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Drugging the 'undruggable' cancer targets

Nature reviews. Cancer, 2017-08, Vol.17 (8), p.502-508

2017

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Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

Nature reviews. Drug discovery, 2016-11, Vol.15 (11), p.771-785

2016

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Drugging MYCN through an Allosteric Transition in Aurora Kinase A

Cancer cell, 2014-09, Vol.26 (3), p.414-427

2014

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Bifunctional Small‐Molecule Ligands of K‐Ras Induce Its Association with Immunophilin Proteins

Angewandte Chemie International Edition, 2019-11, Vol.58 (45), p.16314-16319

International ed. in English, 2019

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The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

Annual review of biochemistry, 2011-07, Vol.80 (1), p.769-795

2011

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A Neo-Substrate that Amplifies Catalytic Activity of Parkinson’s-Disease-Related Kinase PINK1

Cell, 2013-08, Vol.154 (4), p.737-747

2013

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Disease-Causing Mutations in the G Protein Gαs Subvert the Roles of GDP and GTP

Cell, 2018-05, Vol.173 (5), p.1254-1264.e11

2018

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K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

Nature (London), 2013-11, Vol.503 (7477), p.548-551

2013

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Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2

PLoS biology, 2009-02, Vol.7 (2), p.e38-e1000038

2009

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Targeting the cancer kinome through polypharmacology

Nature reviews. Cancer, 2010-02, Vol.10 (2), p.130-137

2010

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RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

Nature (London), 2010-03, Vol.464 (7287), p.427-430

2010

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Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A

Science (American Association for the Advancement of Science), 2021-02, Vol.371 (6532), p.926-931

2021

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A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability

Cancer discovery, 2023-01, Vol.13 (1), p.56-69

2023

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EGFR Phosphorylates Tumor-Derived EGFRvIII Driving STAT3/5 and Progression in Glioblastoma

Cancer cell, 2013-10, Vol.24 (4), p.438-449

2013

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Evolutionarily divergent mTOR remodels translatome for tissue regeneration

Nature (London), 2023-08, Vol.620 (7972), p.163-171

2023

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Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

Nature (London), 2012-06, Vol.486 (7401), p.80-84

2012

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Chemical Genetic Screen for AMPKα2 Substrates Uncovers a Network of Proteins Involved in Mitosis

Molecular cell, 2011-12, Vol.44 (6), p.878-892

2011

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Drugging the Next Undruggable KRAS Allele-Gly12Asp

Journal of medicinal chemistry, 2022-02, Vol.65 (4), p.3119-3122

2022

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Site-specific incorporation of phosphotyrosine using an expanded genetic code

Nature chemical biology, 2017-08, Vol.13 (8), p.842-844

2017

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Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2

Science (American Association for the Advancement of Science), 2021-07, Vol.373 (6554), p.541-547

2021

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Identification of AMPK Phosphorylation Sites Reveals a Network of Proteins Involved in Cell Invasion and Facilitates Large-Scale Substrate Prediction

Cell metabolism, 2015-11, Vol.22 (5), p.907-921

2015

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MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development

Neuron (Cambridge, Mass.), 2014-12, Vol.84 (5), p.968-982

2014

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Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II

Nature structural & molecular biology, 2012-11, Vol.19 (11), p.1108-1115

2012

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Chronic TGF-β exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition

Science signaling, 2019-02, Vol.12 (570)

2019

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Drugging the 'undruggable' cancer targets

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

Drugging MYCN through an Allosteric Transition in Aurora Kinase A

Bifunctional Small‐Molecule Ligands of K‐Ras Induce Its Association with Immunophilin Proteins

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

A Neo-Substrate that Amplifies Catalytic Activity of Parkinson’s-Disease-Related Kinase PINK1

Disease-Causing Mutations in the G Protein Gαs Subvert the Roles of GDP and GTP

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2

Targeting the cancer kinome through polypharmacology

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A

A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability

EGFR Phosphorylates Tumor-Derived EGFRvIII Driving STAT3/5 and Progression in Glioblastoma

Evolutionarily divergent mTOR remodels translatome for tissue regeneration

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

Chemical Genetic Screen for AMPKα2 Substrates Uncovers a Network of Proteins Involved in Mitosis

Drugging the Next Undruggable KRAS Allele-Gly12Asp

Site-specific incorporation of phosphotyrosine using an expanded genetic code

Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2

Identification of AMPK Phosphorylation Sites Reveals a Network of Proteins Involved in Cell Invasion and Facilitates Large-Scale Substrate Prediction

Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells

MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development

Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II

Chronic TGF-β exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition

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