Patrick Ryan Gentry

Research output

Research output per year 2008 2009 2010 2013 2014 2019

• 22 Journal article
• 2 Review
• 1 Ph.D. thesis
• 1 Patent

Research output per year

Research output per year

Search results

• 2019

  Identification of a novel scaffold for a small molecule GPR139 receptor agonist

  Nøhr, A. C., Shehata, M. A., Palmer, D., Pokhrel, R., Vallianou, M., Foster, S. R., Gentry, P. R., Gloriam, D. E. & Bräuner-Osborne, H., 1 Dec 2019, In: Scientific Reports. 9, 1, p. 3802

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Pharmaceutical Chemistry 100%
  • Calcium 99%
  • G-Protein-Coupled Receptors 73%
  • Mutagenesis 71%
  • Libraries 64%
  3 Citations (Scopus)
• 2018

  Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

  Bender, A. M., Cho, H. P., Nance, K. D., Lingenfelter, K. S., Luscombe, V. B., Gentry, P. R., Voigtritter, K., Berizzi, A. E., Sexton, P. M., Langmead, C. J., Christopoulos, A., Locuson, C. W., Bridges, T. M., Chang, S., O'Neill, J. C., Zhan, X., Niswender, C. M., Jones, C. K., Conn, P. J. & Lindsley, C. W., 18 Jul 2018, In: ACS Chemical Neuroscience. 9, 7, p. 1572-1581 10 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • piperidine 100%
  • Parasympathomimetic Agent 86%
  • Amides 82%
  • Muscarinic Receptors 76%
  • Acetylcholine 74%
  3 Citations (Scopus)
• 2016

  Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

  Gogliotti, R. D., Engers, D. W., Garcia-Barrantes, P. M., Panarese, J. D., Gentry, P. R., Blobaum, A. L., Morrison, R. D., Daniels, J. S., Thompson, A. D., Jones, C. K., Conn, P. J., Niswender, C. M., Lindsley, C. W. & Hopkins, C. R., 15 Jun 2016, In: Bioorganic & Medicinal Chemistry Letters. 26, 12, p. 2915-2919 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 3-aminopicolinamide 100%
  • picolinamide 79%
  • metabotropic glutamate receptor 4 65%
  • Picolinamide 59%
  • Catalepsy 26%
  2 Citations (Scopus)

• Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators

  Berizzi, A. E., Gentry, P. R., Rueda, P., Den Hoedt, S., Sexton, P. M., Langmead, C. J. & Christopoulos, A., Oct 2016, In: Molecular Pharmacology. 90, 4, p. 427-36 10 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Muscarinic Receptors 100%
  • Inositol Phosphates 57%
  • Pilocarpine 56%
  • Acetylcholine 42%
  • oxotremorine M 38%
  15 Citations (Scopus)
• 2015

  Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges

  Kurata, H., Gentry, P. R., Kokubo, M., Cho, H. P., Bridges, T. M., Niswender, C. M., Byers, F. W., Wood, M. R., Daniels, J. S., Conn, P. J. & Lindsley, C. W., 1 Feb 2015, In: Bioorganic & Medicinal Chemistry Letters. 25, 3, p. 690-4 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Libraries 100%
  • 1-aminobenzotriazole 97%
  • Deuterium 78%
  • Probe 68%
  • Deuterium(.) 50%
  12 Citations (Scopus)

• Novel Allosteric Modulators of G Protein-coupled Receptors

  Gentry, P. R., Sexton, P. M. & Christopoulos, A., 7 Aug 2015, In: The Journal of Biological Chemistry. 290, 32, p. 19478-88 11 p.

  Research output: Contribution to journal › Review › peer-review

  • G-Protein-Coupled Receptors 100%
  • Allosteric Site 70%
  • Signal Transduction 53%
  • Probe 30%
  • Drug 26%
  108 Citations (Scopus)
• 2014

  Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

  Gentry, P. R., Kokubo, M., Bridges, T. M., Noetzel, M. J., Cho, H. P., Lamsal, A., Smith, E., Chase, P., Hodder, P. S., Niswender, C. M., Daniels, J. S., Conn, P. J., Lindsley, C. W. & Wood, M. R., 25 Sept 2014, In: Journal of Medicinal Chemistry. 57, 18, p. 7804-10 7 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • piperidine-4-carboxamide 100%
  • Parasympathomimetic Agent 55%
  • Muscarinic Receptors 49%
  • Acetylcholine 47%
  • Plasma 27%
  17 Citations (Scopus)

• Discovery, optimization, and characterization of novel subtype-selective M5 muscarinic acetylcholine receptor ligands

