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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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Structural basis for the action of the drug trametinib at KSR-bound MEK

Nature (London), 2020-12, Vol.588 (7838), p.509-514

2020

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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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A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK

Nature (London), 2011-04, Vol.472 (7343), p.366-369

2011

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Integrated computational and Drosophila cancer model platform captures previously unappreciated chemicals perturbing a kinase network

PLoS computational biology, 2019-04, Vol.15 (4), p.e1006878-e1006878

2019

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Understanding and drugging RAS: 40 years to break the tip of the iceberg

Disease models & mechanisms, 2022-02, Vol.15 (2)

2022

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Hepatitis C virus genetics affects miR-122 requirements and response to miR-122 inhibitors

Nature communications, 2014-11, Vol.5 (1), p.5408-5408, Article 5408

2014

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A pickup in pseudokinase activity

Biochemical Society transactions, 2013-08, Vol.41 (4), p.987

Dar, Arvin C

2013

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Structure-Guided Inhibitor Design Expands the Scope of Analog-Sensitive Kinase Technology

ACS chemical biology, 2013-09, Vol.8 (9), p.1931-1938

2013

Volltextzugriff (PDF)

Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic

eLife, 2015-05, Vol.4

2015

Volltextzugriff (PDF)

Formin Leaky Cap Allows Elongation in the Presence of Tight Capping Proteins

Current biology, 2003-10, Vol.13 (20), p.1820-1823

2003

Volltextzugriff (PDF)

Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling

Nature (London), 2016-09, Vol.537 (7618), p.112-116

2016

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RASopathy mutations open new insights into the mechanism of BRAF activation

Molecular cell, 2022-11, Vol.82 (22), p.4192-4193

2022

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Live-cell target engagement of allosteric MEKi on MEK-RAF/KSR-14-3-3 complexes

Nature chemical biology, 2024-03, Vol.20 (3), p.373

2024

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An Antagonist of KSR1‐Driven Adaptive Resistance to Clinical RAS‐MAPK Inhibitors

The FASEB journal, 2022-05, Vol.36 (S1), p.n/a

2022

Volltextzugriff (PDF)

Conformational control and regulation of the pseudokinase KSR via small molecule binding interactions

Methods in enzymology, 2022, Vol.667, p.365-402

2022

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Ploidy Leads a Molecular Motor to Walk Different Paths to Drug Resistance

Cell chemical biology, 2020-07, Vol.27 (7), p.770-772

2020

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X-Ray Crystal Structure and Functional Analysis of Vaccinia Virus K3L Reveals Molecular Determinants for PKR Subversion and Substrate Recognition

Molecular cell, 2002-08, Vol.10 (2), p.295-305

2002

Volltextzugriff (PDF)

Targeting drug-resistant mutations in ALK

Nature cancer, 2022-06, Vol.3 (6), p.659

2022

Volltextzugriff (PDF)

Rapid, scalable assessment of SARS-CoV-2 cellular immunity by whole-blood PCR

Nature biotechnology, 2022-11, Vol.40 (11), p.1680-1689

2022

Volltextzugriff (PDF)

A whole-animal platform to advance a clinical kinase inhibitor into new disease space

Nature chemical biology, 2018-03, Vol.14 (3), p.291

2018

Volltextzugriff (PDF)

Protein kinase PKR mutants resistant to the poxvirus pseudosubstrate K3L protein

Proceedings of the National Academy of Sciences - PNAS, 2008-11, Vol.105 (44), p.16894-16899

2008

Volltextzugriff (PDF)

Type II Binders Targeting the “GLR-Out” Conformation of the Pseudokinase STRADα

Biochemistry (Easton), 2021-02, Vol.60 (4), p.289-302

2021

Volltextzugriff (PDF)

PKR and GCN2 Kinases and Guanine Nucleotide Exchange Factor Eukaryotic Translation Initiation Factor 2B (eIF2B) Recognize Overlapping Surfaces on eIF2α

Molecular and Cellular Biology, 2005-04, Vol.25 (8), p.3063-3075

2005

Volltextzugriff (PDF)

Phenotype-Based Screens with Conformation-Specific Inhibitors Reveal p38 Gamma and Delta as Targets for HCC Polypharmacology

Molecular cancer therapeutics, 2019-09, Vol.18 (9), p.1506-1519

2019

Volltextzugriff (PDF)

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

Structural basis for the action of the drug trametinib at KSR-bound MEK

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

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK

Integrated computational and Drosophila cancer model platform captures previously unappreciated chemicals perturbing a kinase network

Understanding and drugging RAS: 40 years to break the tip of the iceberg

Hepatitis C virus genetics affects miR-122 requirements and response to miR-122 inhibitors

A pickup in pseudokinase activity

Structure-Guided Inhibitor Design Expands the Scope of Analog-Sensitive Kinase Technology

Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic

Formin Leaky Cap Allows Elongation in the Presence of Tight Capping Proteins

Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling

RASopathy mutations open new insights into the mechanism of BRAF activation

Live-cell target engagement of allosteric MEKi on MEK-RAF/KSR-14-3-3 complexes

An Antagonist of KSR1‐Driven Adaptive Resistance to Clinical RAS‐MAPK Inhibitors

Conformational control and regulation of the pseudokinase KSR via small molecule binding interactions

Ploidy Leads a Molecular Motor to Walk Different Paths to Drug Resistance

X-Ray Crystal Structure and Functional Analysis of Vaccinia Virus K3L Reveals Molecular Determinants for PKR Subversion and Substrate Recognition

Targeting drug-resistant mutations in ALK

Rapid, scalable assessment of SARS-CoV-2 cellular immunity by whole-blood PCR

A whole-animal platform to advance a clinical kinase inhibitor into new disease space

Protein kinase PKR mutants resistant to the poxvirus pseudosubstrate K3L protein

Type II Binders Targeting the “GLR-Out” Conformation of the Pseudokinase STRADα

PKR and GCN2 Kinases and Guanine Nucleotide Exchange Factor Eukaryotic Translation Initiation Factor 2B (eIF2B) Recognize Overlapping Surfaces on eIF2α

Phenotype-Based Screens with Conformation-Specific Inhibitors Reveal p38 Gamma and Delta as Targets for HCC Polypharmacology

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