Activation and allosteric modulation of a muscarinic acetylcholine receptor
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
Published in Nature (London) (05.12.2013)
Published in Nature (London) (05.12.2013)
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Journal Article
Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs
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
Published in Nature (London) (14.11.2013)
Published in Nature (London) (14.11.2013)
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Journal Article
Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects
Valant, Celine, Felder, Christian C, Sexton, Patrick M, Christopoulos, Arthur
Published in Molecular pharmacology (01.01.2012)
Published in Molecular pharmacology (01.01.2012)
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Journal Article
Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor
Miao, Yinglong, Goldfeld, Dahlia Anne, Von Moo, Ee, Sexton, Patrick M., Christopoulos, Arthur, McCammon, J. Andrew, Valant, Celine
Published in Proceedings of the National Academy of Sciences - PNAS (20.09.2016)
Published in Proceedings of the National Academy of Sciences - PNAS (20.09.2016)
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Journal Article
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
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
Published in Nature communications (23.07.2019)
Published in Nature communications (23.07.2019)
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Journal Article
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
Koole, Cassandra, Wootten, Denise, Simms, John, Valant, Celine, Sridhar, Rohan, Woodman, Owen L, Miller, Laurence J, Summers, Roger J, Christopoulos, Arthur, Sexton, Patrick M
Published in Molecular pharmacology (01.09.2010)
Published in Molecular pharmacology (01.09.2010)
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Journal Article
Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist
Valant, Celine, May, Lauren T., Aurelio, Luigi, Chuo, Chung Hui, White, Paul J., Baltos, Jo-Anne, Sexton, Patrick M., Scammells, Peter J., Christopoulos, Arthur
Published in Proceedings of the National Academy of Sciences - PNAS (25.03.2014)
Published in Proceedings of the National Academy of Sciences - PNAS (25.03.2014)
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Journal Article
Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR
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.
Published in Nature communications (06.09.2023)
Published in Nature communications (06.09.2023)
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Journal Article
Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
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
Published in Frontiers in pharmacology (29.01.2021)
Published in Frontiers in pharmacology (29.01.2021)
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Journal Article
Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation
Koole, Cassandra, Wootten, Denise, Simms, John, Valant, Celine, Miller, Laurence J, Christopoulos, Arthur, Sexton, Patrick M
Published in Molecular pharmacology (01.09.2011)
Published in Molecular pharmacology (01.09.2011)
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Journal Article
Structure-Based Design and Discovery of New M2 Receptor Agonists
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
Published in Journal of medicinal chemistry (22.11.2017)
Published in Journal of medicinal chemistry (22.11.2017)
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Journal Article
Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics
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
Published in eLife (30.05.2023)
Published in eLife (30.05.2023)
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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
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.
Published in Acta pharmaceutica Sinica. B (01.01.2023)
Published in Acta pharmaceutica Sinica. B (01.01.2023)
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Journal Article
Determination of Adenosine A1 Receptor Agonist and Antagonist Pharmacology Using Saccharomyces cerevisiae: Implications for Ligand Screening and Functional Selectivity
Stewart, Gregory D, Valant, Celine, Dowell, Simon J, Mijaljica, Dalibor, Devenish, Rodney J, Scammells, Peter J, Sexton, Patrick M, Christopoulos, Arthur
Published in The Journal of pharmacology and experimental therapeutics (01.10.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2009)
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Journal Article
3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists
AURELIO, Luigi, VALANT, Celine, FIGLER, Heidi, FLYNN, Bernard L, LINDEN, Joel, SEXTON, Patrick M, CHRISTOPOULOS, Arthur, SCAMMELLS, Peter J
Published in Bioorganic & medicinal chemistry (15.10.2009)
Published in Bioorganic & medicinal chemistry (15.10.2009)
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Journal Article
Fluorescent Derivatives of AC-42 To Probe Bitopic Orthosteric/Allosteric Binding Mechanisms on Muscarinic M1 Receptors
Daval, Sandrine B, Valant, Céline, Bonnet, Dominique, Kellenberger, Esther, Hibert, Marcel, Galzi, Jean-Luc, Ilien, Brigitte
Published in Journal of medicinal chemistry (08.03.2012)
Published in Journal of medicinal chemistry (08.03.2012)
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