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Items: 48


mGlu5 Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu5-Endocannabinoid Signaling.

Xiang Z, Lv X, Maksymetz J, Stansley BJ, Ghoshal A, Gogliotti RG, Niswender CM, Lindsley CW, Conn PJ.

ACS Pharmacol Transl Sci. 2019 Jun 14;2(3):198-209. doi: 10.1021/acsptsci.9b00017. Epub 2019 May 15.


A Coordinated Attack: Rett Syndrome Therapeutic Development.

Gogliotti RG, Niswender CM.

Trends Pharmacol Sci. 2019 Apr;40(4):233-236. doi: 10.1016/ Review.


Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.

Aho ER, Wang J, Gogliotti RD, Howard GC, Phan J, Acharya P, Macdonald JD, Cheng K, Lorey SL, Lu B, Wenzel S, Foshage AM, Alvarado J, Wang F, Shaw JG, Zhao B, Weissmiller AM, Thomas LR, Vakoc CR, Hall MD, Hiebert SW, Liu Q, Stauffer SR, Fesik SW, Tansey WP.

Cell Rep. 2019 Mar 12;26(11):2916-2928.e13. doi: 10.1016/j.celrep.2019.02.047.


Mechanisms underlying prelimbic prefrontal cortex mGlu3/mGlu5-dependent plasticity and reversal learning deficits following acute stress.

Joffe ME, Santiago CI, Stansley BJ, Maksymetz J, Gogliotti RG, Engers JL, Nicoletti F, Lindsley CW, Conn PJ.

Neuropharmacology. 2019 Jan;144:19-28. doi: 10.1016/j.neuropharm.2018.10.013. Epub 2018 Oct 13.


Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.

Wang F, Jeon KO, Salovich JM, Macdonald JD, Alvarado J, Gogliotti RD, Phan J, Olejniczak ET, Sun Q, Wang S, Camper D, Yuh JP, Shaw JG, Sai J, Rossanese OW, Tansey WP, Stauffer SR, Fesik SW.

J Med Chem. 2018 Jul 12;61(13):5623-5642. doi: 10.1021/acs.jmedchem.8b00375. Epub 2018 Jun 29.


Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target.

Gogliotti RG, Fisher NM, Stansley BJ, Jones CK, Lindsley CW, Conn PJ, Niswender CM.

J Pharmacol Exp Ther. 2018 May;365(2):291-300. doi: 10.1124/jpet.117.246991. Epub 2018 Mar 9.


Genetic Reduction or Negative Modulation of mGlu7 Does Not Impact Anxiety and Fear Learning Phenotypes in a Mouse Model of MECP2 Duplication Syndrome.

Fisher NM, Gogliotti RG, Vermudez SAD, Stansley BJ, Conn PJ, Niswender CM.

ACS Chem Neurosci. 2018 Sep 19;9(9):2210-2217. doi: 10.1021/acschemneuro.7b00414. Epub 2017 Dec 14.


Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5.

Stansley BJ, Fisher NM, Gogliotti RG, Lindsley CW, Conn PJ, Niswender CM.

Cereb Cortex. 2018 Dec 1;28(12):4291-4304. doi: 10.1093/cercor/bhx282.


Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.

ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115. doi: 10.1021/acsmedchemlett.7b00317. eCollection 2017 Oct 12.


mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

Gogliotti RG, Senter RK, Fisher NM, Adams J, Zamorano R, Walker AG, Blobaum AL, Engers DW, Hopkins CR, Daniels JS, Jones CK, Lindsley CW, Xiang Z, Conn PJ, Niswender CM.

Sci Transl Med. 2017 Aug 16;9(403). pii: eaai7459. doi: 10.1126/scitranslmed.aai7459.


Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):2984-2987. doi: 10.1016/j.bmcl.2016.05.029. Epub 2016 May 11.


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

Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2915-2919. doi: 10.1016/j.bmcl.2016.04.041. Epub 2016 Apr 19.


Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

ACS Chem Neurosci. 2016 Sep 21;7(9):1192-200. doi: 10.1021/acschemneuro.6b00035. Epub 2016 May 3.


mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome.

Gogliotti RG, Senter RK, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones CK, Lindsley CW, Conn PJ, Niswender CM.

Hum Mol Genet. 2016 May 15;25(10):1990-2004. Epub 2016 Mar 2.


The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia.

Ponnazhagan R, Harms AS, Thome AD, Jurkuvenaite A, Gogliotti R, Niswender CM, Conn PJ, Standaert DG.

J Neuroimmune Pharmacol. 2016 Jun;11(2):231-7. doi: 10.1007/s11481-016-9655-z. Epub 2016 Feb 12.


Pharmacological Treatments for Autism Spectrum Disorder: Will Emerging Approaches Yield New Treatments?

Gogliotti RG, Conn PJ.

