K. Emmitte

发表

Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.

Julie L. Engers, Andrew S. Felts, Brittney S. Bates, 2012, Bioorganic & medicinal chemistry letters.

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.

Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant)

Anna L. Blobaum, C. Lindsley, P. Conn, 2017 .

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.

Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1

M. Cheung, J. Salovich, K. Hornberger, 2008 .

Emerging Novel Enzyme Pathways in Drug Metabolism Evaluating the Disposition of a Mixed Aldehyde Oxidase / Cytochrome P 450 Substrate in Rats with Attenuated P 450 Activity s

C. Lindsley, R. Morrison, Frank W. Byers, 2016 .

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

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

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation

D. Sheffler, Z. Xiang, C. Lindsley, 2017, Neuropsychopharmacology.

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Tudor I. Oprea, Jennifer E. Golden, Joshua A. Bittker, 2015, Cell.

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.

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.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Alison R. Gregro, Julie L. Engers, Bruce J. Melancon, 2016, Bioorganic & medicinal chemistry letters.

Asymmetric total synthesis of (-)-isolaurallene.

M. Crimmins, K. Emmitte, 2001, Journal of the American Chemical Society.

Total synthesis of (+)-laurencin: an asymmetric alkylation-ring-closing metathesis approach to medium ring ethers.

M. Crimmins, K. Emmitte, 1999, Organic 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.

Diastereoselective alkylations of oxazolidinone glycolates: a useful extension of the Evans asymmetric alkylation.

K. A. Emmitte, M. Crimmins, J. Katz, 2000, Organic letters.

Enantioselective total synthesis of brevetoxin A: unified strategy for the B, E, G, and J subunits.

K. A. Emmitte, M. Crimmins, J. Ellis, 2009, Chemistry.

In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1

Kyle A. Emmitte, Masaaki Furuta, N. Noro, 2007, Molecular Cancer Therapeutics.

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Bruce J. Melancon, A. Christopoulos, C. Lindsley, 2012, Journal of medicinal chemistry.

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.

Total synthesis of brevetoxin A.

K. Nicolaou, K. A. Emmitte, J. Gunzner, 2009, Organic letters.

A convergent coupling strategy for the formation of polycyclic ethers: stereoselective synthesis of the BCDE fragment of brevetoxin A.

M. Crimmins, P. J. McDougall, K. Emmitte, 2005, Organic letters.

Ring closing metathesis for the formation of medium ring ethers: the total synthesis of (−)-isolaurallene

M. Crimmins, A. Choy, K. Emmitte, 2002 .

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.

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

K. Gregory, C. Lindsley, C. Hopkins, 2016, Chemical reviews.

Evaluating the Disposition of a Mixed Aldehyde Oxidase/Cytochrome P450 Substrate in Rats with Attenuated P450 Activity

C. Lindsley, R. Morrison, Frank W. Byers, 2016, Drug Metabolism and Disposition.

Discovery of thiophene inhibitors of polo-like kinase.

D. Drewry, T. J. Lansing, R. Mook, 2009, Bioorganic & medicinal chemistry letters.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Brian J. Wilson, L. Shewchuk, P. Sabbatini, 2009, Bioorganic & medicinal chemistry letters.

Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors

T. Skorski, S. Cocklin, K. Sullivan, 2016, Nucleic acids research.

Abstracts list 1 - Identity matters: Ggamma-type dictates efficacy of Gbetagamma signaling and cellular decisions

J. Meiler, M. Schubert, A. Beck‐Sickinger, 2018 .

mGlu5 negative allosteric modulators: a patent review (2013 - 2016)

K. Emmitte, 2013, Expert opinion on therapeutic patents.

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.

Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

Cody J. Wenthur, Z. Xiang, C. Lindsley, 2015, Proceedings of the National Academy of Sciences.

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.

Stress and interferon signalling-mediated apoptosis contributes to pleiotropic anticancer responses induced by targeting NGLY1

Hamed S. Hayatshahi, Yu-Chieh Wang, R. Sampat, 2018, British Journal of Cancer.

Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase

P. Sabbatini, Rakesh Kumar, S. Rabindran, 2009, Clinical Cancer Research.

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.

J. Jackson, T. J. Lansing, R. Mook, 2009, Bioorganic & medicinal chemistry letters.

Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).

K. A. Emmitte, K. Emmitte, 2011, ACS chemical neuroscience.

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

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

VU0606170, a Selective Slack Channels Inhibitor, Decreases Calcium Oscillations in Cultured Cortical Neurons.

C. Weaver, Yu Du, J. Denton, 2020, ACS chemical neuroscience.

Structure-activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels.

Yu Du, Valerie S. Acuña, B. Spitznagel, 2022, Bioorganic & medicinal chemistry letters.

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

Brittney S. Bates, K. Gregory, Z. Xiang, 2016, The Journal of Pharmacology and Experimental Therapeutics.

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 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.

AntitumorActivity of GSK 1904529 A , a Small-molecule Inhibitor of the Insulin-like Growth Factor-IReceptorTyrosine Kinase

P. Sabbatini, Rakesh Kumar, S. Rabindran, 2009 .

Recent progress in the discovery and development of negative allosteric modulators of mGluR5.

Craig W Lindsley, C. Lindsley, K. A. Emmitte, 2009, Current opinion in drug discovery & development.

Highly Selective Y4 Receptor Antagonist Binds in an Allosteric Binding Pocket.

J. Meiler, M. Schubert, A. Beck‐Sickinger, 2021, Journal of medicinal chemistry.

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.

Regioselective Synthesis of Benzimidazole Thiophene Inhibitors of Polo‐Like Kinase 1.

M. Cheung, J. Salovich, K. Hornberger, 2009 .

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

Jens Meiler, P Jeffrey Conn, Jeffrey L. Mendenhall, 2014, ACS chemical neuroscience.

mGlu5 negative allosteric modulators: a patent review (2010 – 2012)

K. Emmitte, 2013, Expert opinion on therapeutic patents.

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

Julie L. Engers, Andrew S. Felts, Anna L. Blobaum, 2015, Journal of medicinal chemistry.

Relationship between In Vivo Receptor Occupancy and Efficacy of Metabotropic Glutamate Receptor Subtype 5 Allosteric Modulators with Different In Vitro Binding Profiles

Andrew S. Felts, R. Kessler, C. Lindsley, 2015, Neuropsychopharmacology.

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.

(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.

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Andrew S. Felts, C. Lindsley, Hyekyung P. Cho, 2013, Bioorganic & medicinal chemistry letters.

The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2012, Drug Metabolism and Disposition.

The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of mGlu5

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2012 .

Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway

Julie L. Engers, Andrew S. Felts, Brittney S. Bates, 2013 .

Negative allosteric modulators of group II metabotropic glutamate receptors: A patent review (2015 – present)

K. A. Emmitte, Alshaima’a M. Qunies, K. Emmitte, 2021, Expert opinion on therapeutic patents.

Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator VU0506013.

J. Meiler, A. Beck‐Sickinger, C. Weaver, 2023, Journal of medicinal chemistry.

Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors

T. Skorski, S. Cocklin, K. Sullivan, 2016, Nucleic acids research.

Stress and interferon signalling-mediated apoptosis contributes to pleiotropic anticancer responses induced by targeting NGLY1

Hamed S. Hayatshahi, Yu-Chieh Wang, R. Sampat, 2018, British Journal of Cancer.

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2017, Journal of medicinal chemistry.

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).

Julie L. Engers, Andrew S. Felts, C. Lindsley, 2013, Journal of medicinal chemistry.

Antitumor Activity of GSK1904529A, a Small-molecule Inhibitor of the Insulin-like Growth Factor-I Receptor Tyrosine Kinase

Brian J. Wilson, P. Sabbatini, S. Rabindran, 2009, Clinical Cancer Research.

mGlu5 negative allosteric modulators: a patent review (2013 - 2016)

K. Emmitte, 2013, Expert opinion on therapeutic patents.

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).

Julie L. Engers, Andrew S. Felts, Cody J. Wenthur, 2013, Journal of medicinal chemistry.