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Items: 1 to 20 of 102


Identification of novel allosteric modulators of mGlu5 acting at site distinct from MPEP binding.

Butkiewicz M, Rodriguez AL, Rainey SE, Wieting JM, Luscombe VB, Stauffer SR, Lindsley CW, Conn PJ, Meiler J.

ACS Chem Neurosci. 2019 May 27. doi: 10.1021/acschemneuro.8b00227. [Epub ahead of print]


Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5.

Rodriguez AL, Tarr JC, Zhou Y, Williams R, Gregory KJ, Bridges TM, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 17 [updated 2013 Mar 22].


Development of allosteric modulators of GPCRs for treatment of CNS disorders.

Nickols HH, Conn PJ.

Neurobiol Dis. 2014 Jan;61:55-71. doi: 10.1016/j.nbd.2013.09.013. Epub 2013 Sep 27. Review.


A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.

Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ.

Mol Pharmacol. 2013 Apr;83(4):835-47. doi: 10.1124/mol.112.082891. Epub 2013 Jan 24. Erratum in: Mol Pharmacol. 2013 Oct;84(4):654.


Identification of a high affinity MPEP-site silent allosteric modulator (SAM) for the metabotropic glutamate subtype 5 receptor (mGlu5).

Gregory KJ, Malosh C, Turlington M, Morrison R, Vinson P, Daniels JS, Jones C, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 15 [updated 2015 Feb 11].


Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.

Hammond AS, Rodriguez AL, Townsend SD, Niswender CM, Gregory KJ, Lindsley CW, Conn PJ.

ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. Epub 2010 Aug 19.


"Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands.

Hellyer SD, Albold S, Wang T, Chen ANY, May LT, Leach K, Gregory KJ.

Mol Pharmacol. 2018 May;93(5):504-514. doi: 10.1124/mol.117.111518. Epub 2018 Mar 7.


Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.

Gregory KJ, Nguyen ED, Malosh C, Mendenhall JL, Zic JZ, Bates BS, Noetzel MJ, Squire EF, Turner EM, Rook JM, Emmitte KA, Stauffer SR, Lindsley CW, Meiler J, Conn PJ.

ACS Chem Neurosci. 2014 Apr 16;5(4):282-95. doi: 10.1021/cn400225x. Epub 2014 Feb 26.


Targeting metabotropic glutamate receptors for novel treatments of schizophrenia.

Maksymetz J, Moran SP, Conn PJ.

Mol Brain. 2017 Apr 26;10(1):15. doi: 10.1186/s13041-017-0293-z. Review.


Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.

Anighoro A, Graziani D, Bettinelli I, Cilia A, De Toma C, Longhi M, Mangiarotti F, Menegon S, Pirona L, Poggesi E, Riva C, Rastelli G.

Bioorg Med Chem. 2015 Jul 1;23(13):3040-58. doi: 10.1016/j.bmc.2015.05.008. Epub 2015 May 12.


Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology.

Sengmany K, Hellyer SD, Albold S, Wang T, Conn PJ, May LT, Christopoulos A, Leach K, Gregory KJ.

Neuropharmacology. 2019 May 1;149:83-96. doi: 10.1016/j.neuropharm.2019.02.005. Epub 2019 Feb 11.


Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology.

Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ.

Mol Pharmacol. 2013 May;83(5):991-1006. doi: 10.1124/mol.112.083949. Epub 2013 Feb 26.


Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine.

Malherbe P, Kratochwil N, Zenner MT, Piussi J, Diener C, Kratzeisen C, Fischer C, Porter RH.

Mol Pharmacol. 2003 Oct;64(4):823-32.


Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5.

Chen ANY, Hellyer SD, Trinh PNH, Leach K, Gregory KJ.

Basic Clin Pharmacol Toxicol. 2019 Apr 14. doi: 10.1111/bcpt.13239. [Epub ahead of print]


Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5.

Bian Y, Feng Z, Yang P, Xie XQ.

AAPS J. 2017 Jul;19(4):1235-1248. doi: 10.1208/s12248-017-0093-5. Epub 2017 May 30.


SAR studies on mGlu5 receptor positive allosteric modulators (2003- 2013).

Hao J, Xiong H.

Curr Top Med Chem. 2014;14(15):1789-841. Review.


Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.

Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Neuropsychopharmacology. 2015 Feb;40(3):755-65. doi: 10.1038/npp.2014.245. Epub 2014 Sep 22.


Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia.

Bradley SJ, Langmead CJ, Watson JM, Challiss RA.

Mol Pharmacol. 2011 May;79(5):874-85. doi: 10.1124/mol.110.068882. Epub 2011 Feb 14.

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