Neuropsychopharmacology. 2016 Jan;41(1):376-7. doi: 10.1038/npp.2015.259. Review. No abstract available.


Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.

Senter T, Gogliotti RD, Han C, Locuson CW, Morrison R, Daniels JS, Cierpicki T, Grembecka J, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2015 Jul 1;25(13):2720-5. doi: 10.1016/j.bmcl.2015.04.026. Epub 2015 Apr 25.


Progress towards small molecule inhibitors of the Menin-Mixed Lineage Leukemia (MLL) interaction with in vivo utility.

Senter T, Gogliotti R, Han C, Locuson CW II, Morrison R, Daniels JS, Cierpicki T, Grembecka J, 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].


High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction.

He S, Senter TJ, Pollock J, Han C, Upadhyay SK, Purohit T, Gogliotti RD, Lindsley CW, Cierpicki T, Stauffer SR, Grembecka J.

J Med Chem. 2014 Feb 27;57(4):1543-56. doi: 10.1021/jm401868d. Epub 2014 Feb 6.


Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.


Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.

Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS.

Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.


Pure Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.

Zhou Y, Chun A, Gogliotti RD, Dawson ES, Vinson PN, Niswender CM, Noetzel MJ, Rook JM, Bridges TM, Daniels JS, Jones C, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2013 Mar 7].


The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models.

Gogliotti RG, Cardona H, Singh J, Bail S, Emery C, Kuntz N, Jorgensen M, Durens M, Xia B, Barlow C, Heier CR, Plasterer HL, Jacques V, Kiledjian M, Jarecki J, Rusche J, DiDonato CJ.

Hum Mol Genet. 2013 Oct 15;22(20):4084-101. doi: 10.1093/hmg/ddt258. Epub 2013 Jun 4.


Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels.

Raphemot R, Rouhier MF, Hopkins CR, Gogliotti RD, Lovell KM, Hine RM, Ghosalkar D, Longo A, Beyenbach KW, Denton JS, Piermarini PM.

PLoS One. 2013 May 29;8(5):e64905. doi: 10.1371/journal.pone.0064905. Print 2013.


Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Biol Psychiatry. 2013 Mar 15;73(6):501-9. doi: 10.1016/j.biopsych.2012.09.012. Epub 2012 Nov 7.


Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR.

Bioorg Med Chem Lett. 2012 May 15;22(10):3467-72. doi: 10.1016/j.bmcl.2012.03.088. Epub 2012 Mar 29.


Motor neuron rescue in spinal muscular atrophy mice demonstrates that sensory-motor defects are a consequence, not a cause, of motor neuron dysfunction.

Gogliotti RG, Quinlan KA, Barlow CB, Heier CR, Heckman CJ, Didonato CJ.

J Neurosci. 2012 Mar 14;32(11):3818-29. doi: 10.1523/JNEUROSCI.5775-11.2012.


Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1.

Raphemot R, Lonergan DF, Nguyen TT, Utley T, Lewis LM, Kadakia R, Weaver CD, Gogliotti R, Hopkins C, Lindsley CW, Denton JS.

Front Pharmacol. 2011 Nov 30;2:75. doi: 10.3389/fphar.2011.00075. eCollection 2011.


Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.

Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

J Med Chem. 2011 Nov 10;54(21):7639-47. doi: 10.1021/jm200956q. Epub 2011 Oct 19.


Characterization of a commonly used mouse model of SMA reveals increased seizure susceptibility and heightened fear response in FVB/N mice.

Gogliotti RG, Lutz C, Jorgensen M, Huebsch K, Koh S, Didonato CJ.

Neurobiol Dis. 2011 Jul;43(1):142-51. doi: 10.1016/j.nbd.2011.03.002. Epub 2011 Mar 21.


Mouse survival motor neuron alleles that mimic SMN2 splicing and are inducible rescue embryonic lethality early in development but not late.

Hammond SM, Gogliotti RG, Rao V, Beauvais A, Kothary R, DiDonato CJ.

PLoS One. 2010 Dec 29;5(12):e15887. doi: 10.1371/journal.pone.0015887.


Cpd-1 null mice display a subtle neurological phenotype.

Kular RK, Gogliotti RG, Opal P.

PLoS One. 2010 Sep 9;5(9). pii: e12649. doi: 10.1371/journal.pone.0012649.


Molecular and phenotypic reassessment of an infrequently used mouse model for spinal muscular atrophy.

Gogliotti RG, Hammond SM, Lutz C, Didonato CJ.

Biochem Biophys Res Commun. 2010 Jan 1;391(1):517-22. doi: 10.1016/j.bbrc.2009.11.090. Epub 2009 Dec 4.


Neuronal SMN expression corrects spinal muscular atrophy in severe SMA mice while muscle-specific SMN expression has no phenotypic effect.

Gavrilina TO, McGovern VL, Workman E, Crawford TO, Gogliotti RG, DiDonato CJ, Monani UR, Morris GE, Burghes AH.

