Search Results - "Rominger, David H."

Biased mu-opioid receptor ligands: a promising new generation of pain therapeutics by Siuda, Edward R, Carr, Richard, Rominger, David H, Violin, Jonathan D

“…Highlights • Biased MOR ligands discovered using empirical, rational and natural product approaches. • Biased MOR ligands produce analgesia with fewer side…”
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Evidence for allosteric interactions of antagonist binding to the smoothened receptor by Rominger, Cynthia M, Bee, Wei-Lin Tiger, Copeland, Robert A, Davenport, Elizabeth A, Gilmartin, Aidan, Gontarek, Richard, Hornberger, Keith R, Kallal, Lorena A, Lai, Zhihong, Lawrie, Kenneth, Lu, Quinn, McMillan, Lynette, Truong, Maggie, Tummino, Peter J, Turunen, Brandon, Will, Matthew, Zuercher, William J, Rominger, David H

“…The Smoothened receptor (Smo) mediates hedgehog (Hh) signaling critical for development, cell growth, and migration, as well as stem cell maintenance. Aberrant…”
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Quantifying ligand bias at seven-transmembrane receptors by Rajagopal, Sudarshan, Ahn, Seungkirl, Rominger, David H, Gowen-MacDonald, William, Lam, Christopher M, Dewire, Scott M, Violin, Jonathan D, Lefkowitz, Robert J

“…Seven transmembrane receptors (7TMRs), commonly referred to as G protein-coupled receptors, form a large part of the "druggable" genome. 7TMRs can signal…”
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Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance by Violin, Jonathan D, DeWire, Scott M, Yamashita, Dennis, Rominger, David H, Nguyen, Lisa, Schiller, Kevin, Whalen, Erin J, Gowen, Maxine, Lark, Michael W

“…Biased G protein-coupled receptor ligands engage subsets of the receptor signals normally stimulated by unbiased agonists. However, it is unclear whether…”
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Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)‑9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain by Chen, Xiao-Tao, Pitis, Philip, Liu, Guodong, Yuan, Catherine, Gotchev, Dimitar, Cowan, Conrad L, Rominger, David H, Koblish, Michael, DeWire, Scott M, Crombie, Aimee L, Violin, Jonathan D, Yamashita, Dennis S

“…The concept of “ligand bias” at G protein coupled receptors has been introduced to describe ligands which preferentially stimulate one intracellular signaling…”
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Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR) by Strachan, Ryan T., Sun, Jin-peng, Rominger, David H., Violin, Jonathan D., Ahn, Seungkirl, Rojas Bie Thomsen, Alex, Zhu, Xiao, Kleist, Andrew, Costa, Tommaso, Lefkowitz, Robert J.

“…The concept of “biased agonism” arises from the recognition that the ability of an agonist to induce a receptor-mediated response (i.e. “efficacy”) can differ…”
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TRV0109101, a G Protein-Biased Agonist of the µ -Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration by Koblish, Michael, Carr, 3rd, Richard, Siuda, Edward R, Rominger, David H, Gowen-MacDonald, William, Cowan, Conrad L, Crombie, Aimee L, Violin, Jonathan D, Lark, Michael W

“…Prescription opioids are a mainstay in the treatment of acute moderate to severe pain. However, chronic use leads to a host of adverse consequences including…”
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Biased ligands: pathway validation for novel GPCR therapeutics by Rominger, David H, Cowan, Conrad L, Gowen-MacDonald, William, Violin, Jonathan D

“…Graphical abstract…”
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A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine by DeWire, Scott M, Yamashita, Dennis S, Rominger, David H, Liu, Guodong, Cowan, Conrad L, Graczyk, Thomas M, Chen, Xiao-Tao, Pitis, Philip M, Gotchev, Dimitar, Yuan, Catherine, Koblish, Michael, Lark, Michael W, Violin, Jonathan D

“…The concept of ligand bias at G protein-coupled receptors broadens the possibilities for agonist activities and provides the opportunity to develop safer, more…”
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Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies by Rominger, D H, Rominger, C M, Fitzgerald, L W, Grzanna, R, Largent, B L, Zaczek, R

“…We describe the binding of [125I]tyr(o)sauvagine to membranes of corticotropin-releasing hormone (CRH2) receptor expressing HEK293/EBNA (293ECRH2 alpha) cells…”
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Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors by Zhang, Ge, Huang, Ning, Li, Yu-Wen, Qi, Xiaoping, Marshall, Anne P, Yan, Xiao-Xin, Hill, Geraldine, Rominger, Cynthia, Prakash, Shimoga R, Bakthavatchalam, Rajagopal, Rominger, David H, Gilligan, Paul J, Zaczek, Robert

“…The in vitro pharmacological profile of a novel small molecule corticotropin-releasing factor 1 (CRF(1)) receptor antagonist,…”
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Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors by Seiffert, Dietmar, Bradley, Jodi D., Rominger, Cynthia M., Rominger, David H., Yang, Fude, Meredith, Jere E., Wang, Qian, Roach, Arthur H., Thompson, Lorin A., Spitz, Susan M., Higaki, Jeffrey N., Prakash, Shimoga R., Combs, Andrew P., Copeland, Robert A., Arneric, Stephen P., Hartig, Paul R., Robertson, David W., Cordell, Barbara, Stern, Andrew M., Olson, Richard E., Zaczek, Robert

“…Presenilins are integral membrane protein involved in the production of amyloid β-protein. Mutations of the presenilin-1 and -2 gene are associated with…”
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Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors by Dietmar Seiffert, Jodi D. Bradley, Cynthia M. Rominger, David H. Rominger, Fude Yang, Jere E. Meredith, Jr, Qian Wang, Arthur H. Roach, Lorin A. Thompson, Susan M. Spitz, Jeffrey N. Higaki, Shimoga R. Prakash, Andrew P. Combs, Robert A. Copeland, Stephen P. Arneric, Paul R. Hartig, David W. Robertson, Barbara Cordell, Andrew M. Stern, Richard E. Olson, Robert Zaczek

“…Presenilins are integral membrane protein involved in the production of amyloid β-protein. Mutations of the presenilin-1 and -2 gene are associated with…”
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