Search Results - "Celine Valant"

Activation and allosteric modulation of a muscarinic acetylcholine receptor by Kruse, Andrew C., Ring, Aaron M., Manglik, Aashish, Hu, Jianxin, Hu, Kelly, Eitel, Katrin, Hübner, Harald, Pardon, Els, Valant, Celine, Sexton, Patrick M., Christopoulos, Arthur, Felder, Christian C., Gmeiner, Peter, Steyaert, Jan, Weis, William I., Garcia, K. Christopher, Wess, Jürgen, Kobilka, Brian K.

“…Despite recent advances in crystallography and the availability of G-protein-coupled receptor (GPCR) structures, little is known about the mechanism of their…”
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Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs by Dror, Ron O., Green, Hillary F., Valant, Celine, Borhani, David W., Valcourt, James R., Pan, Albert C., Arlow, Daniel H., Canals, Meritxell, Lane, J. Robert, Rahmani, Raphaël, Baell, Jonathan B., Sexton, Patrick M., Christopoulos, Arthur, Shaw, David E.

“…Binding modes and molecular mechanisms of several allosteric modulators of a prototypical G-protein-coupled receptor are revealed using atomic-level…”
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Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects by Valant, Celine, Felder, Christian C, Sexton, Patrick M, Christopoulos, Arthur

“…We recently described 3-amino-5-chloro-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxylic acid cyclopropylamide (LY2033298) as a novel allosteric modulator…”
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Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor by Miao, Yinglong, Goldfeld, Dahlia Anne, Von Moo, Ee, Sexton, Patrick M., Christopoulos, Arthur, McCammon, J. Andrew, Valant, Celine

“…Design of ligands that provide receptor selectivity has emerged as a new paradigm for drug discovery of G protein-coupled receptors, and may, for certain…”
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Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor by Davey, Anna E, Leach, Katie, Valant, Celine, Conigrave, Arthur D, Sexton, Patrick M, Christopoulos, Arthur

“…The calcium-sensing receptor (CaSR) is a G protein-coupled receptor whose function can be allosterically modulated in a positive or negative manner by…”
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Opportunities and challenges for the development of M1 muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits by Nguyen, Huong T. M., Westhuizen, Emma T., Langmead, Christopher J., Tobin, Andrew B., Sexton, Patrick M., Christopoulos, Arthur, Valant, Celine

“…Targeting allosteric sites of M1 muscarinic acetylcholine receptors (M1 receptors) is a promising strategy to treat neurocognitive disorders, such as…”
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Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs by Hollingsworth, Scott A., Kelly, Brendan, Valant, Celine, Michaelis, Jordan Arthur, Mastromihalis, Olivia, Thompson, Geoff, Venkatakrishnan, A. J., Hertig, Samuel, Scammells, Peter J., Sexton, Patrick M., Felder, Christian C., Christopoulos, Arthur, Dror, Ron O.

“…Allosteric modulators are highly desirable as drugs, particularly for G-protein-coupled receptor (GPCR) targets, because allosteric drugs can achieve…”
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Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening by Koole, Cassandra, Wootten, Denise, Simms, John, Valant, Celine, Sridhar, Rohan, Woodman, Owen L, Miller, Laurence J, Summers, Roger J, Christopoulos, Arthur, Sexton, Patrick M

“…The glucagon-like peptide-1 (GLP-1) receptor is a key regulator of insulin secretion and a major therapeutic target for treatment of diabetes. However, GLP-1…”
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Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist by Valant, Celine, May, Lauren T., Aurelio, Luigi, Chuo, Chung Hui, White, Paul J., Baltos, Jo-Anne, Sexton, Patrick M., Scammells, Peter J., Christopoulos, Arthur

“…The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G…”
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Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias by van der Westhuizen, Emma T, Choy, K H Christopher, Valant, Celine, McKenzie-Nickson, Simon, Bradley, Sophie J, Tobin, Andrew B, Sexton, Patrick M, Christopoulos, Arthur

“…The M and M muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer's disease and…”
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Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR by Burger, Wessel A. C., Pham, Vi, Vuckovic, Ziva, Powers, Alexander S., Mobbs, Jesse I., Laloudakis, Yianni, Glukhova, Alisa, Wootten, Denise, Tobin, Andrew B., Sexton, Patrick M., Paul, Steven M., Felder, Christian C., Danev, Radostin, Dror, Ron O., Christopoulos, Arthur, Valant, Celine, Thal, David M.