Hum Mol Genet. 2008 Apr 15;17(8):1063-75. doi: 10.1093/hmg/ddm379. Epub 2008 Jan 4.


Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.

Protasevich II, Brouillette CG, Snow ME, Dunham S, Rubin JR, Gogliotti R, Siegel K.

Biochemistry. 2004 Oct 26;43(42):13380-9.


Hyplip2, a new gene for combined hyperlipidemia and increased atherosclerosis.

Wang X, Gargalovic P, Wong J, Gu JL, Wu X, Qi H, Wen P, Xi L, Tan B, Gogliotti R, Castellani LW, Chatterjee A, Lusis AJ.

Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1928-34. Epub 2004 Aug 26.


Inhibition of the early phase of HIV replication by an isothiazolone, PD 161374.

Sharmeen L, McQuade T, Heldsinger A, Gogliotti R, Domagala J, Gracheck S.

Antiviral Res. 2001 Feb;49(2):101-14.


2,2'-Dithiobisbenzamides derived from alpha-, beta- and gamma-amino acids possessing anti-HIV activities: synthesis and structure-activity relationship.

Prasad JV, Loo JA, Boyer FE, Stier MA, Gogliotti RD, Turner WJ, Harvey PJ, Kramer MR, Mack DP, Scholten JD, Gracheck SJ, Domagala JM.

Bioorg Med Chem. 1998 Oct;6(10):1707-30.


2,2'-Dithiobisbenzamides and 2-benzisothiazolones, two new classes of antiretroviral agents: SAR and mechanistic considerations.

Domagala JM, Gogliotti R, Sanchez JP, Stier MA, Musa K, Song Y, Loo J, Reily M, Tummino P, Harvey P, Hupe D, Sharmeen L, Mack D, Scholten J, Saunders J, McQuade T.

Drug Des Discov. 1997 May;15(1):49-61.


A new class of anti-HIV-1 agents targeted toward the nucleocapsid protein NCp7: the 2,2'-dithiobisbenzamides.

Domagala JM, Bader JP, Gogliotti RD, Sanchez JP, Stier MA, Song Y, Prasad JV, Tummino PJ, Scholten J, Harvey P, Holler T, Gracheck S, Hupe D, Rice WG, Schultz R.

Bioorg Med Chem. 1997 Mar;5(3):569-79.


The human immunodeficiency virus type 1 (HIV-1) nucleocapsid protein zinc ejection activity of disulfide benzamides and benzisothiazolones: correlation with anti-HIV and virucidal activities.

Tummino PJ, Harvey PJ, McQuade T, Domagala J, Gogliotti R, Sanchez J, Song Y, Hupe D.

Antimicrob Agents Chemother. 1997 Feb;41(2):394-400.


Biophysical characterization of zinc ejection from HIV nucleocapsid protein by anti-HIV 2,2'-dithiobis[benzamides] and benzisothiazolones.

Loo JA, Holler TP, Sanchez J, Gogliotti R, Maloney L, Reily MD.

J Med Chem. 1996 Oct 11;39(21):4313-20.


The in vitro ejection of zinc from human immunodeficiency virus (HIV) type 1 nucleocapsid protein by disulfide benzamides with cellular anti-HIV activity.

Tummino PJ, Scholten JD, Harvey PJ, Holler TP, Maloney L, Gogliotti R, Domagala J, Hupe D.

Proc Natl Acad Sci U S A. 1996 Feb 6;93(3):969-73.


Inhibitors of HIV nucleocapsid protein zinc fingers as candidates for the treatment of AIDS.

Rice WG, Supko JG, Malspeis L, Buckheit RW Jr, Clanton D, Bu M, Graham L, Schaeffer CA, Turpin JA, Domagala J, Gogliotti R, Bader JP, Halliday SM, Coren L, Sowder RC 2nd, Arthur LO, Henderson LE.

Science. 1995 Nov 17;270(5239):1194-7.


The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.

Sanchez JP, Gogliotti RD, Domagala JM, Gracheck SJ, Huband MD, Sesnie JA, Cohen MA, Shapiro MA.

J Med Chem. 1995 Oct 27;38(22):4478-87.


New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.

Sanchez JP, Bridges AJ, Bucsh R, Domagala JM, Gogliotti RD, Hagen SE, Heifetz CL, Joannides ET, Sesnie JC, Shapiro MA, et al.

J Med Chem. 1992 Jan 24;35(2):361-7.


Quinolone antibacterials: preparation and activity of bridged bicyclic analogues of the C7-piperazine.

Kiely JS, Hutt MP, Culbertson TP, Bucsh RA, Worth DF, Lesheski LE, Gogliotti RD, Sesnie JC, Solomon M, Mich TF.

J Med Chem. 1991 Feb;34(2):656-63.


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