Publications
2023
Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7Molecular Pharmacology. 2023 Jul (104(1)). 17-27
- PMID: PMID: 37105671[PubMed].
There is no publication with 2022 tag
2021
HofmannCS, CarringtonSJ, KellerAN, GregoryKJ, NiswenderCM, Regulation and Functional Consequences of mGlu RNA EditingRNA (New York, N.Y.). 2021 Jul 8
- PMID: 34244459[PubMed].
JoffeME, SantiagoCI, VermudezSAD, FisherNM, DograS, NiswenderCM, Jeffrey ConnP, Frontal cortex genetic ablation of metabotropic glutamate receptor subtype 3 (mGlu) impairs postsynaptic plasticity and modulates affective behaviorsNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2021 May 25
- PMID: 34035469[PubMed].
VermudezSAD, GogliottiRG, ArthurB, BuchA, MoralesC, MoxleyY, RajpalH, ConnPJ, NiswenderCM, Profiling beneficial and potential adverse effects of MeCP2 overexpression in a hypomorphic Rett syndrome mouse modelGenes, brain, and behavior. 2021 May 18 e12752
- PMID: 34002468[PubMed].
XiangZ, LvX, LinX, O'BrienDE, AltmanMK, LindsleyCW, JavitchJA, NiswenderCM, ConnPJ, Input-specific regulation of glutamatergic synaptic transmission in the medial prefrontal cortex by mGlu/mGlu receptor heterodimersScience signaling. 2021 Apr 6 14 (677).
- PMID: 33824180[PubMed].
DograS, StansleyBJ, XiangZ, QianW, GogliottiRG, NicolettiF, LindsleyCW, NiswenderCM, JoffeME, ConnPJ, Activating mGlu Metabotropic Glutamate Receptors Rescues Schizophrenia-like Cognitive Deficits Through Metaplastic Adaptations Within the HippocampusBiological psychiatry. 2021 Mar 6
- PMID: 33965197[PubMed].
KentCN, FultonMG, StillwellKJ, DickersonJW, LochMT, RodriguezAL, BlobaumAL, BoutaudO, RookJL, NiswenderCM, Jeffrey ConnP, LindsleyCW, Discovery and optimization of a novel CNS penetrant series of mGlu PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian modelBioorganic & medicinal chemistry letters. 2021 Feb 5 127838
- PMID: 33556572[PubMed].
FisherNM, AlHashimA, BuchAB, BadivukuH, SammanMM, WeissKM, CesteroGI, DoesMD, RookJM, LindsleyCW, ConnPJ, GogliottiRG, NiswenderCM, A GRM7 mutation associated with developmental delay reduces mGlu7 expression and produces neurological phenotypesJCI insight. 2021 Jan 21
- PMID: 33476302[PubMed].
2020
DavisDC, BungardJD, ChangS, RodriguezAL, BlobaumAL, BoutaudO, MelanconBJ, NiswenderCM, Jeffrey ConnP, LindsleyCW, Lead optimization of the VU0486321 series of mGlu PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMsBioorganic & medicinal chemistry letters. 2020 Nov 27 32 127724
- PMID: 33253881[PubMed].
KalbfleischJJ, ReedCW, ParkC, SpearingPK, QuitaligMC, JenkinsMT, RodriguezAL, BlobaumAL, ConnPJ, NiswenderCM, LindsleyCW, Synthesis and SAR of a series of mGlu NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate coreBioorganic & medicinal chemistry letters. 2020 Sep 2 30 (22). 127529
- PMID: 32890686[PubMed].
ReedCW, KalbfleischJJ, WongMJ, WashecheckJP, HunterA, RodriguezAL, BlobaumAL, ConnPJ, NiswenderCM, LindsleyCW, Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu Positive Allosteric Modulator Tool CompoundACS medicinal chemistry letters. 2020 Aug 20 11 (9). 1773-1779
- PMID: 32944146[PubMed].
