Search Results - "Mathiesen, Jesper M"

Crystal structure of the β2 adrenergic receptor–Gs protein complex by Rasmussen, Søren G. F., DeVree, Brian T., Zou, Yaozhong, Kruse, Andrew C., Chung, Ka Young, Kobilka, Tong Sun, Thian, Foon Sun, Chae, Pil Seok, Pardon, Els, Calinski, Diane, Mathiesen, Jesper M., Shah, Syed T. A., Lyons, Joseph A., Caffrey, Martin, Gellman, Samuel H., Steyaert, Jan, Skiniotis, Georgios, Weis, William I., Sunahara, Roger K., Kobilka, Brian K.

“…G protein-coupled receptors (GPCRs) are responsible for the majority of cellular responses to hormones and neurotransmitters as well as the senses of sight,…”
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Structural insights into the activation of metabotropic glutamate receptors by Koehl, Antoine, Hu, Hongli, Feng, Dan, Sun, Bingfa, Zhang, Yan, Robertson, Michael J., Chu, Matthew, Kobilka, Tong Sun, Laeremans, Toon, Steyaert, Jan, Tarrasch, Jeffrey, Dutta, Somnath, Fonseca, Rasmus, Weis, William I., Mathiesen, Jesper M., Skiniotis, Georgios, Kobilka, Brian K.

“…Metabotropic glutamate receptors are family C G-protein-coupled receptors. They form obligate dimers and possess extracellular ligand-binding Venus flytrap…”
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Structures of metabotropic GABAB receptor by Papasergi-Scott, Makaía M., Robertson, Michael J., Seven, Alpay B., Panova, Ouliana, Mathiesen, Jesper M., Skiniotis, Georgios

“…Stimulation of the metabotropic GABA B receptor by γ-aminobutyric acid (GABA) results in prolonged inhibition of neurotransmission, which is central to brain…”
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Crystal structure of the µ-opioid receptor bound to a morphinan antagonist by Manglik, Aashish, Kruse, Andrew C., Kobilka, Tong Sun, Thian, Foon Sun, Mathiesen, Jesper M., Sunahara, Roger K., Pardo, Leonardo, Weis, William I., Kobilka, Brian K., Granier, Sébastien

“…Opium is one of the world’s oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain. These…”
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Structural Insights into the Process of GPCR-G Protein Complex Formation by Liu, Xiangyu, Xu, Xinyu, Hilger, Daniel, Aschauer, Philipp, Tiemann, Johanna K.S., Du, Yang, Liu, Hongtao, Hirata, Kunio, Sun, Xiaoou, Guixà-González, Ramon, Mathiesen, Jesper M., Hildebrand, Peter W., Kobilka, Brian K.

“…The crystal structure of the β2-adrenergic receptor (β2AR) bound to the G protein adenylyl cyclase stimulatory G protein (Gs) captured the complex in a…”
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Asymmetric activation of the calcium-sensing receptor homodimer by Gao, Yang, Robertson, Michael J., Rahman, Sabrina N., Seven, Alpay B., Zhang, Chensong, Meyerowitz, Justin G., Panova, Ouliana, Hannan, Fadil M., Thakker, Rajesh V., Bräuner-Osborne, Hans, Mathiesen, Jesper M., Skiniotis, Georgios

“…The calcium-sensing receptor (CaSR), a cell-surface sensor for Ca 2+ , is the master regulator of calcium homeostasis in humans and is the target of…”
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G-protein activation by a metabotropic glutamate receptor by Seven, Alpay B., Barros-Álvarez, Ximena, de Lapeyrière, Marine, Papasergi-Scott, Makaía M., Robertson, Michael J., Zhang, Chensong, Nwokonko, Robert M., Gao, Yang, Meyerowitz, Justin G., Rocher, Jean-Philippe, Schelshorn, Dominik, Kobilka, Brian K., Mathiesen, Jesper M., Skiniotis, Georgios

“…Family C G-protein-coupled receptors (GPCRs) operate as obligate dimers with extracellular domains that recognize small ligands, leading to G-protein…”
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Heterogeneous Origins of Calcium Homeostasis Disorders Arising From 5 Heterozygous Calcium-Sensing Receptor Variants by Du, Wei, Boisen, Ida Marie, Rahman, Sabrina N, Poulsen, Nadia Nicholine, Mathiesen, Jesper M, Blomberg Jensen, Martin, Bräuner-Osborne, Hans, Jensen, Anders A

“…Abstract Context The human calcium-sensing receptor (CaSR) plays a key role in calcium homeostasis, and most identified CASR variants are associated with…”
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Detailed functional characterization of four nanobodies as positive allosteric modulators of the human Calcium-Sensing receptor by Du, Wei, Rahman, Sabrina N., Barker, Eleanor, Bräuner-Osborne, Hans, Mathiesen, Jesper M., Ward, Donald T., Jensen, Anders A.

