Mechanisms of acquired resistance to targeted cancer therapies

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

(2015) Ryan B. Corcoran et al.   Oncotarget

Slug and Sox9 Cooperatively Determine the Mammary Stem Cell State

(2012) Wenjun Guo et al.   CELL

ERK Inhibition Overcomes Acquired Resistance to MEK Inhibitors

(2012) G. Hatzivassiliou et al.   MOLECULAR CANCER THERAPEUTICS

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

(2012) Anirudh Prahallad et al.   NATURE

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

Antitumour efficacy of MEK inhibitors in human lung cancer cells and their derivatives with acquired resistance to different tyrosine kinase inhibitors

(2011) F Morgillo et al.   BRITISH JOURNAL OF CANCER

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

(2011) Sarat Chandarlapaty et al.   CANCER CELL

Cell Autonomous Role of PTEN in Regulating Castration-Resistant Prostate Cancer Growth

(2011) David J. Mulholland et al.   CANCER CELL

Reciprocal Feedback Regulation of PI3K and Androgen Receptor Signaling in PTEN-Deficient Prostate Cancer

(2011) Brett S. Carver et al.   CANCER CELL

A Novel ALK Secondary Mutation and EGFR Signaling Cause Resistance to ALK Kinase Inhibitors

(2011) T. Sasaki et al.   CANCER RESEARCH

Identification of the MEK1(F129L) Activating Mutation as a Potential Mechanism of Acquired Resistance to MEK Inhibition in Human Cancers Carrying the B-RafV600E Mutation

(2011) H. Wang et al.   CANCER RESEARCH

Androgen Deprivation Causes Epithelial-Mesenchymal Transition in the Prostate: Implications for Androgen-Deprivation Therapy

(2011) Y. Sun et al.   CANCER RESEARCH

A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients

(2011) R. Tiedt et al.   CANCER RESEARCH

Multiple Mutations and Bypass Mechanisms Can Contribute to Development of Acquired Resistance to MET Inhibitors

(2011) J. Qi et al.   CANCER RESEARCH

p95HER2 and Breast Cancer

(2011) J. Arribas et al.   CANCER RESEARCH

A Kinome-Wide Screen Identifies the Insulin/IGF-I Receptor Pathway as a Mechanism of Escape from Hormone Dependence in Breast Cancer

(2011) E. M. Fox et al.   CANCER RESEARCH

Crizotinib-Resistant Mutants of EML4-ALK Identified Through an Accelerated Mutagenesis Screen

(2011) Sen Zhang et al.   Chemical Biology & Drug Design

Phase I Trial of Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) in Patients with Refractory, Locally Advanced or Metastatic Solid Tumors

(2011) P. M. LoRusso et al.   CLINICAL CANCER RESEARCH

Trastuzumab Emtansine: A Unique Antibody-Drug Conjugate in Development for Human Epidermal Growth Factor Receptor 2-Positive Cancer

(2011) P. M. LoRusso et al.   CLINICAL CANCER RESEARCH

Alternatively spliced androgen receptor variants

(2011) Scott M Dehm et al.   ENDOCRINE-RELATED CANCER

Phenotypic plasticity and epithelial-mesenchymal transitions in cancer and normal stem cells?

(2011) Christina Scheel et al.   INTERNATIONAL JOURNAL OF CANCER

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

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

Phosphatidylinositol 3-Kinase and Antiestrogen Resistance in Breast Cancer

(2011) Todd W. Miller et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of a Novel B-Raf Fusion Protein Related to c-Met Drug Resistance

(2011) Roslyn Dillon et al.   JOURNAL OF PROTEOME RESEARCH

Epithelial to Mesenchymal Transition in an Epidermal Growth Factor Receptor-Mutant Lung Cancer Cell Line with Acquired Resistance to Erlotinib

(2011) Kenichi Suda et al.   Journal of Thoracic Oncology

Antitumor Activity of the Hsp90 Inhibitor IPI-504 in HER2-Positive Trastuzumab-Resistant Breast Cancer

(2011) M. Scaltriti et al.   MOLECULAR CANCER THERAPEUTICS

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

(2011) Poulikos I. Poulikakos et al.   NATURE

A chemical-genetic screen reveals a mechanism of resistance to PI3K inhibitors in cancer

(2011) Markus K Muellner et al.   Nature Chemical Biology

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway–dependent and PI3K pathway–independent mechanisms

(2011) Pixu Liu et al.   NATURE MEDICINE

Combating trastuzumab resistance by targeting SRC, a common node downstream of multiple resistance pathways

(2011) Siyuan Zhang et al.   NATURE MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

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

PI3K-targeted therapy can be evaded by gene amplification along the MYC-eukaryotic translation initiation factor 4E (eIF4E) axis

