Search Results - "Smith, Nicola J."

Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes by Smith, Nicola J, Milligan, Graeme

“…For many years seven transmembrane domain G protein-coupled receptors (GPCRs) were thought to exist and function exclusively as monomeric units. However,…”
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International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1, -2, and -3: Pharmacology and Pathophysiological Functions by Stoddart, Leigh A, Smith, Nicola J, Milligan, Graeme

“…Identification of G protein-coupled receptors that are activated by free fatty acids has led to considerable interest in their pharmacology and function…”
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Drug Discovery Opportunities at the Endothelin B Receptor-Related Orphan G Protein-Coupled Receptors, GPR37 and GPR37L1 by Smith, Nicola J

“…Orphan G protein-coupled receptors (GPCRs) represent a largely untapped resource for the treatment of a variety of diseases, despite sophisticated advances in…”
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Allosteric modulation of heterodimeric G-protein-coupled receptors by Milligan, Graeme, Smith, Nicola J

“…G-protein-coupled receptors (GPCRs) are, and will probably remain, the most tractable class of targets for the development of small-molecule therapeutic…”
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Identifying ligands at orphan GPCRs: current status using structure‐based approaches by Ngo, Tony, Kufareva, Irina, Coleman, James LJ, Graham, Robert M, Abagyan, Ruben, Smith, Nicola J

“…GPCRs are the most successful pharmaceutical targets in history. Nevertheless, the pharmacology of many GPCRs remains inaccessible as their endogenous or…”
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Structural basis of promiscuous substrate transport by Organic Cation Transporter 1 by Zeng, Yi C., Sobti, Meghna, Quinn, Ada, Smith, Nicola J., Brown, Simon H. J., Vandenberg, Jamie I., Ryan, Renae M., O’Mara, Megan L., Stewart, Alastair G.

“…Organic Cation Transporter 1 (OCT1) plays a crucial role in hepatic metabolism by mediating the uptake of a range of metabolites and drugs. Genetic variations…”
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Biogeochemical cycling in the anthropocene: Quantifying global environment-economy exchanges by Smith, Nicola J, McDonald, Garry W, Patterson, Murray G

“…The Global Biogeochemical Cycles (GBCs) are extremely important biosphere functions, critical to the maintenance of conditions necessary for all life…”
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Critically evaluating sweet taste receptor expression and signaling through a molecular pharmacology lens by Smith, Nicola J., Grant, Jennifer N., Moon, Justin I., So, Sean S., Finch, Angela M.

“…The class C G protein‐coupled sweet taste receptor (STR) is responsible for the perception of sweet‐tasting molecules. Considered an obligate heterodimer, it…”
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Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements by Mohr, Klaus, Kostenis, Evi, Schröder, Ralf, Janssen, Nicole, Schmidt, Johannes, Kebig, Anna, Merten, Nicole, Hennen, Stephanie, Müller, Anke, Blättermann, Stefanie, Mohr-Andrä, Marion, Zahn, Sabine, Wenzel, Jörg, Smith, Nicola J, Gomeza, Jesús, Drewke, Christel, Milligan, Graeme

“…Label-free methods for assaying GPCR signaling promise to illuminate the effects of drugs in therapeutically relevant primary cells. Kostenis and colleagues…”
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Cryo-EM reveals distinct conformations of E. coli ATP synthase on exposure to ATP by Sobti, Meghna, Ishmukhametov, Robert, Bouwer, James C, Ayer, Anita, Suarna, Cacang, Smith, Nicola J, Christie, Mary, Stocker, Roland, Duncan, Thomas M, Stewart, Alastair G

“…ATP synthase produces the majority of cellular energy in most cells. We have previously reported cryo-EM maps of autoinhibited ATP synthase imaged without…”
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Regulation of mitochondrial metabolism in murine skeletal muscle by the medium‐chain fatty acid receptor Gpr84 by Montgomery, Magdalene K., Osborne, Brenna, Brandon, Amanda E., O'Reilly, Liam, Fiveash, Corrine E., Brown, Simon H. J., Wilkins, Brendan P., Samsudeen, Azrah, Yu, Josephine, Devanapalli, Beena, Hertzog, Ashley, Tolun, Adviye A., Kavanagh, Tomas, Cooper, Antony A., Mitchell, Todd W., Biden, Trevor J., Smith, Nicola J., Cooney, Gregory J., Turner, Nigel