“…[Display omitted] The calcium-sensing receptor (CaSR) plays a key role in calcium homeostasis, and small-molecule and peptide positive allosteric modulators…”
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Allosteric modulation and G-protein selectivity of the Ca2+-sensing receptor by He, Feng, Wu, Cheng-Guo, Gao, Yang, Rahman, Sabrina N., Zaoralová, Magda, Papasergi-Scott, Makaía M., Gu, Ting-Jia, Robertson, Michael J., Seven, Alpay B., Li, Lingjun, Mathiesen, Jesper M., Skiniotis, Georgios

“…The calcium-sensing receptor (CaSR) is a family C G-protein-coupled receptor 1 (GPCR) that has a central role in regulating systemic calcium homeostasis 2 , 3…”
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Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells by Møller, Thor C., Pedersen, Mie F., van Senten, Jeffrey R., Seiersen, Sofie D., Mathiesen, Jesper M., Bouvier, Michel, Bräuner-Osborne, Hans

“…Most G protein-coupled receptors (GPCRs) recruit β-arrestins and internalize upon agonist stimulation. For the μ-opioid receptor (μ-OR), this process has been…”
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A µ-opioid receptor modulator that works cooperatively with naloxone by O’Brien, Evan S., Rangari, Vipin Ashok, El Daibani, Amal, Eans, Shainnel O., Hammond, Haylee R., White, Elizabeth, Wang, Haoqing, Shiimura, Yuki, Krishna Kumar, Kaavya, Jiang, Qianru, Appourchaux, Kevin, Huang, Weijiao, Zhang, Chensong, Kennedy, Brandon J., Mathiesen, Jesper M., Che, Tao, McLaughlin, Jay P., Majumdar, Susruta, Kobilka, Brian K.

“…The µ-opioid receptor (µOR) is a well-established target for analgesia 1 , yet conventional opioid receptor agonists cause serious adverse effects, notably…”
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Negative allosteric modulation of the glucagon receptor by RAMP2 by O'Brien, Evan S., Krishna Kumar, Kaavya, Habrian, Chris, Latorraca, Naomi R., Wang, Haoqing, Tuneew, Inga, Montabana, Elizabeth, Marqusee, Susan, Hilger, Daniel, Isacoff, Ehud Y., Mathiesen, Jesper M., Kobilka, Brian K.

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Mechanistic insights into G-protein coupling with an agonist-bound G-protein-coupled receptor by Batebi, Hossein, Pérez-Hernández, Guillermo, Rahman, Sabrina N., Lan, Baoliang, Kamprad, Antje, Shi, Mingyu, Speck, David, Tiemann, Johanna K. S., Guixà-González, Ramon, Reinhardt, Franziska, Stadler, Peter F., Papasergi-Scott, Makaía M., Skiniotis, Georgios, Scheerer, Patrick, Kobilka, Brian K., Mathiesen, Jesper M., Liu, Xiangyu, Hildebrand, Peter W.

“…G-protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by promoting guanine nucleotide exchange. Here, we investigate the coupling of G…”
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Delineation of molecular determinants for FR900359 inhibition of Gq/11 unlocks inhibition of Gαs by Boesgaard, Michael W., Harpsøe, Kasper, Malmberg, Michelle, Underwood, Christina R., Inoue, Asuka, Mathiesen, Jesper M., König, Gabriele M., Kostenis, Evi, Gloriam, David E., Bräuner-Osborne, Hans

“…Heterotrimeric G proteins are essential mediators of intracellular signaling of G protein–coupled receptors. The Gq/11 subfamily consists of Gq, G11, G14, and…”
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Delineation of the GPR15 receptor‐mediated Gα protein signalling profile in recombinant mammalian cells by Deng, Yufang, Moo, Ee Von, Almería, Claudia Victoria Pérez, Gentry, Patrick R., Vedel, Line, Mathiesen, Jesper M., Bräuner‐Osborne, Hans

“…The GPR15 receptor is a G protein‐coupled receptor (GPCR), which is activated by an endogenous peptide GPR15L(25–81) and a C‐terminal peptide fragment…”
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Author Correction: Structural insights into the activation of metabotropic glutamate receptors by Koehl, Antoine, Hu, Hongli, Feng, Dan, Sun, Bingfa, Zhang, Yan, Robertson, Michael J., Chu, Matthew, Kobilka, Tong Sun, Laeremans, Toon, Steyaert, Jan, Tarrasch, Jeffrey, Dutta, Somnath, Fonseca, Rasmus, Weis, William I., Mathiesen, Jesper M., Skiniotis, Georgios, Kobilka, Brian K.

“…The surname of author Toon Laeremans was misspelled ‘Laermans’. This error has been corrected online…”
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mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery by Mølck, Christina, Harpsøe, Kasper, Gloriam, David E., Mathiesen, Jesper M., Nielsen, Søren M., Bräuner-Osborne, Hans

“…Since its discovery in 1992, mGluR5 has attracted significant attention and been linked to several neurological and psychiatric diseases. Ligand development…”
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Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators by Mølck, Christina, Harpsøe, Kasper, Gloriam, David E, Clausen, Rasmus P, Madsen, Ulf, Pedersen, Lars Ø, Jimenez, Hermogenes N, Nielsen, Søren M, Mathiesen, Jesper M, Bräuner-Osborne, Hans

“…Metabotropic glutamate receptor subtype 5 (mGluR5) is a potential drug target in neurological and psychiatric disorders, and subtype-selective allosteric…”
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Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists by Grimstrup, Marie, Receveur, Jean-Marie, Rist, Øystein, Frimurer, Thomas M., Nielsen, Peter Aadal, Mathiesen, Jesper M., Högberg, Thomas

“…SAR data have been supported by key analogues of thiazoleacetic acids and modelling studies to arrive at potent and novel chemotypes of CRTH2 antagonists. The…”
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