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Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

Journal of medicinal chemistry, 2012-02, Vol.55 (4), p.1445-1464

2012

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

Proceedings of the National Academy of Sciences - PNAS, 2015-01, Vol.112 (4), p.1196-1201

2015

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Structure–Activity Relationship Studies in a Series of Xanthine Inhibitors of SLACK Potassium Channels

Molecules (Basel, Switzerland), 2024-06, Vol.29 (11), p.2437

2024

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Quercetin and Related Analogs as Therapeutics to Promote Tissue Repair

Bioengineering (Basel), 2023-09, Vol.10 (10), p.1127

2023

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Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies

Pharmaceutical patent analyst, 2022-03, Vol.11 (2), p.45-56

2022

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

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.9027-9040

2015

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

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.925-930

2017

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Enantioselective Total Synthesis of Brevetoxin A: Unified Strategy for the B, E, G, and J Subunits

Chemistry : a European journal, 2009-09, Vol.15 (36), p.9223-9234

2009

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

Molecular cancer therapeutics, 2007-02, Vol.6 (2), p.450-459

2007

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

Expert opinion on therapeutic patents, 2013-04, Vol.23 (4), p.393-408

Emmitte, Kyle A

2013

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

Chemical reviews, 2016-06, Vol.116 (11), p.6707-6741

2016

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

Clinical cancer research, 2009-05, Vol.15 (9), p.3058-3067

2009

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

Expert opinion on therapeutic patents, 2017-06, Vol.27 (6), p.691-706

Emmitte, Kyle A.

2017

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The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5

Drug metabolism and disposition, 2012-09, Vol.40 (9), p.1834

2012

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Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685

Bioorganic & medicinal chemistry, 2023-11, Vol.95, p.117487-117487, Article 117487

2023

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

Expert opinion on therapeutic patents, 2021-08, Vol.31 (8), p.687-708

2021

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

ACS chemical neuroscience, 2011-08, Vol.2 (8), p.411-432

Emmitte, Kyle A

2011

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

Nucleic acids research, 2016-05, Vol.44 (9), p.4189

2016

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mGlu 5 negative allosteric modulators: a patent review (2013 - 2016)

Expert opinion on therapeutic patents, 2017-06, Vol.27 (6), p.691-706

Emmitte, Kyle A

2017

Volltextzugriff (PDF)

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

Bioorganic & medicinal chemistry letters, 2022-11, Vol.76, p.129013-129013, Article 129013

2022

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A Convergent Coupling Strategy for the Formation of Polycyclic Ethers: Stereoselective Synthesis of the BCDE Fragment of Brevetoxin A

Organic letters, 2005-09, Vol.7 (18), p.4033-4036

2005

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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Cell, 2015-06, Vol.161 (6), p.1252-1265

2015

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Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y 4 Receptor Positive Allosteric Modulator VU0506013

Journal of medicinal chemistry, 2023-07, Vol.66 (13), p.8745-8766

2023

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Total Synthesis of (+)-Laurencin: An Asymmetric Alkylation−Ring-Closing Metathesis Approach to Medium Ring Ethers

Organic letters, 1999-12, Vol.1 (12), p.2029-2032

1999

Volltextzugriff (PDF)

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

Journal of medicinal chemistry, 2023-07, Vol.66 (13), p.8745-8766

2023

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Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

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

Structure–Activity Relationship Studies in a Series of Xanthine Inhibitors of SLACK Potassium Channels

Quercetin and Related Analogs as Therapeutics to Promote Tissue Repair

Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies

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

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

Enantioselective Total Synthesis of Brevetoxin A: Unified Strategy for the B, E, G, and J Subunits

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

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

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

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

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

The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5

Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685

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

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

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

mGlu 5 negative allosteric modulators: a patent review (2013 - 2016)

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

A Convergent Coupling Strategy for the Formation of Polycyclic Ethers: Stereoselective Synthesis of the BCDE Fragment of Brevetoxin A

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y 4 Receptor Positive Allosteric Modulator VU0506013

Total Synthesis of (+)-Laurencin: An Asymmetric Alkylation−Ring-Closing Metathesis Approach to Medium Ring Ethers

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

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