(2011) N. Ilic et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK

(2011) R. Katayama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cyclin E amplification/overexpression is a mechanism of trastuzumab resistance in HER2+breast cancer patients

(2011) Maurizio Scaltriti et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors

(2011) A. Chakrabarty et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Normal and neoplastic nonstem cells can spontaneously convert to a stem-like state

(2011) C. L. Chaffer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Amplification of the Driving Oncogene, KRAS or BRAF, Underpins Acquired Resistance to MEK1/2 Inhibitors in Colorectal Cancer Cells

(2011) A. S. Little et al.   Science Signaling

Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors

(2011) L. V. Sequist et al.   Science Translational Medicine

Overexpression of P-glycoprotein induces acquired resistance to imatinib in chronic myelogenous leukemia cells

(2011) Xing-Xiang Peng et al.   Chinese Journal of Cancer

c-MET as a potential therapeutic target and biomarker in cancer

(2011) J. Rafael Sierra et al.   Therapeutic Advances in Medical Oncology

Trastuzumab-DM1 (T-DM1) retains all the mechanisms of action of trastuzumab and efficiently inhibits growth of lapatinib insensitive breast cancer

(2010) Teemu T. Junttila et al.   BREAST CANCER RESEARCH AND TREATMENT

Phenotypic Heterogeneity among Tumorigenic Melanoma Cells from Patients that Is Reversible and Not Hierarchically Organized

(2010) Elsa Quintana et al.   CANCER CELL

Preexistence and Clonal Selection of MET Amplification in EGFR Mutant NSCLC

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

Acquired Resistance to BRAF Inhibitors Mediated by a RAF Kinase Switch in Melanoma Can Be Overcome by Cotargeting MEK and IGF-1R/PI3K

(2010) Jessie Villanueva et al.   CANCER CELL

The Neuroblastoma-Associated F1174L ALK Mutation Causes Resistance to an ALK Kinase Inhibitor in ALK-Translocated Cancers

(2010) T. Sasaki et al.   CANCER RESEARCH

Acquired Resistance of Non-Small Cell Lung Cancer Cells to MET Kinase Inhibition Is Mediated by a Switch to Epidermal Growth Factor Receptor Dependency

(2010) U. McDermott et al.   CANCER RESEARCH

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

(2010) Gerrit J. P. Dijkgraaf et al.   CANCER RESEARCH

A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations

(2010) Sreenath V. Sharma et al.   CELL

A Temporarily Distinct Subpopulation of Slow-Cycling Melanoma Cells Is Required for Continuous Tumor Growth

(2010) Alexander Roesch et al.   CELL

Clinical Benefit of Lapatinib-Based Therapy in Patients with Human Epidermal Growth Factor Receptor 2-Positive Breast Tumors Coexpressing the Truncated p95HER2 Receptor

(2010) M. Scaltriti et al.   CLINICAL CANCER RESEARCH

Quantitation of p95HER2 in Paraffin Sections by Using a p95-Specific Antibody and Correlation with Outcome in a Cohort of Trastuzumab-Treated Breast Cancer Patients

(2010) J. Sperinde et al.   CLINICAL CANCER RESEARCH

Mutation-driven drug development in melanoma

(2010) Keith T Flaherty et al.   CURRENT OPINION IN ONCOLOGY

Function of activation loop tyrosine phosphorylation in the mechanism of c-Kit auto-activation and its implication in sunitinib resistance

(2010) J. P. DiNitto et al.   JOURNAL OF BIOCHEMISTRY

Hyperactivation of phosphatidylinositol-3 kinase promotes escape from hormone dependence in estrogen receptor–positive human breast cancer

(2010) Todd W. Miller et al.   JOURNAL OF CLINICAL INVESTIGATION

Activity of IPI-504, a Novel Heat-Shock Protein 90 Inhibitor, in Patients With Molecularly Defined Non–Small-Cell Lung Cancer

(2010) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Epithelial Mesenchymal Transition Traits in Human Breast Cancer Cell Lines Parallel the CD44hi/CD24lo/- Stem Cell Phenotype in Human Breast Cancer

(2010) Tony Blick et al.   JOURNAL OF MAMMARY GLAND BIOLOGY AND NEOPLASIA

Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs

(2010) Jin-Haeng Chung et al.   LUNG CANCER

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen et al.   NATURE

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

(2010) Ramin Nazarian et al.   NATURE

EML4-ALK Mutations in Lung Cancer That Confer Resistance to ALK Inhibitors

(2010) Young Lim Choi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor

(2010) D Ercan et al.   ONCOGENE

EMT, cancer stem cells and drug resistance: an emerging axis of evil in the war on cancer

(2010) A Singh et al.   ONCOGENE

BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation

(2010) R. B. Corcoran et al.   Science Signaling

Akt-RSK-S6 Kinase Signaling Networks Activated by Oncogenic Receptor Tyrosine Kinases

