Search Results - "Ignar, Diane M."

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules by Briscoe, Celia P, Peat, Andrew J, McKeown, Stephen C, Corbett, David F, Goetz, Aaron S, Littleton, Thomas R, McCoy, David C, Kenakin, Terry P, Andrews, John L, Ammala, Carina, Fornwald, James A, Ignar, Diane M, Jenkinson, Stephen

“…1 Long chain fatty acids have recently been identified as agonists for the G protein‐coupled receptors GPR40 and GPR120. Here, we present the first description…”
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The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids by Brown, Andrew J, Goldsworthy, Susan M, Barnes, Ashley A, Eilert, Michelle M, Tcheang, Lili, Daniels, Dion, Muir, Alison I, Wigglesworth, Mark J, Kinghorn, Ian, Fraser, Neil J, Pike, Nicholas B, Strum, Jay C, Steplewski, Klaudia M, Murdock, Paul R, Holder, Julie C, Marshall, Fiona H, Szekeres, Philip G, Wilson, Shelagh, Ignar, Diane M, Foord, Steve M, Wise, Alan, Dowell, Simon J

“…GPR41 and GPR43 are related members of a homologous family of orphan G protein-coupled receptors that are tandemly encoded at a single chromosomal locus in…”
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Molecular Identification of High and Low Affinity Receptors for Nicotinic Acid by Wise, Alan, Foord, Steven M, Fraser, Neil J, Barnes, Ashley A, Elshourbagy, Nabil, Eilert, Michelle, Ignar, Diane M, Murdock, Paul R, Steplewski, Klaudia, Green, Andrew, Brown, Andrew J, Dowell, Simon J, Szekeres, Philip G, Hassall, David G, Marshall, Fiona H, Wilson, Shelagh, Pike, Nicholas B

“…Nicotinic acid has been used clinically for over 40 years in the treatment of dyslipidemia producing a desirable normalization of a range of cardiovascular…”
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Specific Inhibition of Orai1-mediated Calcium Signalling Resolves Inflammation and Clears Bacteria in an Acute Respiratory Distress Syndrome Model by Ahmad, Saira, Wrennall, Joe A., Goriounova, Alexandra S., Sekhri, Malika, Iskarpatyoti, Jason A., Ghosh, Arunava, Abdelwahab, Sabri H., Voeller, Alexis, Rai, Mani, Mahida, Rahul Y., Krajewski, Krzysztof, Ignar, Diane M., Greenbaum, Alon, Moran, Timothy P., Tilley, Stephen L., Thickett, David R., Sassano, M. Flori, Tarran, Robert

“…ELD607 is a novel Orai1 antagonist that shows promise in treating acute respiratory distress syndrome (ARDS) caused by bacterial pneumonia. ARDS has a high…”
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Potent, Selective, and Orally Efficacious Antagonists of Melanin-Concentrating Hormone Receptor 1 by Tavares, Francis X, Al-Barazanji, Kamal A, Bigham, Eric C, Bishop, Michael J, Britt, Christy S, Carlton, David L, Feldman, Paul L, Goetz, Aaron S, Grizzle, Mary K, Guo, Yu C, Handlon, Anthony L, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

“…The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat…”
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The Effect of PPARα, PPARδ, PPARγ, and PPARpan Agonists on Body Weight, Body Mass, and Serum Lipid Profiles in Diet-Induced Obese AKR/J Mice by Harrington, W. Wallace, Britt, Christy S., Wilson, Joan G., Milliken, Naphtali O., Binz, Jane G., Lobe, David C., Oliver, William R., Lewis, Michael C., Ignar, Diane M.

“…Activation of peroxisome proliferator-activated receptor (PPAR) α , δ , and γ subtypes increases expression of genes involved in fatty acid transport and…”
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Lysosomes contribute to anomalous pharmacokinetic behavior of melanocortin-4 receptor agonists by YUPING GONG, ZHIYANG ZHAO, MCCONN, Donavon J, BEAUDET, Beth, TALLMAN, Melanie, SPEAKE, Jason D, IGNAR, Diane M, KRISE, Jeffrey P

“…A series of melanocortin-4 receptor (MC4R) agonists, developed for use as anti-obesity agents, were found to have unusual pharmacokinetic behavior arising from…”
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Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single-Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ-Opioid Receptor Inverse Agonist by Nathan, Pradeep J., O'Neill, Barry V., Bush, Mark A., Koch, Annelize, Tao, Wenli X., Maltby, Kay, Napolitano, Antonella, Brooke, Allison C., Skeggs, Andrew L., Herman, Craig S., Larkin, Andrew L., Ignar, Diane M., Richards, Duncan B., Williams, Pauline M., Bullmore, Edward T.

