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Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO

PloS one, 2014-06, Vol.9 (6), p.e98896-e98896

2014

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Keap Calm, and Carry on Covalently

Journal of medicinal chemistry, 2013-10, Vol.56 (19), p.7463-7476

2013

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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.15949-15972

2021

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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2

Angewandte Chemie (International ed.), 2001-01, Vol.40 (1), p.196-199

2001

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Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2 H -Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress

The Journal of pharmacology and experimental therapeutics, 2017-10, Vol.363 (1), p.114-125

2017

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3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent

ACS medicinal chemistry letters, 2018-12, Vol.9 (12), p.1164-1169

2018

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Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IκB Kinase-β (IKK-β)

Journal of medicinal chemistry, 2009-05, Vol.52 (9), p.3098-3102

2009

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Progress Towards the Development of Anti-Inflammatory Inhibitors of IKKβ

Current topics in medicinal chemistry, 2009-05, Vol.9 (7), p.623-639

2009

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The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β kinases

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.3972-3977

2007

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Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2

Tetrahedron, 2009-08, Vol.65 (33), p.6470-6488

2009

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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β

Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (8), p.2255-2258

2011

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Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent

Bioorganic & medicinal chemistry letters, 2011-08, Vol.21 (15), p.4409-4415

2011

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3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.3864-3867

2007

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A Highly Convergent Synthesis of 2-Phenyl Quinoline as Dual Antagonists for NK2 and NK3 Receptors

Synthetic communications, 2005-12, Vol.35 (24), p.3105-3112

2005

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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IIK-β

Bioorganic & medicinal chemistry letters, 2011, Vol.21 (8), p.2255-2258

2011

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Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2: 2008 Tetrahedron Prize for Creativity in Organic Chemistry. The Art of Synthesis: Methods, Strategies and Applications

Tetrahedron, 2009, Vol.65 (33)

2009

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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, a NIH Postdoctoral Fellowship to C.S.B., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the

Angewandte Chemie International Edition, 2001-01, Vol.40 (1), p.196-199

2001

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Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IKB Kinase-β (IKK-β)

Journal of medicinal chemistry, 2009, Vol.52 (9), p.3098-3102

2009

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3-Arylamino-2 H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists

Bioorganic & medicinal chemistry letters, 2007, Vol.17 (14), p.3864-3867

2007

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3 -arylamino -2H-1,2,4 -benzothiadiazin -5 -ol 1,1-dioxides as novel and selective CXCR antagonists

Bioorganic & medicinal chemistry letters, 2007, Vol.17 (14), p.3864-3867

2007

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Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta)

Journal of medicinal chemistry, 2009-05, Vol.52 (9), p.3098

2009

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Vitamin K analogs and their action against hepatocellular carcinoma: A case for tyrosine phosphatase inhibition

Kerns, Jeffrey K

1998

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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2

Angewandte Chemie, 2001-01, Vol.113 (1), p.202-205

2001

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Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO

Keap Calm, and Carry on Covalently

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery

Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction

Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction

The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2

Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2 H -Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress

3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent

Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IκB Kinase-β (IKK-β)

Progress Towards the Development of Anti-Inflammatory Inhibitors of IKKβ

The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β kinases

Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2

3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β

Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists

A Highly Convergent Synthesis of 2-Phenyl Quinoline as Dual Antagonists for NK2 and NK3 Receptors

3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IIK-β

Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2: 2008 Tetrahedron Prize for Creativity in Organic Chemistry. The Art of Synthesis: Methods, Strategies and Applications

Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IKB Kinase-β (IKK-β)

3-Arylamino-2 H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists

3 -arylamino -2H-1,2,4 -benzothiadiazin -5 -ol 1,1-dioxides as novel and selective CXCR antagonists

Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta)

Vitamin K analogs and their action against hepatocellular carcinoma: A case for tyrosine phosphatase inhibition

The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2

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