FultonMG, LochMT, RodriguezAL, LinX, JavitchJA, ConnPJ, NiswenderCM, LindsleyCW, Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu heterodimeric receptor results in a compound with mGlu homodimer selectivityBioorganic & medicinal chemistry letters. 2020 Apr 25 30 (13). 127212
- PMID: 32371100[PubMed].
FisherNM, GouldRW, GogliottiRG, McDonaldAJ, BadivukuH, ChennareddyS, BuchAB, MooreAM, JenkinsMT, RobbWH, LindsleyCW, JonesCK, ConnPJ, NiswenderCM, Phenotypic profiling of mGlu knockout mice reveals new implications for neurodevelopmental disordersGenes, brain, and behavior. 2020 Apr 14 19 (7). e12654
- PMID: 32248644[PubMed].
2019
FultonMG, LochMT, CuocoCA, RodriguezAL, DaysE, VinsonPN, KozekKA, WeaverCD, BlobaumAL, ConnPJ, NiswenderCM, LindsleyCW, Challenges in the Discovery and Optimization of mGlu Heterodimer Positive Allosteric ModulatorsLetters in drug design & discovery. 2019 Dec 16 16 (12). 1387-1394
- PMID: 32201485[PubMed].
MoranSP, XiangZ, DoyleCA, MaksymetzJ, LvX, FaltinS, FisherNM, NiswenderCM, RookJM, LindsleyCW, ConnPJ, Biased M receptor-positive allosteric modulators reveal role of phospholipase D in M-dependent rodent cortical plasticityScience signaling. 2019 Dec 3 12 (610).
- PMID: 31796631[PubMed].
GregoryKJ, BridgesTM, GogliottiRG, StaufferSR, NoetzelMJ, JonesCK, LindsleyCW, ConnPJ, NiswenderCM, In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug DiscoveryACS pharmacology & translational science. 2019 Nov 15 2 (6). 442-452
- PMID: 32259076[PubMed].
TempleKJ, EngersJL, LongMF, WatsonKJ, ChangS, LuscombeVB, JenkinsMT, RodriguezAL, NiswenderCM, BridgesTM, ConnPJ, EngersDW, LindsleyCW, Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotypeBioorganic & medicinal chemistry letters. 2019 Nov 13 30 (3). 126812
- PMID: 31784320[PubMed].
TempleKJ, LongMF, EngersJL, WatsonKJ, ChangS, LuscombeVB, RodriguezAL, NiswenderCM, BridgesTM, ConnPJ, EngersDW, LindsleyCW, Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypesBioorganic & medicinal chemistry letters. 2019 Nov 11 30 (4). 126811
- PMID: 31787491[PubMed].
PresleyCC, PerryCK, ChildressES, MulderMJ, LuscombeVB, RodriguezAL, NiswenderCM, ConnPJ, LindsleyCW, Evaluation of Synthetic Cytochrome P-Mimetic Metalloporphyrins To Facilitate “Biomimetic” Biotransformation of a Series of mGlu Allosteric LigandsACS omega. 2019 Jul 26 4 (7). 12782-12789
- PMID: 31460402[PubMed].
ChopkoTC, HanC, GregroAR, EngersDW, FeltsAS, PoslusneyMS, BollingerKA, MorrisonRD, BubserM, LamsalA, LuscombeVB, ChoHP, Schnetz-BoutaudNC, RodriguezAL, ChangS, DanielsJS, StecDF, NiswenderCM, JonesCK, WoodMR, WoodMW, DugganME, BrandonNJ, ConnPJ, BridgesTM, LindsleyCW, MelanconBJ, SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M PAMsBioorganic & medicinal chemistry letters. 2019 Jun 20 29 (16). 2224-2228
- PMID: 31248774[PubMed].
XiangZ, LvX, MaksymetzJ, StansleyBJ, GhoshalA, GogliottiRG, NiswenderCM, LindsleyCW, ConnPJ, mGlu Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu-Endocannabinoid SignalingACS pharmacology & translational science. 2019 May 15 2 (3). 198-209
- PMID: 31259318[PubMed].
