Alice L. Rodriguez

发表

Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators

Anna L. Blobaum, C. Lindsley, C. Niswender, 2019, Letters in drug design & discovery.

Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity.

J. Javitch, C. Lindsley, P. Conn, 2020, Bioorganic & medicinal chemistry letters.

Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4

Kari A. Johnson, Z. Xiang, C. Lindsley, 2008, Molecular Pharmacology.

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.

Anna L. Blobaum, J. Javitch, C. Lindsley, 2016, ACS chemical neuroscience.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, N. Brandon, 2017, ACS medicinal chemistry letters.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

N. Brandon, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Discovery of 2‐(2‐Benzoxazoyl amino)‐4‐Aryl‐5‐Cyanopyrimidine as Negative Allosteric Modulators (NAMs) of Metabotropic Glutamate Receptor 5 (mGlu5): From an Artificial Neural Network Virtual Screen to an In Vivo Tool Compound

Jens Meiler, Andrew S. Felts, Brittney S. Bates, 2012, ChemMedChem.

N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2016, Bioorganic & medicinal chemistry letters.

Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor α coactivator binding

J. Katzenellenbogen, Alice L. Rodriguez, A. Tamrazi, 2004 .

Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

Andrew S. Felts, Brian A. Chauder, K. Gregory, 2012, Molecular Pharmacology.

Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.

A. Newman, P. Conn, M. Zou, 2011, Bioorganic & medicinal chemistry letters.

Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

A. Newman, P. Conn, M. Zou, 2010, Bioorganic & medicinal chemistry.

Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes

P. Conn, Alice L. Rodriguez, Yongqin Zhang, 2005, Journal of Pharmacology and Experimental Therapeutics.

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

Anna L. Blobaum, C. Lindsley, C. Hopkins, 2016, Bioorganic & medicinal chemistry letters.

A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators

P. Jeffrey Conn, David Alagille, P. Conn, 2005, Molecular Pharmacology.

A close structural analog of MPEP acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators

P. Conn, Y. Nong, G. Tamagnan, 2005 .

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

Brittney S. Bates, S. Jadhav, C. Lindsley, 2011, ACS chemical neuroscience.

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.

Andrew S. Felts, S. Jadhav, C. Lindsley, 2010, Bioorganic & medicinal chemistry letters.

Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.

C. Lindsley, P. Conn, Alice L. Rodriguez, 2009, Journal of medicinal chemistry.

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

C. Lindsley, P. Conn, C. Weaver, 2009, Bioorganic & medicinal chemistry letters.

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

C. Lindsley, P. Conn, Stacey Lindsley, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.

C. Lindsley, P. Conn, Alice L. Rodriguez, 2008, Bioorganic & medicinal chemistry letters.

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, ACS chemical neuroscience.

Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.

R. Baldwin, P. Conn, G. Tamagnan, 2011, Bioorganic & medicinal chemistry letters.

3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators.

Edward W. Lowe, J. Meiler, P. Conn, 2010, Bioorganic & medicinal chemistry letters.

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.

Julie L. Engers, C. Lindsley, P. Conn, 2021, ACS medicinal chemistry letters.

Coactivator proteins as determinants of estrogen receptor structure and function: spectroscopic evidence for a novel coactivator-stabilized receptor conformation.

J. Katzenellenbogen, K. Carlson, Alice L. Rodriguez, 2005, Molecular endocrinology.

Allosteric control of ligand selectivity between estrogen receptors alpha and beta: implications for other nuclear receptors.

B. Katzenellenbogen, J. Katzenellenbogen, K. Nettles, 2004, Molecular cell.

Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu3 NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy.

Anna L. Blobaum, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2017, ACS medicinal chemistry letters.

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2013, Bioorganic & medicinal chemistry letters.

Technologies for Screening of mGlu Receptor Allosteric Modulators

C. Niswender, Alice L. Rodriguez, Alice L. Rodriguez, 2021 .

Discovery of “Molecular Switches” within a Series of mGlu5 Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype

O. Boutaud, C. Lindsley, P. Conn, 2021, ACS bio & med chem Au.

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2019, Bioorganic & medicinal chemistry letters.

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2018, Bioorganic & medicinal chemistry letters.

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

Andrew S. Felts, C. Lindsley, P. Conn, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of a novel series of furans: Ligands selective for estrogen receptor α

B. Katzenellenbogen, J. Katzenellenbogen, K. Carlson, 2001 .

Functional impact of allosteric agonist activity of selective positive allosteric modulators of mGlu 5 in regulating CNS function

H. Lavreysen, Z. Xiang, C. Lindsley, 2011 .

Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, D. Sheffler, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a potent M5 antagonist with improved clearance profile. Part 1: piperidine amide-based antagonists.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2022, Bioorganic & medicinal chemistry letters.

Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity

C. Lindsley, H. Brown, Joy E. Marlo, 2009, Molecular Pharmacology.

Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago‐potentiator ADX‐47273

C. Lindsley, P. Conn, D. Engers, 2009, ChemMedChem.

Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

Andrew S. Felts, C. Lindsley, P. Conn, 2016, Neuropsychopharmacology.

Erratum to “Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series” [Bioorg. Med. Chem. Lett. 21 (2011) 3243–3247]

R. Baldwin, P. Conn, G. Tamagnan, 2012 .

Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro.

Anna L. Blobaum, C. Lindsley, C. Niswender, 2022, Bioorganic & medicinal chemistry letters.

Extended Probe Characterization: Development of an M4 PAM with Improved Activity and Brain Exposure, while Avoiding Species Bias

Julie L. Engers, Bruce J. Melancon, D. Sheffler, 2013 .

Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.

Anna L. Blobaum, C. Lindsley, P. Conn, 2020, Bioorganic & medicinal chemistry letters.

Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7 Positive Allosteric Modulator Tool Compound.

Anna L. Blobaum, C. Lindsley, P. Conn, 2020, ACS medicinal chemistry letters.

Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278.

Anna L. Blobaum, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 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).

Anna L. Blobaum, C. Lindsley, P. Conn, 2019, Journal of medicinal chemistry.

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2018, Journal of medicinal chemistry.

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.

Alison R. Gregro, Julie L. Engers, Anna L. Blobaum, 2018, Bioorganic & medicinal chemistry letters.

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

Anna L. Blobaum, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

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

Anna L. Blobaum, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core.

Julie L. Engers, Andrew S. Felts, Anna L. Blobaum, 2017, ACS medicinal chemistry letters.

VU6010608, a Novel mGlu 7 NAM from a Series of N ‑ (2-(1 H ‑ 1,2,4-Triazol-1-yl)-5-(tri ﬂ uoromethoxy)phenyl)benzamides

Anna L. Blobaum, C. Lindsley, C. Niswender, 2017 .

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

N. Brandon, C. Lindsley, P. Conn, 2016, Bioorganic & medicinal chemistry letters.

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Andrew S. Felts, Anna L. Blobaum, N. Schnetz-Boutaud, 2022, Journal of medicinal chemistry.

Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.

Bruce J. Melancon, Z. Xiang, C. Lindsley, 2021, Bioorganic & medicinal chemistry letters.

Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.

G. Macdonald, H. Lavreysen, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening

Jens Meiler, C. David Weaver, P. Jeffrey Conn, 2010, ACS chemical neuroscience.

Diaryl-dialkyl-substituted pyrazoles: regioselective synthesis and binding affinity for the estrogen receptor.

J. Katzenellenbogen, Alice L. Rodriguez, G. Nishiguchi, 2002, Bioorganic & medicinal chemistry letters.

Aryl cyclopentadienyl tricarbonyl rhenium complexes: novel ligands for the estrogen receptor with potential use as estrogen radiopharmaceuticals.

J. Katzenellenbogen, Alice L. Rodriguez, E. Mull, 2002, Bioorganic & medicinal chemistry.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

Alison R. Gregro, Andrew S. Felts, Anna L. Blobaum, 2019, Bioorganic & medicinal chemistry letters.

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4).

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2018, Journal of medicinal chemistry.

Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

P Jeffrey Conn, Craig W Lindsley, Colleen M Niswender, 2010, Molecular Pharmacology.

Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate “Biomimetic” Biotransformation of a Series of mGlu5 Allosteric Ligands

C. Lindsley, P. Conn, C. Niswender, 2019, ACS omega.

Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

H. Lavreysen, Z. Xiang, C. Lindsley, 2012, Molecular Pharmacology.

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2013, Bioorganic & medicinal chemistry letters.

Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding

J. Meiler, C. Lindsley, Mariusz Butkiewicz, 2019, ACS Chemical Neuroscience.

Allosteric Control of Ligand Selectivity between Estrogen Receptors α and β - Implications for Other Nuclear Receptors

John A. Katzenellenbogen, B. Katzenellenbogen, J. Katzenellenbogen, 2004 .

Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Julie L. Engers, Andrew S. Felts, Anna L. Blobaum, 2018, ACS medicinal chemistry letters.

Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2021, ACS pharmacology & translational science.

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2015, Journal of medicinal chemistry.

Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.

Andrew S. Felts, C. Lindsley, P. Conn, 2013, ACS chemical neuroscience.

Persistent challenges in the development of an mGlu7 PAM in vivo tool compound: The discovery of VU6046980.

Anna L. Blobaum, O. Boutaud, C. Lindsley, 2022, Bioorganic & medicinal chemistry letters.

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

Kari A. Johnson, J. Wess, Z. Xiang, 2008, Nature chemical biology.