Mechanisms of drug resistance in kinases

Targeting mTOR with rapamycin: One dose does not fit all

(2011) David A. Foster et al.   CELL CYCLE

New technologies for autoimmune disease monitoring

(2011) Holden T Maecker et al.   Current Opinion in Endocrinology Diabetes and Obesity

Biochemical Mechanisms of Resistance to Small-Molecule Protein Kinase Inhibitors

(2010) Ratika Krishnamurty et al.   ACS Chemical Biology

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 a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

(2010) E. Weisberg et al.   BLOOD

Molecular pathogenesis of tyrosine kinase resistance in chronic myeloid leukemia

(2010) Paul La Rosée et al.   CURRENT OPINION IN HEMATOLOGY

Epidermal growth factor receptor tyrosine kinase inhibitors as first-line treatment in advanced nonsmall-cell lung cancer

(2010) Rafael Rosell et al.   CURRENT OPINION IN ONCOLOGY

Targeted therapies for advanced thyroid cancer

(2010) Efisio Puxeddu et al.   CURRENT OPINION IN ONCOLOGY

Standard treatment of Ph+ CML in 2010: how, when and where not to use what BCR/ABL1 kinase inhibitor?

(2010) Peter Valent   EUROPEAN JOURNAL OF CLINICAL INVESTIGATION

CYP3A activity influences imatinib response in patients with chronic myeloid leukemia: a pilot study on in vivo CYP3A activity

(2010) Henrik Gréen et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Potent, transient inhibition of BCR-ABL with dasatinib 100 mg daily achieves rapid and durable cytogenetic responses and high transformation-free survival rates in chronic phase chronic myeloid leukemia patients with resistance, suboptimal response or intolerance to imatinib

(2010) N. P. Shah et al.   HAEMATOLOGICA

A Type-II Kinase Inhibitor Capable of Inhibiting the T315I “Gatekeeper” Mutant of Bcr-Abl

(2010) Hwan Geun Choi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors of phosphatidylinositol-3-kinase in cancer therapy

(2010) Nathan T. Ihle et al.   MOLECULAR ASPECTS OF MEDICINE

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

(2010) Jianming Zhang et al.   NATURE

Kinase inhibitors attract attention as oral rheumatoid arthritis drugs

(2010) Alisa Opar   NATURE REVIEWS DRUG DISCOVERY

Multifaceted polo-like kinases: drug targets and antitargets for cancer therapy

(2010) Klaus Strebhardt   NATURE REVIEWS DRUG DISCOVERY

Integrating molecular diagnostics into anticancer drug discovery

(2010) István Peták et al.   NATURE REVIEWS DRUG DISCOVERY

Computational solutions to large-scale data management and analysis

(2010) Eric E. Schadt et al.   NATURE REVIEWS GENETICS

Non-ATP competitive protein kinase inhibitors as anti-tumor therapeutics

(2009) Lindsay O. Kirkland et al.   BIOCHEMICAL PHARMACOLOGY

Acute dasatinib exposure commits Bcr-Abl-dependent cells to apoptosis

(2009) J. L. Snead et al.   BLOOD

FMS-Like Tyrosine Kinase 3-Internal Tandem Duplication Tyrosine Kinase Inhibitors Display a Nonoverlapping Profile of Resistance Mutations In vitro

(2009) N. von Bubnoff et al.   CANCER RESEARCH

Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

(2009) M. A. Seeliger et al.   CANCER RESEARCH

Clinical pharmacokinetics of tyrosine kinase inhibitors

(2009) Nielka P. van Erp et al.   CANCER TREATMENT REVIEWS

Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small-Cell Lung Cancers Dependent on the Epidermal Growth Factor Receptor Pathway

(2009) Kim-Son H. Nguyen et al.   Clinical Lung Cancer

Aurora kinase inhibitors

(2009) J.J.E.M. Kitzen et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Kinome signaling through regulated protein–protein interactions in normal and cancer cells

(2009) Tony Pawson et al.   CURRENT OPINION IN CELL BIOLOGY

The road less traveled: modulating signal transduction enzymes by inhibiting their protein–protein interactions

(2009) Michelle R Arkin et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Kinase Inhibitors as Potential Therapeutics for Acute and Chronic Neurodegenerative Conditions

(2009) G. Cuny   CURRENT PHARMACEUTICAL DESIGN

Mechanisms of resistance to FLT3 inhibitors

(2009) S. Haihua Chu et al.   DRUG RESISTANCE UPDATES

Ruboxistaurin: PKC-β inhibition for complications of diabetes

(2009) Ronald P Danis et al.   EXPERT OPINION ON PHARMACOTHERAPY

Hybrid Compound Design To Overcome the Gatekeeper T338M Mutation in cSrc#

(2009) Matthäus Getlik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Microfluidic single cell arrays to interrogate signalling dynamics of individual, patient-derived hematopoietic stem cells

(2009) Shannon L. Faley et al.   LAB ON A CHIP

FIP1L1-PDGFRα D842V, a novel panresistant mutant, emerging after treatment of FIP1L1-PDGFRα T674I eosinophilic leukemia with single agent sorafenib

(2009) E Lierman et al.   LEUKEMIA

Triptolide induces cell death independent of cellular responses to imatinib in blast crisis chronic myelogenous leukemia cells including quiescent CD34+ primitive progenitor cells

(2009) D. H. Mak et al.   MOLECULAR CANCER THERAPEUTICS

A Conserved Salt Bridge in the G Loop of Multiple Protein Kinases Is Important for Catalysis and for In Vivo Lyn Function

(2009) Rina Barouch-Bentov et al.   MOLECULAR CELL

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

A new screening assay for allosteric inhibitors of cSrc

(2009) Jeffrey R Simard et al.   Nature Chemical Biology

Selectivity and therapeutic inhibition of kinases: to be or not to be?