GogliottiRG, NiswenderCM, A Coordinated Attack: Rett Syndrome Therapeutic DevelopmentTrends in pharmacological sciences. 2019 Apr 1 40 (4). 233-236
- PMID: 30905360[PubMed].
ReedCW, YohnSE, WashecheckJP, RoenfanzHF, QuitaligMC, LuscombeVB, JenkinsMT, RodriguezAL, EngersDW, BlobaumAL, ConnPJ, NiswenderCM, LindsleyCW, Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)Journal of medicinal chemistry. 2019 Jan 17 62 (3). 1690-1695
- PMID: 30608678[PubMed].
2018
PoslusneyMS, SalovichJM, WoodMR, MelanconBJ, BollingerKA, LuscombeVB, RodriguezAL, EngersDW, BridgesTM, NiswenderCM, ConnPJ, LindsleyCW, Novel M positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligandsBioorganic & medicinal chemistry letters. 2018 Dec 18 29 (3). 362-366
- PMID: 30580918[PubMed].
FisherNM, SetoM, LindsleyCW, NiswenderCM, Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental DisordersFrontiers in molecular neuroscience. 2018 Dec 14 11 444
- PMID: 30588231[PubMed].
FeltsAS, BollingerKA, BrassardCJ, RodriguezAL, MorrisonRD, Scott DanielsJ, BlobaumAL, NiswenderCM, JonesCK, ConnPJ, EmmitteKA, LindsleyCW, Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5Bioorganic & medicinal chemistry letters. 2018 Nov 10 29 (1). 47-50
- PMID: 30446311[PubMed].
FisherNM, SetoM, LindsleyCW, NiswenderCM, Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental DisordersFrontiers in molecular neuroscience. 2018 Oct 23 11 387
- PMID: 30405350[PubMed].
MarksCR, ShonesyBC, WangX, StephensonJR, NiswenderCM, ColbranRJ, Activated CaMKII Binds to the mGlu Metabotropic Glutamate Receptor and Modulates Calcium MobilizationMolecular pharmacology. 2018 Oct 3 94 (6). 1352-1362
- PMID: 30282777[PubMed].
EngersJL, ChildressES, LongMF, CapstickRA, LuscombeVB, ChoHP, DickersonJW, RookJM, BlobaumAL, NiswenderCM, EngersDW, ConnPJ, LindsleyCW, VU6007477, a Novel M PAM Based on a Pyrrolo[2,3-]pyridine Carboxamide Core Devoid of Cholinergic Adverse EventsACS medicinal chemistry letters. 2018 Sep 4 9 (9). 917-922
- PMID: 30258541[PubMed].
EngersJL, BenderAM, KalbfleischJJ, ChoHP, LingenfelterKS, LuscombeVB, HanC, MelanconBJ, BlobaumAL, DickersonJW, RookJM, NiswenderCM, EmmitteKA, ConnPJ, LindsleyCW, Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M Positive Allosteric ModulatorsACS chemical neuroscience. 2018 Aug 9 10 (3). 1035-1042
- PMID: 30086237[PubMed].
BertronJL, ChoHP, Garcia-BarrantesPM, PanareseJD, SalovichJM, NanceKD, EngersDW, RookJM, BlobaumAL, NiswenderCM, StaufferSR, ConnPJ, LindsleyCW, The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine coreBioorganic & medicinal chemistry letters. 2018 May 5 28 (12). 2175-2179
- PMID: 29754948[PubMed].
MoranSP, ChoHP, MaksymetzJ, RemkeDH, HansonRM, NiswenderCM, LindsleyCW, RookJM, ConnPJ, PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native SystemsACS chemical neuroscience. 2018 Apr 25 9 (9). 2218-2224
- PMID: 29683646[PubMed].
