A small molecule inhibitor of HER3: a proof-of-concept study

HER3 targeting with an antibody‐drug conjugate bypasses resistance to anti‐HER2 therapies

(2020) Lucía Gandullo‐Sánchez et al.   EMBO Molecular Medicine

Prospects for pharmacological targeting of pseudokinases

(2019) Jennifer E. Kung et al.   NATURE REVIEWS DRUG DISCOVERY

Tracing the origin and evolution of pseudokinases across the tree of life

(2019) Annie Kwon et al.   Science Signaling

ERBB3 mutations in cancer: biological aspects, prevalence and therapeutics

(2019) Nicolas Kiavue et al.   ONCOGENE

Pseudokinases: a tribble‐edged sword

(2019) Laura Richmond et al.   FEBS Journal

MEK drives BRAF activation through allosteric control of KSR proteins

(2018) Hugo Lavoie et al.   NATURE

Inhibitor-induced HER2-HER3 heterodimerisation promotes proliferation through a novel dimer interface

(2018) Jeroen Claus et al.   eLife

The structure of serum resistance-associated protein and its implications for human African trypanosomiasis

(2018) Sebastian Zoll et al.   Nature Microbiology

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells

(2018) Daniel M. Foulkes et al.   Science Signaling

The architecture of EGFR’s basal complexes reveals autoinhibition mechanisms in dimers and oligomers

(2018) Laura C. Zanetti-Domingues et al.   Nature Communications

Pseudokinases: update on their functions and evaluation as new drug targets

(2017) Dominic P Byrne et al.   Future Medicinal Chemistry

RAF inhibitors promote RAS-RAF interaction by allosterically disrupting RAF autoinhibition

(2017) Ting Jin et al.   Nature Communications

A comprehensive review of heregulins, HER3, and HER4 as potential therapeutic targets in cancer

(2017) Jose Mauricio Mota et al.   Oncotarget

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

(2016) Neil S. Dhawan et al.   NATURE

Structural Basis for the Non-catalytic Functions of Protein Kinases

(2016) Jennifer E. Kung et al.   STRUCTURE

Going for broke: targeting the human cancer pseudokinome

(2015) Fiona P. Bailey et al.   BIOCHEMICAL JOURNAL

Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain

(2015) John S. Tokarski et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting HER3 by interfering with its Sec61-mediated cotranslational insertion into the endoplasmic reticulum

(2015) A Ruiz-Saenz et al.   ONCOGENE

Inhibition of ErbB3 by a monoclonal antibody that locks the extracellular domain in an inactive configuration

(2015) Sangwon Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A role for the pseudokinase HER3 in the acquired resistance against EGFR- and HER2-directed targeted therapy

(2014) Jeroen Claus et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

HER3, serious partner in crime

(2014) Arjan Kol et al.   PHARMACOLOGY & THERAPEUTICS

Day of the dead: pseudokinases and pseudophosphatases in physiology and disease

(2014) Veronika Reiterer et al.   TRENDS IN CELL BIOLOGY

A robust methodology to subclassify pseudokinases based on their nucleotide-binding properties

(2013) James M. Murphy et al.   BIOCHEMICAL JOURNAL

Pseudokinase drug intervention: a potentially poisoned chalice

(2013) Jeroen Claus et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Oncogenic ERBB3 Mutations in Human Cancers

(2013) Bijay S. Jaiswal et al.   CANCER CELL

The Gray Institute ‘open’ high-content, fluorescence lifetime microscopes

(2013) P.R. BARBER et al.   JOURNAL OF MICROSCOPY

RAF Inhibitor-Induced KSR1/B-RAF Binding and Its Effects on ERK Cascade Signaling

(2011) Melissa M. McKay et al.   CURRENT BIOLOGY

Automated multidimensional single molecule fluorescence microscopy feature detection and tracking

(2011) Daniel J. Rolfe et al.   EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS

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

(2011) Damian F. Brennan et al.   NATURE

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

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

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation

(2010) Fumin Shi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A dimerization-dependent mechanism drives RAF catalytic activation

(2009) Thanashan Rajakulendran et al.   NATURE

Inhibitor hijacking of Akt activation

(2009) Tatsuya Okuzumi et al.   Nature Chemical Biology

PKC maturation is promoted by nucleotide pocket occupation independently of intrinsic kinase activity

(2009) Angus J M Cameron et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3

(2009) N. Jura et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of the LKB1-STRAD-MO25 Complex Reveals an Allosteric Mechanism of Kinase Activation

(2009) E. Zeqiraj et al.   SCIENCE

ATP and MO25α Regulate the Conformational State of the STRADα Pseudokinase and Activation of the LKB1 Tumour Suppressor

(2009) Elton Zeqiraj et al.   PLOS BIOLOGY

Mechanisms of acquired resistance to cetuximab: role of HER (ErbB) family members

(2008) D L Wheeler et al.   ONCOGENE