“…Fatty acid receptors have been recognized as important players in glycaemic control. This study is the first to describe a role for the medium‐chain fatty acid…”
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A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor by Grundmann, Manuel, Tikhonova, Irina G, Hudson, Brian D, Smith, Nicola J, Mohr, Klaus, Ulven, Trond, Milligan, Graeme, Kenakin, Terry, Kostenis, Evi

“…Ligands targeting G protein-coupled receptors (GPCRs) are currently classified as either orthosteric, allosteric, or dualsteric/bitopic. Here, we introduce a…”
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Type 2 diabetes influences intraepithelial corneal nerve parameters and corneal stromal‐epithelial nerve penetration sites by Machet, Joshua, Park, Mijeong, Richardson, Alexander, Carnell, Michael, Mouat, Margaret A, Smith, Nicola J, Turner, Nigel, Cochran, Blake J, Rye, Kerry‐Anne, Di Girolamo, Nick

“…Introduction The quantification of intraepithelial corneal basal nerve parameters by in vivo confocal microscopy represents a promising modality to identify…”
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Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13 by Jenkins, Laura, Brea, Jose, Smith, Nicola J, Hudson, Brian D, Reilly, Graeme, Bryant, Nia J, Castro, Marian, Loza, María-Isabel, Milligan, Graeme

“…The poorly characterized G-protein-coupled receptor GPR35 has been suggested as a potential exploratory target for the treatment of both metabolic disorders…”
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Conserved Polar Residues in Transmembrane Domains V, VI, and VII of Free Fatty Acid Receptor 2 and Free Fatty Acid Receptor 3 Are Required for the Binding and Function of Short Chain Fatty Acids by Stoddart, Leigh A., Smith, Nicola J., Jenkins, Laura, Brown, Andrew J., Milligan, Graeme

“…FFA2 and FFA3 are closely related G protein-coupled receptors that bind and respond to short chain fatty acids. (FFA2 and FFA3 are the provisional…”
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Metalloprotease cleavage of the N terminus of the orphan G protein-coupled receptor GPR37L1 reduces its constitutive activity by Coleman, James L J, Ngo, Tony, Schmidt, Johannes, Mrad, Nadine, Liew, Chu Kong, Jones, Nicole M, Graham, Robert M, Smith, Nicola J

“…Little is known about the pharmacology or physiology of GPR37L1, a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor that is…”
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Retraction Note: Orphan receptor ligand discovery by pickpocketing pharmacological neighbors by Ngo, Tony, Ilatovskiy, Andrey V., Stewart, Alastair G., Coleman, James L. J., McRobb, Fiona M., Riek, R. Peter, Graham, Robert M., Abagyan, Ruben, Kufareva, Irina, Smith, Nicola J.

“…This article has been retracted. Please see the Retraction Notice for more detail: https://doi.org/10.1038/s41589-021-00746-1…”
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The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1 by Smith, Nicola J., Stoddart, Leigh A., Devine, Nicola M., Jenkins, Laura, Milligan, Graeme

“…The endogenous ligands for free fatty acid receptor 1 (FFA1) are medium and longer chain free fatty acids. However, a range of selective, small molecule…”
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Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3 by Milligan, Graeme, Stoddart, Leigh A., Smith, Nicola J.

“…The free fatty acid receptors FFA2 and FFA3 are recently de‐orphanized G protein‐coupled receptors that share a group of short‐chain free fatty acids as…”
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Deletion of Orphan G Protein-Coupled Receptor GPR37L1 in Mice Alters Cardiovascular Homeostasis in a Sex-Specific Manner by Mouat, Margaret A, Jackson, Kristy L, Coleman, James L J, Paterson, Madeleine R, Graham, Robert M, Head, Geoffrey A, Smith, Nicola J

“…GPR37L1 is a family A orphan G protein-coupled receptor (GPCR) with a putative role in blood pressure regulation and cardioprotection. In mice, genetic…”
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