FeltsAS, RodriguezAL, MorrisonRD, BlobaumAL, ByersFW, DanielsJS, NiswenderCM, ConnPJ, LindsleyCW, EmmitteKA, Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5Bioorganic & medicinal chemistry letters. 2018 Apr 22 28 (10). 1679-1685
- PMID: 29705142[PubMed].
O'BrienDE, ShawDM, ChoHP, CrossAJ, WesolowskiSS, FeltsAS, BergareJ, ElmoreCS, LindsleyCW, NiswenderCM, ConnPJ, Differential Pharmacology and Binding of mGlu Receptor Allosteric ModulatorsMolecular pharmacology. 2018 Mar 15 93 (5). 526-540
- PMID: 29545267[PubMed].
MoranSP, DickersonJW, ChoHP, XiangZ, MaksymetzJ, RemkeDH, LvX, DoyleCA, RajanDH, NiswenderCM, EngersDW, LindsleyCW, RookJM, ConnPJ, M-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognitionNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2018 Mar 14 43 (8). 1763-1771
- PMID: 29581537[PubMed].
2017
StansleyBJ, FisherNM, GogliottiRG, LindsleyCW, ConnPJ, NiswenderCM, Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5Cerebral cortex (New York, N.Y. : 1991). 2017 Nov 9 28 (12). 4291-4304
- PMID: 29136107[PubMed].
ReedCW, McGowanKM, SpearingPK, StansleyBJ, RoenfanzHF, EngersDW, RodriguezAL, EngelbergEM, LuscombeVB, LochMT, RemkeDH, RookJM, BlobaumAL, ConnPJ, NiswenderCM, LindsleyCW, VU6010608, a Novel mGlu NAM from a Series of -(2-(1-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamidesACS medicinal chemistry letters. 2017 Nov 8 8 (12). 1326-1330
- PMID: 29259756[PubMed].
2016
SenterRK, GhoshalA, WalkerAG, XiangZ, NiswenderCM, ConnPJ, The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic StrategiesCurrent neuropharmacology. 2016 Jul 2 14 (5). 455-73
- PMID: 27296640[PubMed].
LindsleyCW, EmmitteKA, HopkinsCR, BridgesTM, GregoryKJ, NiswenderCM, ConnPJ, Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsChemical reviews. 2016 Feb 16 116 (11). 6707-41
- PMID: 26882314[PubMed].
2014
HanC, ChatterjeeA, NoetzelMJ, PanareseJD, SmithE, ChaseP, HodderP, NiswenderC, ConnPJ, LindsleyCW, StaufferSR, Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulatorsBioorganic & medicinal chemistry letters. 2014 Nov 18 25 (2). 384-8
- PMID: 25435150[PubMed].
ConnPJ, LindsleyCW, MeilerJ, NiswenderCM, Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disordersNature reviews. Drug discovery. 2014 Sep 3 13 (9). 692-708
- PMID: 25176435[PubMed].
YinS, NiswenderCM, Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indicationsCellular signalling. 2014 May 2 26 (10). 2284-97
- PMID: 24793301[PubMed].
WuH, WangC, GregoryKJ, HanGW, ChoHP, XiaY, NiswenderCM, KatritchV, MeilerJ, CherezovV, ConnPJ, StevensRC, Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulatorScience (New York, N.Y.). 2014 Mar 6 344 (6179). 58-64
- PMID: 24603153[PubMed].
2013
MankaJT, RodriguezAL, MorrisonRD, VenableDF, ChoHP, BlobaumAL, DanielsJS, NiswenderCM, ConnPJ, LindsleyCW, EmmitteKA, Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1Bioorganic & medicinal chemistry letters. 2013 Jul 23 23 (18). 5091-6
- PMID: 23932792[PubMed].
KleinMT, VinsonPN, NiswenderCM, Approaches for probing allosteric interactions at 7 transmembrane spanning receptorsProgress in molecular biology and translational science. 2013 Jun 15 115 1-59
- PMID: 23415091[PubMed].