  Gentry, P. R., Aug 2014

  Research output: Book/Report › Ph.D. thesis

• Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

  Gentry, P. R., Kokubo, M., Bridges, T. M., Cho, H. P., Smith, E., Chase, P., Hodder, P. S., Utley, T. J., Rajapakse, A., Byers, F., Niswender, C. M., Morrison, R. D., Daniels, J. S., Wood, M. R., Conn, P. J. & Lindsley, C. W., Aug 2014, In: ChemMedChem. 9, 8, p. 1677-82 6 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 5-((3-acetylphenoxy)methyl)-N-methyl-N-(1-(pyridin-2-yl)ethyl)isoxazole-3-carboxamide 100%
  • Molecular Probes 52%
  • Parasympathomimetic Agent 48%
  • Molecular Probe 45%
  • Muscarinic Receptors 42%
  15 Citations (Scopus)

• 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)

  Morris, L. C., Nance, K. D., Gentry, P. R., Days, E. L., Weaver, C. D., Niswender, C. M., Thompson, A. D., Jones, C. K., Locuson, C. W., Morrison, R. D., Daniels, J. S., Niswender, K. D. & Lindsley, C. W., 11 Dec 2014, In: Journal of Medicinal Chemistry. 57, 23, p. 10192-7 6 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido(3,4-b)indole-4-carboxamide 100%
  • Glucagon-Like Peptide 1 61%
  • Glucagon-Like Peptides 59%
  • Catalepsy 53%
  • Exenatide 52%
  28 Citations (Scopus)

• Drugs for allosteric sites on receptors

  Wenthur, C. J., Gentry, P. R., Mathews, T. P. & Lindsley, C. W., Jan 2014, In: Annual Review of Pharmacology and Toxicology. 54, p. 165-84 20 p.

  Research output: Contribution to journal › Review › peer-review

  • Allosteric Site 100%
  • Ligands 49%
  • Drug 37%
  • Ligand 30%
  • Pharmaceutical Preparations 29%
  132 Citations (Scopus)

• M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location

  Foster, D. J., Gentry, P. R., Lizardi-Ortiz, J. E., Bridges, T. M., Wood, M. R., Niswender, C. M., Sulzer, D., Lindsley, C. W., Xiang, Z. & Conn, P. J., 26 Feb 2014, In: The Journal of neuroscience : the official journal of the Society for Neuroscience. 34, 9, p. 3253-62 10 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione 100%
  • Pars Compacta 81%
  • Dopaminergic Neurons 66%
  • Neurons 25%
  • Mesencephalon 21%
  41 Citations (Scopus)
• 2013

  Discovery of ML326: The first sub-micromolar, selective M5 PAM

  Gentry, P. R., Bridges, T. M., Lamsal, A., Vinson, P. N., Smith, E., Chase, P., Hodder, P. S., Engers, J. L., Niswender, C. M., Daniels, J. S., Conn, P. J., Wood, M. R. & Lindsley, C. W., 15 May 2013, In: Bioorganic & Medicinal Chemistry Letters. 23, 10, p. 2996-3000 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Isatin 100%
  • Ether 66%
  • Probe 18%
  • ML326 9%
  15 Citations (Scopus)

• Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

  Gentry, P. R., Kokubo, M., Bridges, T. M., Kett, N. R., Harp, J. M., Cho, H. P., Smith, E., Chase, P., Hodder, P. S., Niswender, C. M., Daniels, J. S., Conn, P. J., Wood, M. R. & Lindsley, C. W., 27 Nov 2013, In: Journal of Medicinal Chemistry. 56, 22, p. 9351-5 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo(2,1-a)isoindol-5(9bH)-one 100%
  • Parasympathomimetic Agent 48%
  • Muscarinic Receptors 42%
  • Acetylcholine 41%
  • Inhibitory Concentration 50 35%
  33 Citations (Scopus)

• Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule

  Melancon, B. J., Poslusney, M. S., Gentry, P. R., Tarr, J. C., Sheffler, D. J., Mattmann, M. E., Bridges, T. M., Utley, T. J., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Wood, M. R., 15 Jan 2013, In: Bioorganic & Medicinal Chemistry Letters. 23, 2, p. 412-6 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • ML 137 100%
  • Isatin 67%
  • Parasympathomimetic Agent 49%
  • Cholinergic Agents 37%
  • Probe 24%
  19 Citations (Scopus)

• Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule

  Poslusney, M. S., Melancon, B. J., Gentry, P. R., Sheffler, D. J., Bridges, T. M., Utley, T. J., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Wood, M. R., 15 Mar 2013, In: Bioorganic & Medicinal Chemistry Letters. 23, 6, p. 1860-4 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • ML 137 100%
  • Isatin 67%
  • Parasympathomimetic Agent 49%
  • Cholinergic Agents 37%
  • Structure-Activity Relationship 34%
  23 Citations (Scopus)
• 2012

