Search Results - "Gentry, Patrick R"

Drugs for allosteric sites on receptors by Wenthur, Cody J, Gentry, Patrick R, Mathews, Thomas P, Lindsley, Craig W

“…The presence of druggable, topographically distinct allosteric sites on a wide range of receptor families has offered new paradigms for small molecules to…”
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Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats by Brady, Ashley E, Jones, Carrie K, Bridges, Thomas M, Kennedy, J Phillip, Thompson, Analisa D, Heiman, Justin U, Breininger, Micah L, Gentry, Patrick R, Yin, Huiyong, Jadhav, Satyawan B, Shirey, Jana K, Conn, P Jeffrey, Lindsley, Craig W

“…Previous clinical and animal studies suggest that selective activators of M(1) and/or M(4) muscarinic acetylcholine receptors (mAChRs) have potential as novel…”
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Novel Allosteric Modulators of G Protein-coupled Receptors by Gentry, Patrick R., Sexton, Patrick M., Christopoulos, Arthur

“…G protein-coupled receptors (GPCRs) are allosteric proteins, because their signal transduction relies on interactions between topographically distinct, yet…”
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Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins by Bridges, Thomas M, Marlo, Joy E, Niswender, Colleen M, Jones, Carrie K, Jadhav, Satyawan B, Gentry, Patrick R, Plumley, Hyekyung C, Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W

“…This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5…”
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Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5-Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe by Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Utley, Thomas J., Rajapakse, Anuruddha, Byers, Frank, Niswender, Colleen M., Morrison, Ryan D., Daniels, J. Scott, Wood, Michael R., Conn, P. Jeffrey, Lindsley, Craig W.

“…Of the five G‐protein‐coupled muscarinic acetylcholine receptors (mAChRs; M1–M5), M5 is the least explored and understood due to a lack of mAChR…”
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Synthesis and Structure–Activity Relationships of Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor by Kennedy, J. Phillip, Bridges, Thomas M., Gentry, Patrick R., Brogan, John T., Kane, Alexander S., Jones, Carrie K., Brady, Ashley E., Shirey, Jana K., Conn, P. Jeffrey, Lindsley, Craig W.

“…An iterative analogue library synthesis strategy rapidly developed comprehensive SAR data for a novel series of M4 positive allosteric modulators (PAMs). This…”
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Crystal structure of the M₅ muscarinic acetylcholine receptor by Vuckovic, Ziva, Gentry, Patrick R., Berizzi, Alice E., Hirata, Kunio, Varghese, Swapna, Thompson, Geoff, van der Westhuizen, Emma T., Burger, Wessel A. C., Rahmani, Raphaël, Valant, Celine, Langmead, Christopher J., Lindsley, Craig W., Baell, Jonathan B., Tobin, Andrew B., Sexton, Patrick M., Christopoulos, Arthur, Thal, David M.

“…The human M₅ muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug…”
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Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139 by Zhou, Yali, Daver, Henrik, Trapkov, Boris, Wu, Lijie, Wu, Meng, Harpsøe, Kasper, Gentry, Patrick R., Liu, Kaiwen, Larionova, Marina, Liu, Junlin, Chen, Na, Bräuner-Osborne, Hans, Gloriam, David E., Hua, Tian, Liu, Zhi-Jie

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In Vivo Structure−Activity Relationship Study of Dorsomorphin Analogues Identifies Selective VEGF and BMP Inhibitors by Hao, Jijun, Ho, Joshua N, Lewis, Jana A, Karim, Kaleh A, Daniels, R. Nathan, Gentry, Patrick R, Hopkins, Corey R, Lindsley, Craig W, Hong, Charles C

“…The therapeutic potential of small molecule signaling inhibitors is often limited by off-target effects. Recently, in a screen for compounds that perturb the…”
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Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139 by Pallareti, Lisa, Rath, Tine F., Trapkov, Boris, Tsonkov, Tsonko, Nielsen, Anders Thorup, Harpsøe, Kasper, Gentry, Patrick R., Bräuner-Osborne, Hans, Gloriam, David E., Foster, Simon R.