(2010) A. Moritz et al.   Science Signaling

Gatekeeper Mutations Mediate Resistance to BRAF-Targeted Therapies

(2010) S. Whittaker et al.   Science Translational Medicine

Interfering with Resistance to Smoothened Antagonists by Inhibition of the PI3K Pathway in Medulloblastoma

(2010) S. Buonamici et al.   Science Translational Medicine

Reactivation of Androgen Receptor-Regulated TMPRSS2:ERG Gene Expression in Castration-Resistant Prostate Cancer

(2009) C. Cai et al.   CANCER RESEARCH

Loss of Phosphatase and Tensin Homologue Deleted on Chromosome 10 Engages ErbB3 and Insulin-Like Growth Factor-I Receptor Signaling to Promote Antiestrogen Resistance in Breast Cancer

(2009) T. W. Miller et al.   CANCER RESEARCH

PIK3CA and PIK3CB Inhibition Produce Synthetic Lethality when Combined with Estrogen Deprivation in Estrogen Receptor-Positive Breast Cancer

(2009) R. J. Crowder et al.   CANCER RESEARCH

Novel Mechanism of Lapatinib Resistance in HER2-Positive Breast Tumor Cells: Activation of AXL

(2009) L. Liu et al.   CANCER RESEARCH

PTEN Loss Contributes to Erlotinib Resistance in EGFR-Mutant Lung Cancer by Activation of Akt and EGFR

(2009) M. L. Sos et al.   CANCER RESEARCH

Identification of Selective Inhibitors of Cancer Stem Cells by High-Throughput Screening

(2009) Piyush B. Gupta et al.   CELL

Inhibition of PI3K and MEK: It Is All about Combinations and Biomarkers

(2009) B. N. Rexer et al.   CLINICAL CANCER RESEARCH

Clinical Features and Outcome of Patients With Non–Small-Cell Lung Cancer Who Harbor EML4-ALK

(2009) Alice T. Shaw et al.   JOURNAL OF CLINICAL ONCOLOGY

Understanding the Mechanisms Behind Trastuzumab Therapy for Human Epidermal Growth Factor Receptor 2–Positive Breast Cancer

(2009) Neil L. Spector et al.   JOURNAL OF CLINICAL ONCOLOGY

Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy

(2009) N. T. Ihle et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of focal adhesion kinase as a potential therapeutic strategy for imatinib-resistant gastrointestinal stromal tumor

(2009) K. Sakurama et al.   MOLECULAR CANCER THERAPEUTICS

Screening for Epidermal Growth Factor Receptor Mutations in Lung Cancer

(2009) Rafael Rosell et al.   NEW ENGLAND JOURNAL OF MEDICINE

Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449

(2009) Charles M. Rudin et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Smoothened Mutation Confers Resistance to a Hedgehog Pathway Inhibitor in Medulloblastoma

(2009) R. L. Yauch et al.   SCIENCE

The androgen receptor can signal through Wnt/β-Catenin in prostate cancer cells as an adaptation mechanism to castration levels of androgens

(2008) Liang Schweizer et al.   BMC CELL BIOLOGY

Evidence that Resistance to Nilotinib May Be Due to BCR-ABL, Pgp, or Src Kinase Overexpression

(2008) F.-X. Mahon et al.   CANCER RESEARCH

Elevated CRAF as a Potential Mechanism of Acquired Resistance to BRAF Inhibition in Melanoma

(2008) C. Montagut et al.   CANCER RESEARCH

The Epithelial-Mesenchymal Transition Generates Cells with Properties of Stem Cells

(2008) Sendurai A. Mani et al.   CELL

Acquired resistance to tyrosine kinase inhibitors during cancer therapy

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

Targeting the androgen receptor pathway in prostate cancer

(2008) Yu Chen et al.   CURRENT OPINION IN PHARMACOLOGY

Correlation of Kinase Genotype and Clinical Outcome in the North American Intergroup Phase III Trial of Imatinib Mesylate for Treatment of Advanced Gastrointestinal Stromal Tumor: CALGB 150105 Study by Cancer and Leukemia Group B and Southwest Oncology Group

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

Intrinsic Resistance of Tumorigenic Breast Cancer Cells to Chemotherapy

(2008) X. Li et al.   JNCI-Journal of the National Cancer Institute

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

FDA Drug Approval Summary: Lapatinib in Combination with Capecitabine for Previously Treated Metastatic Breast Cancer That Overexpresses HER-2

(2008) Q. Ryan et al.   ONCOLOGIST

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

The role of hormonal therapy in the management of hormonal-receptor-positive breast cancer with co-expression of HER2

(2008) Aleix Prat et al.   Nature clinical practice. Oncology