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Development of targeted protein degradation therapeutics

Nature chemical biology, 2019-10, Vol.15 (10), p.937-944

2019

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Accessing Drug Metabolites via Transition-Metal Catalyzed C−H Oxidation: The Liver as Synthetic Inspiration

Angewandte Chemie International Edition, 2016-11, Vol.55 (46), p.14218-14238

International ed. in English, 2016

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Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

Journal of medicinal chemistry, 2020-07, Vol.63 (13), p.6648-6676

2020

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Crystal structure of the SALL4-pomalidomide-cereblon-DDB1 complex

Nature structural & molecular biology, 2020-04, Vol.27 (4), p.319-322

2020

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SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

Nature chemical biology, 2018-10, Vol.14 (10), p.981-987

2018

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Late-stage C–H functionalization of complex alkaloids and drug molecules via intermolecular rhodium-carbenoid insertion

Nature communications, 2015-01, Vol.6 (1), p.5943-5943, Article 5943

2015

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Quaternary Charge-Transfer Complex Enables Photoenzymatic Intermolecular Hydroalkylation of Olefins

Journal of the American Chemical Society, 2021-01, Vol.143 (1), p.97-102

2021

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Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11021-11036

2018

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Intermolecular Crossed [2 + 2] Cycloaddition Promoted by Visible-Light Triplet Photosensitization: Expedient Access to Polysubstituted 2‑Oxaspiro[3.3]heptanes

Journal of the American Chemical Society, 2021-03, Vol.143 (10), p.4055-4063

2021

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Small molecule allosteric inhibitors of RORγt block Th17-dependent inflammation and associated gene expression in vivo

PloS one, 2021-11, Vol.16 (11), p.e0248034

2021

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Sustainable Practices in Medicinal Chemistry: Current State and Future Directions

Journal of medicinal chemistry, 2013-08, Vol.56 (15), p.6007-6021

2013

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Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

Nature (London), 2010-05, Vol.465 (7294), p.96-100

2010

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Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

Journal of medicinal chemistry, 2018-04, Vol.61 (7), p.2837-2864

2018

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Synthetic strategy: natural products on demand

Nature chemistry, 2014-06, Vol.6 (6), p.460

Hamann, Lawrence G

2014

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Expedient access to saturated nitrogen heterocycles by photoredox cyclization of imino-tethered dihydropyridines

Chemical science (Cambridge), 2019-11, Vol.1 (41), p.9591-9596

2019

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Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.4744-4761

2021

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Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

ACS medicinal chemistry letters, 2019-12, Vol.10 (12), p.1592-1602

2019

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Regioselective Synthesis and Slow-Release Suzuki–Miyaura Cross-Coupling of MIDA Boronate-Functionalized Isoxazoles and Triazoles

Journal of organic chemistry, 2011-12, Vol.76 (24), p.10241-10248

2011

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Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2)

Journal of medicinal chemistry, 2023-12, Vol.66 (23), p.15750-15760

2023

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Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Journal of medicinal chemistry, 2005-07, Vol.48 (15), p.5025-5037

2005

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Non-directed allylic C–H acetoxylation in the presence of Lewis basic heterocycles

Chemical science (Cambridge), 2014-01, Vol.5 (6), p.2352

2014

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Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.2790-2818

2017

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Discovery of a novel, highly potent and orally bioavailable pyrrolidinone indole series of irreversible Myeloperoxidase (MPO) inhibitors

Biochemical pharmacology, 2023-03, Vol.209, p.115418, Article 115418

2023

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Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders

Journal of medicinal chemistry, 2020-02, Vol.63 (3), p.1068-1083

2020

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Development of targeted protein degradation therapeutics

Accessing Drug Metabolites via Transition-Metal Catalyzed C−H Oxidation: The Liver as Synthetic Inspiration

Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

Crystal structure of the SALL4-pomalidomide-cereblon-DDB1 complex

SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

Late-stage C–H functionalization of complex alkaloids and drug molecules via intermolecular rhodium-carbenoid insertion

Quaternary Charge-Transfer Complex Enables Photoenzymatic Intermolecular Hydroalkylation of Olefins

Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Intermolecular Crossed [2 + 2] Cycloaddition Promoted by Visible-Light Triplet Photosensitization: Expedient Access to Polysubstituted 2‑Oxaspiro[3.3]heptanes

Small molecule allosteric inhibitors of RORγt block Th17-dependent inflammation and associated gene expression in vivo

SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice

Sustainable Practices in Medicinal Chemistry: Current State and Future Directions

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

Synthetic strategy: natural products on demand

Expedient access to saturated nitrogen heterocycles by photoredox cyclization of imino-tethered dihydropyridines

Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

Regioselective Synthesis and Slow-Release Suzuki–Miyaura Cross-Coupling of MIDA Boronate-Functionalized Isoxazoles and Triazoles

Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2)

Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Non-directed allylic C–H acetoxylation in the presence of Lewis basic heterocycles

Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer

Discovery of a novel, highly potent and orally bioavailable pyrrolidinone indole series of irreversible Myeloperoxidase (MPO) inhibitors

Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders

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