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Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains

Journal of medicinal chemistry, 2020-03, Vol.63 (6), p.3227-3237

2020

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Advances of small molecule targeting of kinases

Current opinion in chemical biology, 2017-08, Vol.39, p.126-132

2017

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Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity

Journal of medicinal chemistry, 2022-08, Vol.65 (15), p.10441-10458

2022

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Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof

Journal of medicinal chemistry, 2021-02, Vol.64 (4), p.2228-2241

2021

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Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors

ACS chemical biology, 2018-03, Vol.13 (3), p.582-590

2018

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Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

ACS chemical biology, 2014-05, Vol.9 (5), p.1160-1171

2014

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Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain

Journal of medicinal chemistry, 2022-03, Vol.65 (5), p.4182-4200

2022

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Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors

Journal of medicinal chemistry, 2017-09, Vol.60 (18), p.7863-7875

2017

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Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.15772-15786

2021

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An Advanced Tool To Interrogate BRD9

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4459-4461

2016

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Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

ACS chemical biology, 2013-11, Vol.8 (11), p.2360-2365

2013

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Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice

Journal of medicinal chemistry, 2023-02, Vol.66 (3), p.1928-1940

2023

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New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

Journal of medicinal chemistry, 2021-09, Vol.64 (18), p.13902-13917

2021

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Development of Dimethylisoxazole-Attached Imidazo[1,2‑a]pyridines as Potent and Selective CBP/P300 Inhibitors

Journal of medicinal chemistry, 2021-05, Vol.64 (9), p.5787-5801

2021

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Discovery of a Potential Allosteric Ligand Binding Site in CDK2

ACS chemical biology, 2011-05, Vol.6 (5), p.492-501

2011

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Molecular basis for the herbicide resistance of Roundup Ready crops

Proceedings of the National Academy of Sciences - PNAS, 2006-08, Vol.103 (35), p.13010-13015

2006

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NMR Analyses of Acetylated H2A.Z Isoforms Identify Differential Binding Interactions with the Bromodomain of the NURF Nucleosome Remodeling Complex

Biochemistry (Easton), 2020-05, Vol.59 (20), p.1871-1880

2020

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Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding

Nature communications, 2023-06, Vol.14 (1), p.3213-3213, Article 3213

2023

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Chemical Proteomics with Novel Fully Functionalized Fragments and Stringent Target Prioritization Identifies the Glutathione-Dependent Isomerase GSTZ1 as a Lung Cancer Target

ACS chemical biology, 2023-02, Vol.18 (2), p.251-264

2023

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The Fungal Product Terreic Acid Is a Covalent Inhibitor of the Bacterial Cell Wall Biosynthetic Enzyme UDP-N-Acetylglucosamine 1-Carboxyvinyltransferase (MurA)

Biochemistry (Easton), 2010-05, Vol.49 (19), p.4276-4282

2010

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Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon

The Journal of biological chemistry, 2018-04, Vol.293 (16), p.6187-6200

2018

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Tetrahydroindazole inhibitors of CDK2/cyclin complexes

European journal of medicinal chemistry, 2021-03, Vol.214, p.113232-113232, Article 113232

2021

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Ack1 mediated AKT/PKB tyrosine 176 phosphorylation regulates its activation

PloS one, 2010-03, Vol.5 (3), p.e9646-e9646

2010

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BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen

Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.4805-4817

2017

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Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains

Advances of small molecule targeting of kinases

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity

Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof

Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors

Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors

An Advanced Tool To Interrogate BRD9

Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

Development of Dimethylisoxazole-Attached Imidazo[1,2‑a]pyridines as Potent and Selective CBP/P300 Inhibitors

Discovery of a Potential Allosteric Ligand Binding Site in CDK2

Molecular basis for the herbicide resistance of Roundup Ready crops

NMR Analyses of Acetylated H2A.Z Isoforms Identify Differential Binding Interactions with the Bromodomain of the NURF Nucleosome Remodeling Complex

Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding

Chemical Proteomics with Novel Fully Functionalized Fragments and Stringent Target Prioritization Identifies the Glutathione-Dependent Isomerase GSTZ1 as a Lung Cancer Target

The Fungal Product Terreic Acid Is a Covalent Inhibitor of the Bacterial Cell Wall Biosynthetic Enzyme UDP-N-Acetylglucosamine 1-Carboxyvinyltransferase (MurA)

EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma

Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon

Tetrahydroindazole inhibitors of CDK2/cyclin complexes

Ack1 mediated AKT/PKB tyrosine 176 phosphorylation regulates its activation

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen

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