“…Endogenous opioids and µ-opioid receptors have been linked to hedonic and rewarding aspects of palatable food intake. The authors examined the safety,…”
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Characterisation of olanzapine-induced weight gain and effect of aripiprazole vs olanzapine on body weight and prolactin secretion in female rats by KALINICHEV, Mikhail, ROURKE, Claire, DANIELS, Alex J, GRIZZLE, Mary K, BRITT, Christy S, IGNAR, Diane M, JONES, Declan N. C

“…Atypical antipsychotic drug (APD)-induced weight gain causes non-compliance, increasing the risk of relapse and medical complications. In an animal model, we…”
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The discovery and optimization of pyrimidinone-containing MCH R1 antagonists by Hertzog, Donald L., Al-Barazanji, Kamal A., Bigham, Eric C., Bishop, Michael J., Britt, Christy S., Carlton, David L., Cooper, Joel P., Daniels, Alex J., Garrido, Dulce M., Goetz, Aaron S., Grizzle, Mary K., Guo, Yu C., Handlon, Anthony L., Ignar, Diane M., Morgan, Ronda O., Peat, Andrew J., Tavares, Francis X., Zhou, Huiqiang

“…Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided potent and selective compounds that are…”
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A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity by Szewczyk, Jerzy R., Laudeman, Chris P., Sammond, Doug M., Villeneuve, Manon, Minick, Douglas J., Grizzle, Mary K., Daniels, Alejandro J., Andrews, John L., Ignar, Diane M.

“…Finding small non-peptide molecules for G protein-coupled receptors (GPCR) whose endogenous ligands are peptides, is a very important task for medicinal…”
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Novel benzimidazole-based MCH R1 antagonists by Carpenter, Andrew J., Al-Barazanji, Kamal A., Barvian, Kevin K., Bishop, Michael J., Britt, Christy S., Cooper, Joel P., Goetz, Aaron S., Grizzle, Mary K., Hertzog, Donald L., Ignar, Diane M., Morgan, Ronda O., Peckham, Gregory E., Speake, Jason D., Swain, Will R.

“…Structure–activity relationships and efforts to optimize pharmacokinetic properties of a class of benzimidazole-based MCH R1 antagonists are described. The…”
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6-(4-Chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-Based Melanin-Concentrating Hormone Receptor 1 Antagonist by Tavares, Francis X, Al-Barazanji, Kamal A, Bishop, Michael J, Britt, Christy S, Carlton, David L, Cooper, Joel P, Feldman, Paul L, Garrido, Dulce M, Goetz, Aaron S, Grizzle, Mary K, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, McIntyre, Maggie S, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

“…Genetic manipulation studies in mice at both the MCH receptor 1 (MCHR1) as well as the MCH peptide levels have implicated MCHR1 as a key player in energy…”
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Regulation of TNF-α secretion by a specific melanocortin-1 receptor peptide agonist by Ignar, Diane M., Andrews, John L., Jansen, Marilyn, Eilert, Michelle M., Pink, Heather M., Lin, Peiyuan, Sherrill, Ronald G., Szewczyk, Jerzy R., Conway, James G.

“…The lack of specific pharmacological tools has impeded the evaluation of the role of each melanocortin receptor (MCR) subtype in the myriad physiological…”
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Characterization of melanocortin receptors by Goetz, Aaron S, Ignar, Diane M

“…This unit describes a Scintillation Proximity Assay (SPA) for the measurement of ligand binding to melanocortin receptors (MCRs) using membranes prepared from…”
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Development of a facile method for high throughput screening with reporter gene assays by Goetz, A S, Andrews, J L, Littleton, T R, Ignar, D M

“…This report describes a facile methodology for high throughput screening with stable mammalian cell reporter gene assays. We have adapted a 96-well adherent…”
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Coupling of Dual Signaling Pathways: Epidermal Growth Factor Action Involves the Estrogen Receptor by Ignar-Trowbridge, Diane M., Nelson, Karen G., Bidwell, Mark C., Curtis, Sylvia W., Washburn, Todd F., McLachlan, John A., Korach, Kenneth S.

“…Epidermal growth factor (EGF) reproduces many of the effects of estrogen on the murine female reproductive tract and may partially mediate estrogen-induced…”
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A combination assay for simultaneous assessment of multiple signaling pathways by Goetz, Aaron S, Liacos, James, Yingling, Jeff, Ignar, Diane M

“…We have developed an assay in which modulation of two or more signaling pathways can be assessed concurrently by combining reporter gene systems with…”
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The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids by Briscoe, Celia P, Tadayyon, Mohammad, Andrews, John L, Benson, William G, Chambers, Jon K, Eilert, Michelle M, Ellis, Catherine, Elshourbagy, Nabil A, Goetz, Aaron S, Minnick, Dana T, Murdock, Paul R, Sauls, Jr, Howard R, Shabon, Usman, Spinage, Lisa D, Strum, Jay C, Szekeres, Philip G, Tan, Kong B, Way, James M, Ignar, Diane M, Wilson, Shelagh, Muir, Alison I

“…GPR40 is a member of a subfamily of homologous G protein-coupled receptors that include GPR41 and GPR43 and that have no current function or ligand ascribed…”
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Specific Inhibition of Orai1-mediated Calcium Signalling Resolves Inflammation and Clears Bacteria in an ARDS Model by Ahmad, Saira, Wrennall, Joe A, Goriounova, Alexandra S, Sekhri, Malika, Iskarpatyoti, Jason A, Ghosh, Arunava, Abdelwahab, Sabri H, Voeller, Alexis, Rai, Mani, Mahida, Rahul Y, Krajewski, Krzysztof, Ignar, Diane M, Greenbaum, Alon, Moran, Timothy P, Tilley, Stephen L, Thickett, David R, Sassano, M Flori, Tarran, Robert

“…Acute Respiratory Distress Syndrome (ARDS) has an unacceptably high mortality rate (35%) and is without effective therapy. Orai1 is a Ca channel involved in…”
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