“…The orphan G protein-coupled receptor GPR139 is predominantly expressed in the central nervous system and has attracted considerable interest as a therapeutic…”
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Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators by Berizzi, Alice E, Gentry, Patrick R, Rueda, Patricia, Den Hoedt, Sandra, Sexton, Patrick M, Langmead, Christopher J, Christopoulos, Arthur

“…Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular…”
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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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M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location by Foster, Daniel J, Gentry, Patrick R, Lizardi-Ortiz, Jose E, Bridges, Thomas M, Wood, Michael R, Niswender, Colleen M, Sulzer, David, Lindsley, Craig W, Xiang, Zixiu, Conn, P Jeffrey

“…Of the five muscarinic receptor subtypes, the M5 receptor is the only one detectable in midbrain dopaminergic neurons, making it an attractive potential…”
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Identification of a novel scaffold for a small molecule GPR139 receptor agonist by Nøhr, Anne Cathrine, Shehata, Mohamed A., Palmer, Daniel, Pokhrel, Rina, Vallianou, Maria, Foster, Simon R., Gentry, Patrick R., Gloriam, David E., Bräuner-Osborne, Hans

“…GPR139 is an orphan G protein-coupled receptor (GPCR) that is primarily expressed in the brain in regions known to regulate motor control and metabolism. Here,…”
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Discovery of (S)‑2-Cyclopentyl‑N‑((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro‑1H‑pyrrido[3,4‑b]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM) by Morris, Lindsey C, Nance, Kellie D, Gentry, Patrick R, Days, Emily L, Weaver, C. David, Niswender, Colleen M, Thompson, Analisa D, Jones, Carrie K, Locuson, Chuck W, Morrison, Ryan D, Daniels, J. Scott, Niswender, Kevin D, Lindsley, Craig W

“…A duplexed, functional multiaddition high throughput screen and subsequent iterative parallel synthesis effort identified the first highly selective and CNS…”
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Crystal structure of the M 5 muscarinic acetylcholine receptor by Vuckovic, Ziva, Gentry, Patrick R, Berizzi, Alice E, Hirata, Kunio, Varghese, Swapna, Thompson, Geoff, van der Westhuizen, Emma T, Burger, Wessel A C, Rahmani, Raphaël, Valant, Celine, Langmead, Christopher J, Lindsley, Craig W, Baell, Jonathan B, Tobin, Andrew B, Sexton, Patrick M, Christopoulos, Arthur, Thal, David M

“…The human M muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug…”
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Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor by Burger, Wessel A. C, Gentry, Patrick R, Berizzi, Alice E, Vuckovic, Ziva, van der Westhuizen, Emma T, Thompson, Geoff, Yeasmin, Mahmuda, Lindsley, Craig W, Sexton, Patrick M, Langmead, Christopher J, Tobin, Andrew B, Christopoulos, Arthur, Valant, Celine, Thal, David M

“…The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders. This…”
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Identification of a Novel Allosteric Site at the M 5 Muscarinic Acetylcholine Receptor by Burger, Wessel A C, Gentry, Patrick R, Berizzi, Alice E, Vuckovic, Ziva, van der Westhuizen, Emma T, Thompson, Geoff, Yeasmin, Mahmuda, Lindsley, Craig W, Sexton, Patrick M, Langmead, Christopher J, Tobin, Andrew B, Christopoulos, Arthur, Valant, Celine, Thal, David M

“…The M muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders. This has…”
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Further optimization of the M5 NAM MLPCN probe ML375: Tactics and challenges by Kurata, Haruto, Gentry, Patrick R., Kokubo, Masaya, Cho, Hyekyung P., Bridges, Thomas M., Niswender, Colleen M., Byers, Frank W., Wood, Michael R., Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W.

“…[Display omitted] This Letter describes the continued optimization of the MLPCN probe ML375, a highly selective M5 negative allosteric modulator (NAM), through…”
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Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: The continued optimization of an MLPCN probe molecule by Poslusney, Michael S., Melancon, Bruce J., Gentry, Patrick R., Sheffler, Douglas J., Bridges, Thomas M., Utley, Thomas J., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.

“…This Letter describes the further optimization of an MLPCN probe molecule (ML137) through the introduction of 5- and 6-membered spirocycles in place of the…”
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