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Dirk A. Heerding

GlaxoSmithKline

48

Papers

1977

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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells.

2021 Journal of Medicinal Chemistry
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Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

2021
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Discovery of Isoxazone Amides as Potent and Selective SMYD3 Inhibitors

2020 ACS Medicinal Chemistry Letters
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Generation and Validation of Intracellular Ubiquitin Variant Inhibitors for USP7 and USP10

2017 Journal of Molecular Biology
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Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity

2015 Molecular Pharmacology
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Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction

2014 Nature Chemical Biology
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Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK).

2012 Journal of Medicinal Chemistry
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Phosphoinositide-Dependent Kinase-1 (PDK1) kinase domain with 6-(3-Amino-1H-indazol-6-yl)-N4-ethyl-2,4-pyrimidinediamine

2011
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Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors.

2011 Journal of Medicinal Chemistry
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Derives d'indoline substitue comme inhibiteurs de perk

2011
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