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In vitro and in vivo pharmacological characterization of dasotraline, a dual dopamine and norepinephrine transporter inhibitor in vivo

Biomedicine & pharmacotherapy, 2022-09, Vol.153, p.113359-113359, Article 113359

2022

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Functional deficit in hippocampal activity during fear extinction recall in the single prolonged-stress model of PTSD in male rats

Behavioural brain research, 2021-01, Vol.396, p.112902-112902, Article 112902

2021

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Novel human D-amino acid oxidase inhibitors stabilize an active-site lid-open conformation

Bioscience reports, 2014-08, Vol.34 (4), p.e00133

2014

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Structural, Kinetic, and Pharmacodynamic Mechanisms of d‑Amino Acid Oxidase Inhibition by Small Molecules

Journal of medicinal chemistry, 2013-05, Vol.56 (9), p.3710-3724

2013

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Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors

Bioorganic & medicinal chemistry, 2011-01, Vol.19 (1), p.663-676

2011

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Structures of Leishmania major Pteridine Reductase Complexes Reveal the Active Site Features Important for Ligand Binding and to Guide Inhibitor Design

Journal of molecular biology, 2005-09, Vol.352 (1), p.105-116

2005

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Synthesis and Pharmacological Characterization of Bicyclic Triple Reuptake Inhibitor 3-Aryl Octahydrocyclopenta[c]pyrrole Analogues

Journal of medicinal chemistry, 2011-08, Vol.54 (15), p.5283-5295

2011

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Exploratory Biomarker Study of the Triple Reuptake Inhibitor SEP‐432 Compared to the Dual Reuptake Inhibitor Duloxetine in Healthy Normal Subjects

CNS neuroscience & therapeutics, 2016-05, Vol.22 (5), p.404-412

2016

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Development of α-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease

Bioorganic & medicinal chemistry, 2005-03, Vol.13 (6), p.2141-2156

2005

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Pteridine reductase mechanism correlates pterin metabolism with drug resistance in trypanosomatid parasites

Nature structural & molecular biology, 2001-06, Vol.8 (6), p.521-525

2001

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The multiple orthogonal tools approach to define molecular causation in the validation of druggable targets

Drug Discovery Today, 2004-02, Vol.9 (3), p.117-126

2004

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Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1438-1441

2011

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Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.520-523

2011

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Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1434-1437

2011

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The Roles of Pteridine Reductase 1 and Dihydrofolate Reductase-Thymidylate Synthase in Pteridine Metabolism in the Protozoan Parasite Leishmania major

The Journal of biological chemistry, 1997-05, Vol.272 (21), p.13883-13891

1997

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PTR1: A Reductase Mediating Salvage of Oxidized Pteridines and Methotrexate Resistance in the Protozoan Parasite Leishmania major

Proceedings of the National Academy of Sciences - PNAS, 1994-11, Vol.91 (24), p.11442-11446

1994

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Resecting the neck of the medicine bottle

Drug discovery today, 2002-03, Vol.7 (6), p.349-350

Hardy, Larry W

2002

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Parameters Affecting the Restoration of Activity to Inactive Mutants of Thymidylate Synthase via Subunit Exchange: Further Evidence That Thymidylate Synthase Is a Half-of-the-Sites Activity Enzyme

Biochemistry (Easton), 2001-05, Vol.40 (17), p.5275-5282

2001

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Crystal Structures of Rat Thymidylate Synthase Inhibited by Tomudex, a Potent Anticancer Drug

Biochemistry (Easton), 1999-01, Vol.38 (3), p.1087-1094

1999

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Affinity Ligand Selection from a Library of Small Molecules: Assay Development, Screening, and Application

Biotechnology progress, 2005, Vol.21 (1), p.300-308

2005

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Structure, multiple site binding, and segmental accommodation in thymidylate synthase on binding dUMP and an anti-folate

Biochemistry (Easton), 1990-07, Vol.29 (30), p.6964-6977

1990

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Atomic Structure of Thymidylate Synthase: Target for Rational Drug Design

Science (American Association for the Advancement of Science), 1987-01, Vol.235 (4787), p.448-455

1987

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Asn(177) in Escherichia coli thymidylate synthase is a major determinant of pyrimidine specificity

Proceedings of the National Academy of Sciences - PNAS, 1992-10, Vol.89 (20), p.9725

1992

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Leishmania major Pteridine Reductase 1 Belongs to the Short Chain Dehydrogenase Family: Stereochemical and Kinetic Evidence

Biochemistry (Easton), 1998-03, Vol.37 (12), p.4093-4104

1998

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Design, Synthesis, and Structure−Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5

Journal of medicinal chemistry, 2010-10, Vol.53 (19), p.7107-7118

2010

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In vitro and in vivo pharmacological characterization of dasotraline, a dual dopamine and norepinephrine transporter inhibitor in vivo

Functional deficit in hippocampal activity during fear extinction recall in the single prolonged-stress model of PTSD in male rats

Novel human D-amino acid oxidase inhibitors stabilize an active-site lid-open conformation

Structural, Kinetic, and Pharmacodynamic Mechanisms of d‑Amino Acid Oxidase Inhibition by Small Molecules

Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors

Structures of Leishmania major Pteridine Reductase Complexes Reveal the Active Site Features Important for Ligand Binding and to Guide Inhibitor Design

Synthesis and Pharmacological Characterization of Bicyclic Triple Reuptake Inhibitor 3-Aryl Octahydrocyclopenta[c]pyrrole Analogues

Exploratory Biomarker Study of the Triple Reuptake Inhibitor SEP‐432 Compared to the Dual Reuptake Inhibitor Duloxetine in Healthy Normal Subjects

Development of α-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease

Pteridine reductase mechanism correlates pterin metabolism with drug resistance in trypanosomatid parasites

The multiple orthogonal tools approach to define molecular causation in the validation of druggable targets

Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor

Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor

Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor

The Roles of Pteridine Reductase 1 and Dihydrofolate Reductase-Thymidylate Synthase in Pteridine Metabolism in the Protozoan Parasite Leishmania major

PTR1: A Reductase Mediating Salvage of Oxidized Pteridines and Methotrexate Resistance in the Protozoan Parasite Leishmania major

Resecting the neck of the medicine bottle

Parameters Affecting the Restoration of Activity to Inactive Mutants of Thymidylate Synthase via Subunit Exchange: Further Evidence That Thymidylate Synthase Is a Half-of-the-Sites Activity Enzyme

Crystal Structures of Rat Thymidylate Synthase Inhibited by Tomudex, a Potent Anticancer Drug

Affinity Ligand Selection from a Library of Small Molecules: Assay Development, Screening, and Application

Structure, multiple site binding, and segmental accommodation in thymidylate synthase on binding dUMP and an anti-folate

Atomic Structure of Thymidylate Synthase: Target for Rational Drug Design

Asn(177) in Escherichia coli thymidylate synthase is a major determinant of pyrimidine specificity

Leishmania major Pteridine Reductase 1 Belongs to the Short Chain Dehydrogenase Family: Stereochemical and Kinetic Evidence

Design, Synthesis, and Structure−Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5

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