  MGluR4 allosteric potentiators and their preparation, compositions, and methods of treating neurological dysfunction

  Conn, P. J., Lindsley, C. W., Hopkins, C. R., Weaver, D., Niswender, C. M., Engers, D. W., Gentry, P. R., Cheung, Y-Y., Salovich, J. & Gogliotti, R. D., 27 Sept 2012, Patent No. US20120245153A1, 4 Sept 2010

  Research output: Patent
• 2010

  Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM

  Bridges, T. M., Kennedy, J. P., Cho, H. P., Breininger, M. L., Gentry, P. R., Hopkins, C. R., Conn, P. J. & Lindsley, C. W., 15 Jan 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 2, p. 558-62 5 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione 100%
  • Lead 38%
  36 Citations (Scopus)

• Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM

  Bridges, T. M., Phillip Kennedy, J., Noetzel, M. J., Breininger, M. L., Gentry, P. R., Conn, P. J. & Lindsley, C. W., 15 Mar 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 6, p. 1972-5 4 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Lead 100%
  48 Citations (Scopus)

• In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors

  Hao, J., Ho, J. N., Lewis, J. A., Karim, K. A., Daniels, R. N., Gentry, P. R., Hopkins, C. R., Lindsley, C. W. & Hong, C. C., 19 Feb 2010, In: ACS chemical biology. 5, 2, p. 245-53 9 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Dorsomorphin 100%
  • dorsomorphin 75%
  • Bone Morphogenetic Proteins 55%
  • Structure-Activity Relationship 53%
  • Vascular Endothelial Growth Factor A 39%
  253 Citations (Scopus)

• Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

  Engers, D. W., Gentry, P. R., Williams, R., Bolinger, J. D., Weaver, C. D., Menon, U. N., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., 1 Sept 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 17, p. 5175-8 4 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • High Throughput Screening 100%
  21 Citations (Scopus)
• 2009

  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

  Bridges, T. M., Marlo, J. E., Niswender, C. M., Jones, C. K., Jadhav, S. B., Gentry, P. R., Plumley, H. C., Weaver, C. D., Conn, P. J. & Lindsley, C. W., 11 Jun 2009, In: Journal of Medicinal Chemistry. 52, 11, p. 3445-8 4 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione 100%
  • Isatin 70%
  • Parasympathomimetic Agent 52%
  • Muscarinic Receptors 46%
  • Acetylcholine 45%
  79 Citations (Scopus)

• Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

  Williams, R., Johnson, K. A., Gentry, P. R., Niswender, C. M., Weaver, C. D., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., 1 Sept 2009, In: Bioorganic & Medicinal Chemistry Letters. 19, 17, p. 4967-70 4 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • VU 0155041 100%
  • metabotropic glutamate receptor 4 78%
  • Parkinson Disease 19%
  • Rodentia 19%
  25 Citations (Scopus)

• Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor

  Kennedy, J. P., Bridges, T. M., Gentry, P. R., Brogan, J. T., Kane, A. S., Jones, C. K., Brady, A. E., Shirey, J. K., Conn, P. J. & Lindsley, C. W., Oct 2009, In: ChemMedChem. 4, 10, p. 1600-7 8 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  33 Citations (Scopus)
• 2008

  Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats

  Brady, A. E., Jones, C. K., Bridges, T. M., Kennedy, J. P., Thompson, A. D., Heiman, J. U., Breininger, M. L., Gentry, P. R., Yin, H., Jadhav, S. B., Shirey, J. K., Conn, P. J. & Lindsley, C. W., Dec 2008, In: The Journal of Pharmacology and Experimental Therapeutics. 327, 3, p. 941-53 13 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • 3-amino-N-(4-methoxybenzyl)-4,6-dimethylthieno(2,3-b)pyridine-2-carboxamide 100%
  • Muscarinic Receptors 49%
  • Amphetamine 49%
  • pyridine 29%
  • Antipsychotic Agents 20%
  148 Citations (Scopus)

• Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

  Bridges, T. M., Brady, A. E., Kennedy, J. P., Daniels, R. N., Miller, N. R., Kim, K., Breininger, M. L., Gentry, P. R., Brogan, J. T., Jones, C. K., Conn, P. J. & Lindsley, C. W., 15 Oct 2008, In: Bioorganic & Medicinal Chemistry Letters. 18, 20, p. 5439-42 4 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

  • Agonist 100%
  • Libraries 92%
  36 Citations (Scopus)