rosamaria Orlando, Luisa Di Menna, Paola Casolini, Giovanni Sebastiano Alemà, Gabriele Di Cicco, Giuseppe Battaglia, Ferdinando Nicoletti, Ferdinando Nicoletti   +9 more
doaj   +1 more source

Allostery of atypical modulators at oligomeric G protein-coupled receptors

Scientific Reports, 2021
Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine, Brendan Kelly, Gwendolynne Elmslie, Xi-Ping Huang, Yue John Dong, Margaret Seidenberg, James W. Wells, John Ellis   +7 more
doaj   +1 more source

Ufmylation‐Deficient DDRGK1 Ameliorates Obesity by Inhibiting FASN‐Mediated Adipocyte Lipogenesis

Advanced Science, EarlyView.
DDRGK1 regulates de novo lipogenesis via stabilization of fatty acid synthase (FASN). DDRGK1‐mediated UFMylation of FASN prevents its ubiquitin–proteasomal degradation. Reduced DDRGK1 expression or mutation at the key UFMylation site enhances FASN degradation and suppresses fatty acid synthesis (FAS), resulting in smaller adipocytes and improved ...
Yin Li, Tangjun Zhou, Xiao Yang, Kewei Rong, Xiankun Cao, Lei Shi, Xin Wang, Hongjin Wan, Lei Cui, Kexin Liu, Tong Xing, Hang Zhang, Chen Zhao, Tingxian Guo, Peixiang Ma, Jie Zhao, An Qin   +16 more
wiley   +1 more source

Progress in GABAA receptor agonists for insomnia disorder

Frontiers in Pharmacology
Insomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health.
Weiyi Wang, Wanting Fu, Hongyan Zhu, Jing Ma, Jian Zhang, Jia Qi   +5 more
doaj   +1 more source

Roles of Cholecystokinin in the Nutritional Continuum. Physiology and Potential Therapeutics

Frontiers in Endocrinology, 2021
Cholecystokinin is a gastrointestinal peptide hormone with important roles in metabolic physiology and the maintenance of normal nutritional status, as well as potential roles in the prevention and management of obesity, currently one of the dominant ...
Laurence J. Miller, Kaleeckal G. Harikumar, Denise Wootten, Patrick M. Sexton   +3 more
doaj   +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

Resolvin D5 Inhibits CXCL8 Expression in Colonic Epithelial Cells Through Activating GPR101 to Impede Neutrophil Recruitment and Consequently Alleviate Ulcerative Colitis

Advanced Science, EarlyView.
RvD5 effectively alleviates UC by inhibiting STAT1 signaling to reduce CXCL8 expression in colonic epithelial cells via activation of GPR101, which subsequently decreases the infiltration of neutrophils in the colonic mucosal epithelium. Epimedin A1, a natural allosteric inhibitor of 5‐LOX, demonstrates potential as a therapeutic agent for UC by ...
Pengxiang Guo, Yilei Guo, Yanrong Zhu, Ke Yan, Yulai Fang, Jiafeng Zhang, Yue He, Zhifeng Wei, Yufeng Xia, Yue Dai   +9 more
wiley   +1 more source

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E, Mahoney, Jacob P, Manglik, Aashish, Sunahara, Roger K, Traynor, John R   +4 more
core