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Covalent PROTACs: the best of both worlds?

RSC medicinal chemistry, 2021-09, Vol.12 (9), p.1452-1458

Grimster, Neil P

2021

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Toward the Molecular Mechanism(s) by Which EGCG Treatment Remodels Mature Amyloid Fibrils

Journal of the American Chemical Society, 2013-05, Vol.135 (20), p.7503-7510

2013

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Cu(II)-Catalyzed Direct and Site-Selective Arylation of Indoles Under Mild Conditions

Journal of the American Chemical Society, 2008-07, Vol.130 (26), p.8172-8174

2008

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Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

Nature chemical biology, 2016-11, Vol.12 (11), p.931-936

2016

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Palladium-Catalyzed Intermolecular Alkenylation of Indoles by Solvent-Controlled Regioselective CH Functionalization

Angewandte Chemie International Edition, 2005-05, Vol.44 (20), p.3125-3129

2005

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Mild Aerobic Oxidative Palladium (II) Catalyzed C−H Bond Functionalization: Regioselective and Switchable C−H Alkenylation and Annulation of Pyrroles

Journal of the American Chemical Society, 2006-03, Vol.128 (8), p.2528-2529

2006

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The Design of Covalent-Based Inhibitors

1, 2021

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Beyond cysteine: recent developments in the area of targeted covalent inhibition

Current opinion in chemical biology, 2018-06, Vol.44, p.30-38

2018

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Catalytic Asymmetric Transannulation of NH-1,2,3-Triazoles with Olefins

Angewandte Chemie International Edition, 2014-03, Vol.53 (13), p.3452-3456

International ed. in English, 2014

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Selective Janus kinase 1 inhibition resolves inflammation and restores hair growth offering a viable treatment option for alopecia areata

Skin health and disease, 2023-06, Vol.3 (3), p.e209-n/a

2023

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Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate

Journal of the American Chemical Society, 2013-04, Vol.135 (15), p.5656-5668

2013

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Discovery and optimization of covalent Bcl-xL antagonists

Bioorganic & medicinal chemistry letters, 2019-12, Vol.29 (23), p.126682-126682, Article 126682

2019

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Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization

Journal of medicinal chemistry, 2023-10, Vol.66 (19), p.13400-13415

2023

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Discovery of (2R)‑N‑[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]‑1H‑indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor

Journal of medicinal chemistry, 2020-05, Vol.63 (9), p.4517-4527

2020

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Accelerated Discovery of Carbamate Cbl‑b Inhibitors Using Generative AI Models and Structure-Based Drug Design

Journal of medicinal chemistry, 2024-08, Vol.67 (16), p.14210-14233

2024

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Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1

Expert opinion on therapeutic patents, 2017-02, Vol.27 (2), p.127-143

2017

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Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Bioorganic & medicinal chemistry letters, 2023-07, Vol.91, p.129352-129352, Article 129352

2023

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Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors via in situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template

Journal of the American Chemical Society, 2012-04, Vol.134 (15), p.6732-6740

2012

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Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors

Journal of medicinal chemistry, 2018-06, Vol.61 (12), p.5235-5244

2018

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Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Bioorganic & medicinal chemistry letters, 2020-10, Vol.30 (19), p.127433, Article 127433

2020

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Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2

Expert opinion on therapeutic patents, 2017-02, Vol.27 (2), p.145-161

2017

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Discovery of (2 R )- N -[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H -indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor

Journal of medicinal chemistry, 2020-05, Vol.63 (9), p.4517-4527

2020

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Discovery of a Novel Benzodiazepine Series of Cbl‑b Inhibitors for the Enhancement of Antitumor Immunity

ACS medicinal chemistry letters, 2023-12, Vol.14 (12), p.1848-1856

2023

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Binding of 3,4,5,6-Tetrahydroxyazepanes to the Acid-β-glucosidase Active Site: Implications for Pharmacological Chaperone Design for Gaucher Disease

Biochemistry (Easton), 2011-12, Vol.50 (49), p.10647-10657

2011

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Covalent PROTACs: the best of both worlds?

Toward the Molecular Mechanism(s) by Which EGCG Treatment Remodels Mature Amyloid Fibrils

Cu(II)-Catalyzed Direct and Site-Selective Arylation of Indoles Under Mild Conditions

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

Palladium-Catalyzed Intermolecular Alkenylation of Indoles by Solvent-Controlled Regioselective CH Functionalization

Mild Aerobic Oxidative Palladium (II) Catalyzed C−H Bond Functionalization: Regioselective and Switchable C−H Alkenylation and Annulation of Pyrroles

The Design of Covalent-Based Inhibitors

Beyond cysteine: recent developments in the area of targeted covalent inhibition

Catalytic Asymmetric Transannulation of NH-1,2,3-Triazoles with Olefins

Selective Janus kinase 1 inhibition resolves inflammation and restores hair growth offering a viable treatment option for alopecia areata

Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate

Discovery and optimization of covalent Bcl-xL antagonists

Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization

Discovery of (2R)‑N‑[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]‑1H‑indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor

Accelerated Discovery of Carbamate Cbl‑b Inhibitors Using Generative AI Models and Structure-Based Drug Design

Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl‑b Inhibitors

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1

Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors via in situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template

Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2

Discovery of (2 R )- N -[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H -indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor

Discovery of a Novel Benzodiazepine Series of Cbl‑b Inhibitors for the Enhancement of Antitumor Immunity

Binding of 3,4,5,6-Tetrahydroxyazepanes to the Acid-β-glucosidase Active Site: Implications for Pharmacological Chaperone Design for Gaucher Disease

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