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MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

PLoS biology, 2019-09, Vol.17 (9), p.e3000354-e3000354

2019

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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Journal of medicinal chemistry, 2022-11, Vol.65 (21), p.14721-14739

2022

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Four-Component Synthesis of Fully Substituted 1,2,4-Triazoles

Angewandte Chemie (International ed.), 2010-01, Vol.49 (2), p.325-328

2010

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Gold(I)-Catalyzed Stereoselective Olefin Cyclopropanation

Journal of the American Chemical Society, 2005-12, Vol.127 (51), p.18002-18003

2005

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Au(I)-Catalyzed Ring Expanding Cycloisomerizations: Total Synthesis of Ventricosene

Organic letters, 2008-10, Vol.10 (19), p.4315-4318

2008

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Gold(I)-Catalyzed Ring Expansion of Cyclopropanols and Cyclobutanols

Journal of the American Chemical Society, 2005-07, Vol.127 (27), p.9708-9709

2005

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Gold(I)-Catalyzed Cyclizations of Silyl Enol Ethers: Application to the Synthesis of (+)-Lycopladine A

Angewandte Chemie (International ed.), 2006-09, Vol.45 (36), p.5991-5994

2006

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The Crystal Structure of the Catalytic Domain of the NF-κB Inducing Kinase Reveals a Narrow but Flexible Active Site

Structure (London), 2012-10, Vol.20 (10), p.1704-1714

2012

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Correction: MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

PLoS biology, 2019-10, Vol.17 (10), p.e3000529-e3000529

2019

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Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.7957-7985

2020

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Monomeric Targeted Protein Degraders

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11330-11361

2020

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Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Journal of medicinal chemistry, 2020-03, Vol.63 (6), p.2807-2813

2020

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Selective activation of PFKL suppresses the phagocytic oxidative burst

Cell, 2021-08, Vol.184 (17), p.4480-4494.e15

2021

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A General Strategy for the Construction of Functionalized Azaindolines via Domino Palladium-Catalyzed Heck Cyclization/Suzuki Coupling

Organic letters, 2017-07, Vol.19 (13), p.3616-3619

2017

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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16589-16621

2022

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Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Nature biotechnology, 2022-01, Vol.40 (1), p.86-93

2022

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Targeted degradation via direct 26S proteasome recruitment

Nature chemical biology, 2023-01, Vol.19 (1), p.55-63

2023

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Cancer discovery, 2022-01, Vol.12 (1), p.204-219

2022

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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4597-4610

2013

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Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

Journal of medicinal chemistry, 2019-08, Vol.62 (15), p.7032-7041

2019

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Heteroarylation of Azine N-Oxides

Organic letters, 2012-02, Vol.14 (3), p.862-865

2012

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Primary Amine Tethered Small Molecules Promote the Degradation of X‑Linked Inhibitor of Apoptosis Protein

Journal of the American Chemical Society, 2021-07, Vol.143 (28), p.10571-10575

2021

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Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

Journal of medicinal chemistry, 2022-09, Vol.65 (17), p.11500-11512

2022

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Four-Component Synthesis of Fully Substituted 1,2,4-Triazoles

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus

Gold(I)-Catalyzed Stereoselective Olefin Cyclopropanation

Au(I)-Catalyzed Ring Expanding Cycloisomerizations: Total Synthesis of Ventricosene

Gold(I)-Catalyzed Ring Expansion of Cyclopropanols and Cyclobutanols

Gold(I)-Catalyzed Cyclizations of Silyl Enol Ethers: Application to the Synthesis of (+)-Lycopladine A

The Crystal Structure of the Catalytic Domain of the NF-κB Inducing Kinase Reveals a Narrow but Flexible Active Site

Correction: MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Monomeric Targeted Protein Degraders

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Selective activation of PFKL suppresses the phagocytic oxidative burst

A General Strategy for the Construction of Functionalized Azaindolines via Domino Palladium-Catalyzed Heck Cyclization/Suzuki Coupling

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα

Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Targeted degradation via direct 26S proteasome recruitment

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

Heteroarylation of Azine N-Oxides

Primary Amine Tethered Small Molecules Promote the Degradation of X‑Linked Inhibitor of Apoptosis Protein

Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

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