“…The M 4 muscarinic acetylcholine receptor (M 4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain…”
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Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation by Koole, Cassandra, Wootten, Denise, Simms, John, Valant, Celine, Miller, Laurence J, Christopoulos, Arthur, Sexton, Patrick M

“…The glucagon-like peptide-1 receptor (GLP-1R) is a key physiological regulator of insulin secretion and a major therapeutic target for the treatment of type II…”
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Structure-Based Design and Discovery of New M2 Receptor Agonists by Fish, Inbar, Stößel, Anne, Eitel, Katrin, Valant, Celine, Albold, Sabine, Huebner, Harald, Möller, Dorothee, Clark, Mary J, Sunahara, Roger K, Christopoulos, Arthur, Shoichet, Brian K, Gmeiner, Peter

“…Muscarinic receptor agonists are characterized by apparently strict restraints on their tertiary or quaternary amine and their distance to an ester or related…”
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Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics by Vuckovic, Ziva, Wang, Jinan, Pham, Vi, Mobbs, Jesse I, Belousoff, Matthew J, Bhattarai, Apurba, Burger, Wessel A C, Thompson, Geoff, Yeasmin, Mahmuda, Nawaratne, Vindhya, Leach, Katie, van der Westhuizen, Emma T, Khajehali, Elham, Liang, Yi-Lynn, Glukhova, Alisa, Wootten, Denise, Lindsley, Craig W, Tobin, Andrew, Sexton, Patrick, Danev, Radostin, Valant, Celine, Miao, Yinglong, Christopoulos, Arthur, Thal, David M

“…Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level…”
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Probing Structural Requirements of Positive Allosteric Modulators of the M4 Muscarinic Receptor by Huynh, Tracey, Valant, Celine, Crosby, Ian T, Sexton, Patrick M, Christopoulos, Arthur, Capuano, Ben

“…The M4 mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh…”
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Structure–activity relationship of pyrazol-4-yl-pyridine derivatives and identification of a radiofluorinated probe for imaging the muscarinic acetylcholine receptor M4 by Haider, Ahmed, Deng, Xiaoyun, Mastromihalis, Olivia, Pfister, Stefanie K., Jeppesen, Troels E., Xiao, Zhiwei, Pham, Vi, Sun, Shaofa, Rong, Jian, Zhao, Chunyu, Chen, Jiahui, Li, Yinlong, Connors, Theresa R., Davenport, April T., Daunais, James B., Hosseini, Vahid, Ran, Wenqing, Christopoulos, Arthur, Wang, Lu, Valant, Celine, Liang, Steven H.

“…There is an accumulating body of evidence implicating the muscarinic acetylcholine receptor 4 (M4) in schizophrenia and dementia with Lewy bodies, however, a…”
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Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity by Stewart, Gregory D, Valant, Celine, Dowell, Simon J, Mijaljica, Dalibor, Devenish, Rodney J, Scammells, Peter J, Sexton, Patrick M, Christopoulos, Arthur

“…The budding yeast, Saccharomyces cerevisiae, is a convenient system for coupling heterologous G protein-coupled receptors (GPCRs) to the pheromone response…”
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Synthesis and Pharmacological Evaluation of M4 Muscarinic Receptor Positive Allosteric Modulators Derived from VU10004 by Huynh, Tracey, Valant, Celine, Crosby, Ian T, Sexton, Patrick M, Christopoulos, Arthur, Capuano, Ben

“…The M4 mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh…”
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3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists by AURELIO, Luigi, VALANT, Celine, FIGLER, Heidi, FLYNN, Bernard L, LINDEN, Joel, SEXTON, Patrick M, CHRISTOPOULOS, Arthur, SCAMMELLS, Peter J

“…A series of 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines were prepared and evaluated as potential allosteric modulators at the A(1) adenosine receptor. The…”
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Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o- and β-arrestin2-mediated pathways by Rahman, Sabrina N., Imhaouran, Faissal, Leurs, Rob, Christopoulos, Arthur, Valant, Céline, Langmead, Christopher J.

“…[Display omitted] The histamine H3 receptor (H3R) is a neurotransmitter receptor that is primarily found in the brain, where it controls the release and…”
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