(2009) Kamran Ghoreschi et al.   NATURE IMMUNOLOGY

Somatic EGFR mutations and efficacy of tyrosine kinase inhibitors in NSCLC

(2009) Helena Linardou et al.   Nature Reviews Clinical Oncology

Imatinib and beyond—exploring the full potential of targeted therapy for CML

(2009) Alfonso Quintás-Cardama et al.   Nature Reviews Clinical Oncology

Factors underlying sensitivity of cancers to small-molecule kinase inhibitors

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

Cell cycle kinases as therapeutic targets for cancer

(2009) Silvia Lapenna et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting innate immunity protein kinase signalling in inflammation

(2009) Matthias Gaestel et al.   NATURE REVIEWS DRUG DISCOVERY

Kinase mutations in human disease: interpreting genotype–phenotype relationships

(2009) Piya Lahiry et al.   NATURE REVIEWS GENETICS

Anticipating drug resistance in the MAP kinase pathway

(2009) Ronen Marmorstein   Pigment Cell & Melanoma Research

Conformational disturbance in Abl kinase upon mutation and deregulation

(2009) R. E. Iacob et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MEK1 mutations confer resistance to MEK and B-RAF inhibition

(2009) C. M. Emery et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients

(2009) K. S. Gajiwala et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein kinase inhibitors: contributions from structure to clinical compounds

(2009) Louise N. Johnson   QUARTERLY REVIEWS OF BIOPHYSICS

Mechanisms of resistance to tyrosine kinase inhibitors in chronic myeloid leukemia and recent therapeutic strategies to overcome resistance

(2009) D. Bixby et al.   Hematology-American Society of Hematology Education Program

Structure-Based View of Epidermal Growth Factor Receptor Regulation

(2008) Kathryn M. Ferguson   Annual Review of Biophysics

Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations

(2008) Egle Avizienyte et al.   BIOCHEMICAL JOURNAL

Molecular basis explanation for imatinib resistance of BCR-ABL due to T315I and P-loop mutations from molecular dynamics simulations

(2008) Tai-Sung Lee et al.   CANCER

Discovery of Drug-Resistant and Drug-Sensitizing Mutations in the Oncogenic PI3K Isoform p110α

(2008) Eli R. Zunder et al.   CANCER CELL

Palomid 529, a Novel Small-Molecule Drug, Is a TORC1/TORC2 Inhibitor That Reduces Tumor Growth, Tumor Angiogenesis, and Vascular Permeability

(2008) Q. Xue et al.   CANCER RESEARCH

Hepatocyte Growth Factor Induces Gefitinib Resistance of Lung Adenocarcinoma with Epidermal Growth Factor Receptor-Activating Mutations

(2008) S. Yano et al.   CANCER RESEARCH

Secondary mutations in the kinase domain of the KIT gene are predominant in imatinib-resistant gastrointestinal stromal tumor

(2008) Toshirou Nishida et al.   CANCER SCIENCE

Structure and dynamic regulation of Src-family kinases

(2008) J. R. Engen et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Molecular Basis of Drug Resistance in Aurora Kinases

(2008) Fiona Girdler et al.   CHEMISTRY & BIOLOGY

Acquired Resistance to Epidermal Growth Factor Receptor Kinase Inhibitors Associated with a Novel T854A Mutation in a Patient with EGFR-Mutant Lung Adenocarcinoma

(2008) J. Bean et al.   CLINICAL CANCER RESEARCH

EXEL-7647 Inhibits Mutant Forms of ErbB2 Associated with Lapatinib Resistance and Neoplastic Transformation

(2008) T. Trowe et al.   CLINICAL CANCER RESEARCH

Doing more than just the structure—structural genomics in kinase drug discovery

(2008) Brian D Marsden et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Acquired resistance to tyrosine kinase inhibitors during cancer therapy

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

Therapeutic strategies for inhibiting oncogenic BRAF signaling

(2008) Ensar Halilovic et al.   CURRENT OPINION IN PHARMACOLOGY

Kinase inhibitors as drugs for chronic inflammatory and immunological diseases: progress and challenges

(2008) Laura L Rokosz et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Clinical significance of oncogenicKITandPDGFRAmutations in gastrointestinal stromal tumours

(2008) J Lasota et al.   HISTOPATHOLOGY

T-Cell–Targeted Signaling Inhibitors

(2008) Jonghwa Won et al.   INTERNATIONAL REVIEWS OF IMMUNOLOGY

Solution Conformations and Dynamics of ABL Kinase-Inhibitor Complexes Determined by NMR Substantiate the Different Binding Modes of Imatinib/Nilotinib and Dasatinib

(2008) Navratna Vajpai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Primary and Secondary Kinase Genotypes Correlate With the Biological and Clinical Activity of Sunitinib in Imatinib-Resistant Gastrointestinal Stromal Tumor

(2008) Michael C. Heinrich et al.   JOURNAL OF CLINICAL ONCOLOGY

Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants

(2008) Sara Redaelli et al.   JOURNAL OF CLINICAL ONCOLOGY

BCR-ABL mutants spread resistance to non-mutated cells through a paracrine mechanism

(2008) J Liu et al.   LEUKEMIA

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

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

Disruption of the EGFR E884–R958 ion pair conserved in the human kinome differentially alters signaling and inhibitor sensitivity

(2008) Z Tang et al.   ONCOGENE

Commentary: Novel Therapies for Cancer: Why Dirty Might Be Better

(2008) T. Fojo   ONCOLOGIST

A conserved protonation-dependent switch controls drug binding in the Abl kinase

(2008) Y. Shan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Overcoming kinase resistance in chronic myeloid leukemia

(2007) Francis Lee et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY