Ten things you should know about protein kinases: IUPHAR Review 14

Potential Therapeutic Strategies to Overcome Acquired Resistance to BRAF or MEK Inhibitors in BRAF Mutant Cancers

(2015) Ryan B. Corcoran et al.   Oncotarget

Ponatinib: A Review of Its Use in Adults with Chronic Myeloid Leukaemia or Philadelphia Chromosome-Positive Acute Lymphoblastic Leukaemia

(2014) Sheridan M. Hoy   DRUGS

Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases

(2014) Sandra W Cowan-Jacob et al.   Future Medicinal Chemistry

Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial

(2014) Martin Reck et al.   LANCET ONCOLOGY

PI3K and cancer: lessons, challenges and opportunities

(2014) David A. Fruman et al.   NATURE REVIEWS DRUG DISCOVERY

Efficacy and Safety of Nintedanib in Idiopathic Pulmonary Fibrosis

(2014) Luca Richeldi et al.   NEW ENGLAND JOURNAL OF MEDICINE

PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma

(2014) Ajay K. Gopal et al.   NEW ENGLAND JOURNAL OF MEDICINE

Ibrutinib Resistance in Chronic Lymphocytic Leukemia

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mechanism of Activation of Protein Kinase JAK2 by the Growth Hormone Receptor

(2014) A. J. Brooks et al.   SCIENCE

Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001): Processes, Limitations, and Further Proposals

(2014) Terence O'Reilly et al.   Translational Oncology

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer

(2014) L. Friboulet et al.   Cancer Discovery

A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery

(2013) Yinghong Gao et al.   BIOCHEMICAL JOURNAL

Structure-based discovery of cellular-active allosteric inhibitors of FAK

(2013) Naoki Tomita et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Everolimus plus exemestane as first-line therapy in HR+, HER2− advanced breast cancer in BOLERO-2

(2013) J. Thaddeus Beck et al.   BREAST CANCER RESEARCH AND TREATMENT

The Concise Guide to PHARMACOLOGY 2013/14: Catalytic Receptors

(2013) Stephen P.H. Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2013/14: Enzymes

(2013) Stephen P.H. Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Molecular Mechanism of SSR128129E, an Extracellularly Acting, Small-Molecule, Allosteric Inhibitor of FGF Receptor Signaling

(2013) Corentin Herbert et al.   CANCER CELL

Inhibition of Tumor Angiogenesis and Growth by a Small-Molecule Multi-FGF Receptor Blocker with Allosteric Properties

(2013) Françoise Bono et al.   CANCER CELL

RAF Inhibitors Activate the MAPK Pathway by Relieving Inhibitory Autophosphorylation

(2013) Matthew Holderfield et al.   CANCER CELL

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Ibrutinib and Indolent B-Cell Lymphomas

(2013) Akintunde Akinleye et al.   Clinical Lymphoma Myeloma & Leukemia

Targeting kinases: a new approach to treating inflammatory rheumatic diseases

(2013) David L Simmons   CURRENT OPINION IN PHARMACOLOGY

Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology

(2013) Paul Workman et al.   CURRENT OPINION IN PHARMACOLOGY

Trametinib: First Global Approval

(2013) Cameron J. M. Wright et al.   DRUGS

Dabrafenib: First Global Approval

(2013) Anita D. Ballantyne et al.   DRUGS

Trametinib (GSK1120212) in the treatment of melanoma

(2013) April KS Salama et al.   EXPERT OPINION ON PHARMACOTHERAPY

Cabozantinib (XL184) for the treatment of locally advanced or metastatic progressive medullary thyroid cancer

(2013) David Viola et al.   Future Oncology

The BCR-ABLT315I mutation compromises survival in chronic phase chronic myelogenous leukemia patients resistant to tyrosine kinase inhibitors, in a matched pair analysis

(2013) F. E. Nicolini et al.   HAEMATOLOGICA

DEF Pocket in p38α Facilitates Substrate Selectivity and Mediates Autophosphorylation

(2013) Netanel Tzarum et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cancer Drugs in the United States: Justum Pretium—The Just Price

(2013) Hagop M. Kantarjian et al.   JOURNAL OF CLINICAL ONCOLOGY

Axitinib in Metastatic Renal Cell Carcinoma: Results of a Pharmacokinetic and Pharmacodynamic Analysis

(2013) Brian I. Rini et al.   JOURNAL OF CLINICAL PHARMACOLOGY

MEK and the inhibitors: from bench to bedside

(2013) Akintunde Akinleye et al.   Journal of Hematology & Oncology

A selective ALK inhibitor in ALK-rearranged patients

(2013) James Chih-Hsin Yang   LANCET ONCOLOGY

The complexity of NF-κB signaling in inflammation and cancer

(2013) Bastian Hoesel et al.   Molecular Cancer

Afatinib Prolongs Survival Compared with Gefitinib in an Epidermal Growth Factor Receptor-Driven Lung Cancer Model

(2013) T. Ninomiya et al.   MOLECULAR CANCER THERAPEUTICS

mTOR kinase structure, mechanism and regulation

(2013) Haijuan Yang et al.   NATURE

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

(2013) Georgia Hatzivassiliou et al.   NATURE

ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

(2013) Sigrun Polier et al.   Nature Chemical Biology

The quest to overcome resistance to EGFR-targeted therapies in cancer

(2013) Curtis R Chong et al.   NATURE MEDICINE

Development of PI3K inhibitors: lessons learned from early clinical trials

(2013) Jordi Rodon et al.   Nature Reviews Clinical Oncology

Drugging cancer genomes

(2013) Paul Workman et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting the sphingosine-1-phosphate axis in cancer, inflammation and beyond

(2013) Gregory T. Kunkel et al.   NATURE REVIEWS DRUG DISCOVERY

Validating therapeutic targets through human genetics

(2013) Robert M. Plenge et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands

(2013) Adam J. Pawson et al.   NUCLEIC ACIDS RESEARCH

Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions

(2013) Alastair J. King et al.   PLoS One

NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors

(2013) L. Skora et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phosphoinositide 3-Kinase   Gene Mutation Predisposes to Respiratory Infection and Airway Damage

(2013) I. Angulo et al.   SCIENCE

Randomized Trial of Everolimus-Facilitated Calcineurin Inhibitor Minimization Over 24 Months in Renal Transplantation

(2013) Diane Cibrik et al.   TRANSPLANTATION

Kinase dysfunction and kinase inhibitors

(2013) Cheryl A. London   VETERINARY DERMATOLOGY

The Genetic Landscape of Clinical Resistance to RAF Inhibition in Metastatic Melanoma

(2013) E. M. Van Allen et al.   Cancer Discovery

Regorafenib: from bench to bedside in colorectal cancer

(2013) Safi Shahda et al.   Expert Review of Clinical Pharmacology

JAK2/STAT5 Inhibition Circumvents Resistance to PI3K/mTOR Blockade: A Rationale for Cotargeting These Pathways in Metastatic Breast Cancer

(2012) Adrian Britschgi et al.   CANCER CELL

Substrate-Selective Inhibition of Protein Kinase PDK1 by Small Compounds that Bind to the PIF-Pocket Allosteric Docking Site

(2012) Katrien Busschots et al.   CHEMISTRY & BIOLOGY

Vandetanib for the Treatment of Medullary Thyroid Cancer

(2012) N. G. Chau et al.   CLINICAL CANCER RESEARCH

Exploiting the anti-inflammatory effects of AMP-activated protein kinase activation

(2012) Ian P Salt et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

(2012) Tadeusz Robak et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Targeting the PI3K signaling pathway in cancer therapy

(2012) Chandra Bartholomeusz et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Complexity in the signaling network: insights from the use of targeted inhibitors in cancer therapy

(2012) J. S. Logue et al.   GENES & DEVELOPMENT

Targeting B-Cell Receptor Signaling for Anticancer Therapy: The Bruton's Tyrosine Kinase Inhibitor Ibrutinib Induces Impressive Responses in B-Cell Malignancies

(2012) Adrian Wiestner   JOURNAL OF CLINICAL ONCOLOGY

Profiling the kinome: Current capabilities and future challenges

(2012) James D.R. Knight et al.   Journal of Proteomics

Omics and therapy - A basis for precision medicine

(2012) Joseph P. Garay et al.   Molecular Oncology

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

(2012) Jordi Barretina et al.   NATURE

A public-private partnership to unlock the untargeted kinome

(2012) Stefan Knapp et al.   Nature Chemical Biology

Natural-product-derived fragments for fragment-based ligand discovery

(2012) Björn Over et al.   Nature Chemistry

Chipping away at the lung cancer genome

(2012) William Pao et al.   NATURE MEDICINE

JAK Inhibition with Ruxolitinib versus Best Available Therapy for Myelofibrosis

(2012) Claire Harrison et al.   NEW ENGLAND JOURNAL OF MEDICINE

Modular evolution of phosphorylation-based signalling systems

(2012) J. Jin et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

An ATP-Site On-Off Switch That Restricts Phosphatase Accessibility of Akt

(2012) K. Lin et al.   Science Signaling

Mechanisms of Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancers

(2012) R. Katayama et al.   Science Translational Medicine

Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

(2012) Rita Andraos et al.   Cancer Discovery

Negative Feedback and Adaptive Resistance to the Targeted Therapy of Cancer

(2012) Sarat Chandarlapaty   Cancer Discovery

Compensatory Pathways in Oncogenic Kinase Signaling and Resistance to Targeted Therapies: Six Degrees of Separation: Figure 1.

(2012) Livio Trusolino et al.   Cancer Discovery

Targeting Diverse Signaling Interaction Sites Allows the Rapid Generation of Bivalent Kinase Inhibitors

(2011) Zachary B. Hill et al.   ACS Chemical Biology

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

A Blueprint for Advancing Genetics-Based Cancer Therapy

(2011) William R. Sellers   CELL

The secret life of kinases: functions beyond catalysis

(2011) Jens Rauch et al.   Cell Communication and Signaling

Allosteric Regulation of Protein Kinase PKCζ by the N-Terminal C1 Domain and Small Compounds to the PIF-Pocket

(2011) Laura A. Lopez-Garcia et al.   CHEMISTRY & BIOLOGY

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases

(2011) Matthew P. Patricelli et al.   CHEMISTRY & BIOLOGY

Discovery and Characterization of a Cell-Permeable, Small-Molecule c-Abl Kinase Activator that Binds to the Myristoyl Binding Site

(2011) Jingsong Yang et al.   CHEMISTRY & BIOLOGY

Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: Therapeutic implications

(2011) M. Sánchez-Martín et al.   INTERNATIONAL JOURNAL OF CANCER

Targeting Energy Metabolic and Oncogenic Signaling Pathways in Triple-negative Breast Cancer by a Novel Adenosine Monophosphate-activated Protein Kinase (AMPK) Activator

(2011) Kuen-Haur Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dissecting Therapeutic Resistance to RAF Inhibition in Melanoma by Tumor Genomic Profiling

(2011) Nikhil Wagle et al.   JOURNAL OF CLINICAL ONCOLOGY

Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms

(2011) Natalia Jura et al.   MOLECULAR CELL

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

(2011) Poulikos I. Poulikakos et al.   NATURE

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

(2011) Theonie Anastassiadis et al.   NATURE BIOTECHNOLOGY

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Crizotinib

(2011) Alice T. Shaw et al.   NATURE REVIEWS DRUG DISCOVERY

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

(2011) José Baselga et al.   NEW ENGLAND JOURNAL OF MEDICINE

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

(2011) V Serra et al.   ONCOGENE

Turning a protein kinase on or off from a single allosteric site via disulfide trapping

(2011) J. D. Sadowsky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Ras-ERK and PI3K-mTOR pathways: cross-talk and compensation

(2011) Michelle C. Mendoza et al.   TRENDS IN BIOCHEMICAL SCIENCES

mTOR Kinase Inhibition Causes Feedback-Dependent Biphasic Regulation of AKT Signaling

(2011) V. S. Rodrik-Outmezguine et al.   Cancer Discovery

Discovery and Characterization of Non-ATP Site Inhibitors of the Mitogen Activated Protein (MAP) Kinases

(2010) Kenneth M. Comess et al.   ACS Chemical Biology

Everolimus in the treatment of renal cell carcinoma and neuroendocrine tumors

(2010) Hiu-yan Chan et al.   ADVANCES IN THERAPY

Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site

(2010) Doriano Fabbro et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Discovery of selective irreversible inhibitors for EGFR-T790M

(2010) Wenjun Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Preexistence and Clonal Selection of MET Amplification in EGFR Mutant NSCLC

(2010) Alexa B. Turke et al.   CANCER CELL

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

Ceramide kinase: The first decade

(2010) Frédéric Bornancin   CELLULAR SIGNALLING

Targeting kinases for the treatment of inflammatory diseases

(2010) Susanne Müller et al.   Expert Opinion on Drug Discovery

Kinase inhibition-related adverse events predicted from in vitro kinome and clinical trial data

(2010) Xinan Yang et al.   JOURNAL OF BIOMEDICAL INFORMATICS

Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents

(2010) Stephen M. Massa et al.   JOURNAL OF CLINICAL INVESTIGATION

The PI3K Pathway As Drug Target in Human Cancer

(2010) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

Binding or Bending: Distinction of Allosteric Abl Kinase Agonists from Antagonists by an NMR-Based Conformational Assay

(2010) Wolfgang Jahnke et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

(2010) Jianming Zhang et al.   NATURE

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

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen et al.   NATURE

The (un)targeted cancer kinome

(2010) Oleg Fedorov et al.   Nature Chemical Biology

The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors

(2010) Taro Kawai et al.   NATURE IMMUNOLOGY

Everolimus for Subependymal Giant-Cell Astrocytomas in Tuberous Sclerosis

(2010) Darcy A. Krueger et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

(2010) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Cyclotraxin-B, the First Highly Potent and Selective TrkB Inhibitor, Has Anxiolytic Properties in Mice

(2010) Maxime Cazorla et al.   PLoS One

Why do Kinase Inhibitors Cause Cardiotoxicity and What can be Done About It?

(2010) Hui Cheng et al.   PROGRESS IN CARDIOVASCULAR DISEASES

Allosteric Protein Kinase Regulation by Pseudokinases: Insights from STRAD

(2010) T. Rajakulendran et al.   Science Signaling

Protein kinases: evolution of dynamic regulatory proteins

(2010) Susan S. Taylor et al.   TRENDS IN BIOCHEMICAL SCIENCES

Allosteric IGF-1R Inhibitors

(2010) Timo Heinrich et al.   ACS Medicinal Chemistry Letters

Characterization of the CHK1 Allosteric Inhibitor Binding Site

(2009) Darin Vanderpool et al.   BIOCHEMISTRY

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction

(2009) Ji Luo et al.   CELL

Structural biology contributions to tyrosine kinase drug discovery

(2009) Sandra W Cowan-Jacob et al.   CURRENT OPINION IN CELL BIOLOGY

Enhancing mTOR-targeted cancer therapy

(2009) Xuerong Wang et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

(2009) Fabio Zuccotto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dissecting Specificity in the Janus Kinases: The Structures of JAK-Specific Inhibitors Complexed to the JAK1 and JAK2 Protein Tyrosine Kinase Domains

(2009) Neal K. Williams et al.   JOURNAL OF MOLECULAR BIOLOGY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1

(2009) Valerie Hindie et al.   Nature Chemical Biology

Inhibitor hijacking of Akt activation

(2009) Tatsuya Okuzumi et al.   Nature Chemical Biology

Factors underlying sensitivity of cancers to small-molecule kinase inhibitors

(2009) Pasi A. Jänne et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting protein kinases in central nervous system disorders

(2009) Laura K. Chico et al.   NATURE REVIEWS DRUG DISCOVERY

Kinase mutations in human disease: interpreting genotype–phenotype relationships

(2009) Piya Lahiry et al.   NATURE REVIEWS GENETICS

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

(2009) E. Zeqiraj et al.   SCIENCE

Cell Signaling in Space and Time: Where Proteins Come Together and When They're Apart

(2009) J. D. Scott et al.   SCIENCE

Is resistance useless? Multidrug resistance and collateral sensitivity

(2009) Matthew D. Hall et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

(2008) Peter J. Tummino et al.   BIOCHEMISTRY

Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

(2008) Antonella Converso et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Beyond the MEK-pocket: Can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?

(2008) Haile Tecle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation

(2008) Panagis Filippakopoulos et al.   CELL

Rethinking Pseudokinases

(2008) Natarajan Kannan et al.   CELL

Acquired resistance to tyrosine kinase inhibitors during cancer therapy

(2008) Jeffrey A Engelman et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Measuring the tyrosine kinase activity: a review of biochemical and cellular assay technologies

(2008) Yong Jia et al.   Expert Opinion on Drug Discovery

The challenge of selecting protein kinase assays for lead discovery optimization

(2008) Haiching Ma et al.   Expert Opinion on Drug Discovery

Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase†

(2008) Brian K. Albrecht et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Peptoid “Antibody Surrogate” That Antagonizes VEGF Receptor 2 Activity

(2008) D. Gomika Udugamasooriya et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

(2008) Jeffrey A Engelman et al.   NATURE MEDICINE

High-throughput kinase profiling as a platform for drug discovery

(2008) David M. Goldstein et al.   NATURE REVIEWS DRUG DISCOVERY

Activation of tyrosine kinases by mutation of the gatekeeper threonine

(2008) Mohammad Azam et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

PI3K pathway alterations in cancer: variations on a theme

(2008) T L Yuan et al.   ONCOGENE

Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity

(2008) M Scaltriti et al.   ONCOGENE

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

(2008) J. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA