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Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors

Journal of lipid research, 2016-01, Vol.57 (1), p.131-141

2016

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Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia

Journal of medicinal chemistry, 2011-07, Vol.54 (14), p.5082-5096

2011

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Protein tyrosine phosphatase: enzymatic assays

Methods (San Diego, Calif.), 2005, Vol.35 (1), p.2-8

2005

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Residues Distant from the Active Site Influence Protein-tyrosine Phosphatase 1B Inhibitor Binding

The Journal of biological chemistry, 2006-02, Vol.281 (8), p.5258-5266

2006

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Broadening the Spectrum of β-Lactam Antibiotics through Inhibition of Signal Peptidase Type I

Antimicrobial Agents and Chemotherapy, 2012-09, Vol.56 (9), p.4662-4670

2012

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The development of potent non-peptidic PTP-1B inhibitors

Bioorganic & medicinal chemistry letters, 2004-02, Vol.14 (4), p.1039-1042

2004

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The YRD Motif Is a Major Determinant of Substrate and Inhibitor Specificity in T-cell Protein-tyrosine Phosphatase

The Journal of biological chemistry, 2001-07, Vol.276 (28), p.26036-26043

2001

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Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2349-2368

2024

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Abstract P054: RP-3500: A novel, potent and selective ATR inhibitor that is effective in pre-clinical models as a monotherapy and in combination with PARP inhibitors

Molecular cancer therapeutics, 2021-12, Vol.20 (12_Supplement), p.P054-P054

2021

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How Does Alendronate Inhibit Protein-tyrosine Phosphatases?

The Journal of biological chemistry, 1997-09, Vol.272 (36), p.22472-22480

1997

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Calcium Is Not Required for 5-Lipoxygenase Activity at High Phosphatidyl Choline Vesicle Concentrations

Biochemistry (Easton), 1998-06, Vol.37 (22), p.8027-8034

1998

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The Structural Basis for the Selectivity of Benzotriazole Inhibitors of PTP1B

Biochemistry (Easton), 2003-10, Vol.42 (39), p.11451-11459

2003

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Characterization of the non-heme iron center of human 5-lipoxygenase by electron paramagnetic resonance, fluorescence, and ultraviolet-visible spectroscopy: Redox cycling between ferrous and ferric states

Biochemistry (Easton), 1993-09, Vol.32 (37), p.9763-9771

1993

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2-Aryl benzimidazoles: Human SCD1-specific stearoyl coenzyme-A desaturase inhibitors

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (22), p.6366-6369

2010

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Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.479-483

2011

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Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3200-3205

2008

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Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods

Journal of biomolecular screening, 2011-10, Vol.16 (9), p.1098-1105

2011

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Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6505-6509

2011

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Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors

Bioorganic & medicinal chemistry letters, 2004-02, Vol.14 (4), p.1043-1048

2004

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Enzyme occupancy measurement of intracellular protein tyrosine phosphatase 1B using photoaffinity probes

Analytical biochemistry, 2006-02, Vol.349 (1), p.49-61

2006

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High-throughput scintillation proximity assay for stearoyl-CoA desaturase-1

Journal of biomolecular screening, 2011-06, Vol.16 (5), p.506-517

2011

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Development of a Robust Scintillation Proximity Assay for Protein Tyrosine Phosphatase 1B Using the Catalytically Inactive (C215S) Mutant

Analytical biochemistry, 2001-04, Vol.291 (2), p.269-278

2001

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Using mass spectrometry to study the photo-affinity labeling of protein tyrosine phosphatase 1B

International journal of mass spectrometry, 2004-11, Vol.238 (2), p.99-106

2004

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Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors

Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia

Protein tyrosine phosphatase: enzymatic assays

Residues Distant from the Active Site Influence Protein-tyrosine Phosphatase 1B Inhibitor Binding

Broadening the Spectrum of β-Lactam Antibiotics through Inhibition of Signal Peptidase Type I

The development of potent non-peptidic PTP-1B inhibitors

RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors

The YRD Motif Is a Major Determinant of Substrate and Inhibitor Specificity in T-cell Protein-tyrosine Phosphatase

Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)

Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics

Abstract P054: RP-3500: A novel, potent and selective ATR inhibitor that is effective in pre-clinical models as a monotherapy and in combination with PARP inhibitors

How Does Alendronate Inhibit Protein-tyrosine Phosphatases?

Calcium Is Not Required for 5-Lipoxygenase Activity at High Phosphatidyl Choline Vesicle Concentrations

The Structural Basis for the Selectivity of Benzotriazole Inhibitors of PTP1B

Characterization of the non-heme iron center of human 5-lipoxygenase by electron paramagnetic resonance, fluorescence, and ultraviolet-visible spectroscopy: Redox cycling between ferrous and ferric states

2-Aryl benzimidazoles: Human SCD1-specific stearoyl coenzyme-A desaturase inhibitors

Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors

Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor

Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods

Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors

Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors

Enzyme occupancy measurement of intracellular protein tyrosine phosphatase 1B using photoaffinity probes

High-throughput scintillation proximity assay for stearoyl-CoA desaturase-1

Development of a Robust Scintillation Proximity Assay for Protein Tyrosine Phosphatase 1B Using the Catalytically Inactive (C215S) Mutant

Using mass spectrometry to study the photo-affinity labeling of protein tyrosine phosphatase 1B

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