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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

Cell chemical biology, 2019-11, Vol.26 (11), p.1486-1500

2019

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Copper(I)-Catalyzed Addition of Grignard Reagents to in Situ-Derived N-Sulfonyl Azoalkenes: An Umpolung Alkylation Procedure Applicable to the Formation of Up to Three Contiguous Quaternary Centers

Journal of the American Chemical Society, 2010-04, Vol.132 (13), p.4546-4547

2010

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Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth

The Journal of clinical investigation, 2018-10, Vol.128 (10), p.4397-4412

2018

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A kinase-independent role for CDK8 in BCR-ABL1+ leukemia

Nature communications, 2019-10, Vol.10 (1), p.4741-15, Article 4741

2019

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Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer

ACS chemical biology, 2015-12, Vol.10 (12), p.2687-2696

2015

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Crystal structure of human IRAK1

Proceedings of the National Academy of Sciences - PNAS, 2017-12, Vol.114 (51), p.13507-13512

2017

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SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform

Cell chemical biology, 2018-04, Vol.25 (4), p.460-470.e6

2018

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Development of CDK2 and CDK5 Dual Degrader TMX‐2172

Angewandte Chemie International Edition, 2020-08, Vol.59 (33), p.13865-13870

International ed. in English, 2020

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Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

ACS medicinal chemistry letters, 2018-06, Vol.9 (6), p.540-545

2018

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Development of a highly potent and selective degrader of LRRK2

Bioorganic & medicinal chemistry letters, 2023-10, Vol.94, p.129449-129449, Article 129449

2023

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Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions

Journal of medicinal chemistry, 2023-04, Vol.66 (8), p.5524-5535

2023

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A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer

Cancer research (Chicago, Ill.), 2022-04, Vol.82 (8), p.1633-1645

2022

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Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors

Cancer research (Chicago, Ill.), 2023-01, Vol.83 (2), p.285-300

2023

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Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor–associated kinase 4 (IRAK4)

The Journal of biological chemistry, 2019-03, Vol.294 (12), p.4511-4519

2019

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Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation

Journal of medicinal chemistry, 2015-12, Vol.58 (23), p.9296-9308

2015

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Peptide-based covalent inhibitors of MALT1 paracaspase

Bioorganic & medicinal chemistry letters, 2019-06, Vol.29 (11), p.1336-1339

2019

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Quinoline and thiazolopyridine allosteric inhibitors of MALT1

Bioorganic & medicinal chemistry letters, 2019-07, Vol.29 (14), p.1694-1698

2019

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Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19

ACS medicinal chemistry letters, 2021-11, Vol.12 (11), p.1689-1693

2021

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Selective Macrocyclic Inhibitors of DYRK1A/B

ACS medicinal chemistry letters, 2022-04, Vol.13 (4), p.577-585

2022

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Brain Penetrant LRRK2 Inhibitor

ACS medicinal chemistry letters, 2012-08, Vol.3 (8), p.658-662

2012

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Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B‑Cell Lymphoma

ACS medicinal chemistry letters, 2020-11, Vol.11 (11), p.2238-2243

2020

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Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor

ACS medicinal chemistry letters, 2015-05, Vol.6 (5), p.584-589

2015

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Catalytic Asymmetric Addition of Thiols to Nitrosoalkenes Leading to Chiral Non-Racemic α-Sulfenyl Ketones

Organic letters, 2011-08, Vol.13 (15), p.3810-3813

2011

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Small-Molecule Inhibitors of LRRK2

Advances in neurobiology, 2017-01, Vol.14, p.241-264

2017

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Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor

ACS medicinal chemistry letters, 2016-05, Vol.7 (5), p.476-481

2016

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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

Copper(I)-Catalyzed Addition of Grignard Reagents to in Situ-Derived N-Sulfonyl Azoalkenes: An Umpolung Alkylation Procedure Applicable to the Formation of Up to Three Contiguous Quaternary Centers

Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth

A kinase-independent role for CDK8 in BCR-ABL1+ leukemia

Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer

Crystal structure of human IRAK1

SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform

Development of CDK2 and CDK5 Dual Degrader TMX‐2172

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

Development of a highly potent and selective degrader of LRRK2

Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions

A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer

Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors

Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor–associated kinase 4 (IRAK4)

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation

Peptide-based covalent inhibitors of MALT1 paracaspase

Quinoline and thiazolopyridine allosteric inhibitors of MALT1

Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19

Selective Macrocyclic Inhibitors of DYRK1A/B

Brain Penetrant LRRK2 Inhibitor

Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B‑Cell Lymphoma

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor

Catalytic Asymmetric Addition of Thiols to Nitrosoalkenes Leading to Chiral Non-Racemic α-Sulfenyl Ketones

Small-Molecule Inhibitors of LRRK2

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor

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