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Polyoxometalate HIV-1 Protease Inhibitors. A New Mode of Protease Inhibition

Journal of the American Chemical Society, 2001-02, Vol.123 (5), p.886-897

2001

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Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase)

Journal of the American Chemical Society, 2000-04, Vol.122 (14), p.3522-3523

2000

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Structure-Based Design: Potent Inhibitors of Human Brain Memapsin 2 (β-Secretase)

Journal of medicinal chemistry, 2001-08, Vol.44 (18), p.2865-2868

2001

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Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays

Analytical biochemistry, 2011-07, Vol.414 (2), p.179-186

2011

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Protein tyrosine phosphatase 1B inhibitors for diabetes

Nature reviews. Drug discovery, 2002-09, Vol.1 (9), p.696-709

2002

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Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( S )-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H -1,2,4-triazol-3-one, by Fragment-Based Drug Design”

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.16318-16318

2021

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Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design”

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.16318-16318

2021

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Design and Discovery of a Potent and Selective Inhibitor of Integrin αvβ1

Journal of medicinal chemistry, 2024-06, Vol.67 (12), p.10306-10320

2024

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Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp3 character and an exquisite selectivity profile

Bioorganic & medicinal chemistry letters, 2020-09, Vol.30 (17), p.127405-127405, Article 127405

2020

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Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 Inhibitors

The Journal of pharmacology and experimental therapeutics, 2019-11, Vol.371 (2), p.299

2019

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Residence time and kinetic efficiency analysis of extracellular signal-regulated kinase 2 inhibitors

Analytical biochemistry, 2015-03, Vol.473, p.46-52

2015

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Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure

ACS medicinal chemistry letters, 2017-03, Vol.8 (3), p.316-320

2017

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Biochemical and Cellular Profile of NIK Inhibitors with Long Residence Times

SLAS discovery, 2021-06, Vol.26 (5), p.676-683

2021

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Abstract ND12: TNG260: A novel, orally active, CoREST-selective deacetylase inhibitor for the treatment of STK11-mutant cancers

Cancer research (Chicago, Ill.), 2023-05, Vol.83 (7_Supplement), p.ND12-ND12

2023

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Time-dependent inhibition of PHD2

Bioscience reports, 2017-06, Vol.37 (3)

2017

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Characterization of the CHK1 Allosteric Inhibitor Binding Site

Biochemistry (Easton), 2009-10, Vol.48 (41), p.9823-9830

2009

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Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp 3 character and an exquisite selectivity profile

Bioorganic & medicinal chemistry letters, 2020-09, Vol.30 (17), p.127405

2020

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444 TNG260, a CoREST-selective deacetylase inhibitor, reverses anti-PD1 resistance driven by loss of STK11

Journal for immunotherapy of cancer, 2022, Vol.10 (Suppl 2), p.A464-A464

2022

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Proteolytic Activation of Recombinant Pro-memapsin 2 (Pro-β-secretase) Studied with New Fluorogenic Substrates

Biochemistry (Easton), 2000-10, Vol.39 (40), p.12450-12456

2000

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The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors

Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (9), p.2897-2902

2010

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Abstract 3578: A novel and selective 3-phosphoinositide-dependent kinase-1 inhibitor, PF-5177624, blocks insulin-like growth factor-1 induced tumorigenesis in breast cancer cells

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (8_Supplement), p.3578-3578

2011

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Discovery of Novel, Potent, and Selective Inhibitors of 3-Phosphoinositide-Dependent Kinase (PDK1)

Journal of medicinal chemistry, 2011-12, Vol.54 (24), p.8490-8500

2011

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Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery

Journal of computer-aided molecular design, 2011-07, Vol.25 (7), p.689-698

2011

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Correction to “Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure”

ACS medicinal chemistry letters, 2017-12, Vol.8 (12), p.1341-1341

2017

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N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275

Bioorganic & medicinal chemistry letters, 2009-07, Vol.19 (13), p.3493-3497

2009

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Polyoxometalate HIV-1 Protease Inhibitors. A New Mode of Protease Inhibition

Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase)

Structure-Based Design: Potent Inhibitors of Human Brain Memapsin 2 (β-Secretase)

Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays

Protein tyrosine phosphatase 1B inhibitors for diabetes

Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( S )-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H -1,2,4-triazol-3-one, by Fragment-Based Drug Design”

Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design”

Design and Discovery of a Potent and Selective Inhibitor of Integrin αvβ1

Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp3 character and an exquisite selectivity profile

Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 Inhibitors

Residence time and kinetic efficiency analysis of extracellular signal-regulated kinase 2 inhibitors

Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure

Biochemical and Cellular Profile of NIK Inhibitors with Long Residence Times

Abstract ND12: TNG260: A novel, orally active, CoREST-selective deacetylase inhibitor for the treatment of STK11-mutant cancers

Time-dependent inhibition of PHD2

Characterization of the CHK1 Allosteric Inhibitor Binding Site

Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp 3 character and an exquisite selectivity profile

444 TNG260, a CoREST-selective deacetylase inhibitor, reverses anti-PD1 resistance driven by loss of STK11

Proteolytic Activation of Recombinant Pro-memapsin 2 (Pro-β-secretase) Studied with New Fluorogenic Substrates

The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors

Abstract 3578: A novel and selective 3-phosphoinositide-dependent kinase-1 inhibitor, PF-5177624, blocks insulin-like growth factor-1 induced tumorigenesis in breast cancer cells

Discovery of Novel, Potent, and Selective Inhibitors of 3-Phosphoinositide-Dependent Kinase (PDK1)

Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery

Correction to “Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure”

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275

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