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Curt A. Dvorak
Researcher at Janssen Pharmaceutica
Publications - 26
Citations - 429
Curt A. Dvorak is an academic researcher from Janssen Pharmaceutica. The author has contributed to research in topics: Receptor & Agonist. The author has an hindex of 12, co-authored 26 publications receiving 367 citations.
Papers
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Journal ArticleDOI
GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Changlu Liu,Pascal Bonaventure,Grace Lee,Diane Nepomuceno,Chester Kuei,Jiejun Wu,Qingqin Li,Victory Joseph,Steven W. Sutton,William A. Eckert,Xiang Yao,Lynn Yieh,Curt A. Dvorak,Nicholas I. Carruthers,Coate Heather R,Sujin Yun,Christine Dugovic,Anthony Harrington,Timothy W. Lovenberg +18 more
TL;DR: The findings suggest that l-Trp and l-Phe are candidate physiologic ligands for GPR139, and it is hypothesize that this receptor may act as a sensor to detect dynamic changes of l- Trp andl- Phe in the brain.
Journal ArticleDOI
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Christa C. Chrovian,Akinola Soyode-Johnson,Alexander A. Peterson,Christine F. Gelin,Xiaohu Deng,Curt A. Dvorak,Nicholas I. Carruthers,Brian Lord,Ian Fraser,Leah Aluisio,Kevin J. Coe,Brian Scott,Tatiana Koudriakova,Freddy Schoetens,Kia Sepassi,David J. Gallacher,Anindya Bhattacharya,Michael A. Letavic +17 more
TL;DR: Compound 35 was chosen as a clinical candidate for advancement into phase I clinical trials to assess safety and tolerability in healthy human subjects prior to the initiation of proof of concept studies for the treatment of mood disorders.
Journal ArticleDOI
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate
Michael A. Letavic,Brad M. Savall,Allison Brett Douglas,Leah Aluisio,José Ignacio Andrés,Meri De Angelis,Hong Ao,Derek A. Beauchamp,Pascal Bonaventure,Stewart Bryant,Nicholas I. Carruthers,Ceusters Marc Andre,Kevin J. Coe,Curt A. Dvorak,Ian Fraser,Christine F. Gelin,Tatiana Koudriakova,Jimmy T. Liang,Brian Lord,Timothy W. Lovenberg,Monicah A. Otieno,Freddy Schoetens,Devin M. Swanson,Qi Wang,Alan D. Wickenden,Anindya Bhattacharya +25 more
TL;DR: The synthesis and preclinical characterization of novel 4-(R)-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridines that are potent and selective brain penetrant P2X7 antagonists are described.
Journal ArticleDOI
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.
Curt A. Dvorak,Changlu Liu,Jonathan Shelton,Chester Kuei,Steven W. Sutton,Timothy W. Lovenberg,Nicholas I. Carruthers +6 more
TL;DR: An examination of structurally similar arylhydroxy acids led to the identification of 3-chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo effects on lipolysis in a mouse model of obesity.
Patent
Pyrimidine compounds as serotonin receptor modulators
TL;DR: The pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases as discussed by the authors, and they have been shown to be effective in treating depression.