Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors

PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer

(2017) Mathilde Guerin et al.   EUROPEAN JOURNAL OF CANCER

Durable Control of Metastatic AKT1-Mutant WHO Grade 1 Meningothelial Meningioma by the AKT Inhibitor, AZD5363

(2017) Michael Weller et al.   JNCI-Journal of the National Cancer Institute

PLX8394, a new generation BRAF inhibitor, selectively inhibits BRAF in colonic adenocarcinoma cells and prevents paradoxical MAPK pathway activation

(2017) Candani S. A. Tutuka et al.   Molecular Cancer

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors

(2017) Dejan Juric et al.   Cancer Discovery

Durable Control of Metastatic AKT1-Mutant WHO Grade 1 Meningothelial Meningioma by the AKT Inhibitor, AZD5363

(2017) Michael Weller et al.   JNCI-Journal of the National Cancer Institute

Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen

(2017) I-Chun Chen et al.   Scientific Reports

First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas

(2016) A. Patnaik et al.   ANNALS OF ONCOLOGY

Coadministration of Trametinib and Palbociclib Radiosensitizes KRAS-Mutant Non-Small Cell Lung Cancers In Vitro and In Vivo

(2016) Z. Tao et al.   CLINICAL CANCER RESEARCH

Targeting mTOR pathway in gynecological malignancies: Biological rationale and systematic review of published data

(2016) Loay Kassem et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Treatment strategies for advanced hormone receptor-positive and human epidermal growth factor 2-negative breast cancer: the role of treatment order

(2016) Edith A. Perez   DRUG RESISTANCE UPDATES

New and developing chemical pharmacotherapy for treating hormone receptor-positive/HER2-negative breast cancer

(2016) Rossella Martinello et al.   EXPERT OPINION ON PHARMACOTHERAPY

Afatinib Activity in Platinum-Refractory Metastatic Urothelial Carcinoma in Patients With ERBB Alterations

(2016) Noura J. Choudhury et al.   JOURNAL OF CLINICAL ONCOLOGY

Second- and third-generation ALK inhibitors for non-small cell lung cancer

(2016) Jingjing Wu et al.   Journal of Hematology & Oncology

Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer

(2016) Shuhang Wang et al.   Journal of Hematology & Oncology

LBA1_PR: Osimertinib as first-line treatment for EGFR mutation-positive advanced NSCLC: updated efficacy and safety results from two Phase I expansion cohorts

(2016) S. Ramalingam et al.   Journal of Thoracic Oncology

Antiangiogenic therapy in oncology: current status and future directions

(2016) Gordon C Jayson et al.   LANCET

RET inhibitors for patients with RET fusion-positive and RET wild-type non-small-cell lung cancer

(2016) Rafael Rosell et al.   LANCET ONCOLOGY

Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial

(2016) Joel W Neal et al.   LANCET ONCOLOGY

Cobimetinib combined with vemurafenib in advanced BRAFV600-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial

(2016) Paolo A Ascierto et al.   LANCET ONCOLOGY

Alectinib in ALK -positive, crizotinib-resistant, non-small-cell lung cancer: a single-group, multicentre, phase 2 trial

(2016) Alice T Shaw et al.   LANCET ONCOLOGY

Dabrafenib plus trametinib in patients with previously treated BRAF V600E -mutant metastatic non-small cell lung cancer: an open-label, multicentre phase 2 trial

(2016) David Planchard et al.   LANCET ONCOLOGY

Ten years of anti-vascular endothelial growth factor therapy

(2016) Napoleone Ferrara et al.   NATURE REVIEWS DRUG DISCOVERY

A novel AKT inhibitor, AZD5363, inhibits phosphorylation of AKT downstream molecules, and activates phosphorylation of mTOR and SMG-1 dependent on the liver cancer cell type

(2016) YUNCHENG ZHANG et al.   Oncology Letters

Cabozantinib in the treatment of advanced renal cell carcinoma: design, development, and potential place in the therapy

(2016) Giuseppe Procopio et al.   Drug Design Development and Therapy

LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer

(2016) Eliza Vakana et al.   Oncotarget

Oncogenic BRAF-Mediated Melanoma Cell Invasion

(2016) Hezhe Lu et al.   Cell Reports

Mechanisms of resistance to third-generation EGFR tyrosine kinase inhibitors

(2016) Shuhang Wang et al.   Frontiers of Medicine

Imatinib and Nilotinib increase glioblastoma cell invasion via Abl-independent stimulation of p130Cas and FAK signalling

(2016) Antonina Frolov et al.   Scientific Reports

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers

(2015) Sheng-Bin Peng et al.   CANCER CELL

Platelet-derived growth factor (PDGF) signalling in cancer: rapidly emerging signalling landscape

(2015) Ammad Ahmad Farooqi et al.   CELL BIOCHEMISTRY AND FUNCTION

PD-L1 Expression and Tumor-Infiltrating Lymphocytes Define Different Subsets of MAPK Inhibitor-Treated Melanoma Patients

(2015) H. Kakavand et al.   CLINICAL CANCER RESEARCH

RAS/MAPK Activation Is Associated with Reduced Tumor-Infiltrating Lymphocytes in Triple-Negative Breast Cancer: Therapeutic Cooperation Between MEK and PD-1/PD-L1 Immune Checkpoint Inhibitors

(2015) S. Loi et al.   CLINICAL CANCER RESEARCH

Cobimetinib: First Global Approval

(2015) Karly P. Garnock-Jones   DRUGS

High Efficacy of Combination Therapy Using PI3K/AKT Inhibitors with Androgen Deprivation in Prostate Cancer Preclinical Models

(2015) Rute B. Marques et al.   EUROPEAN UROLOGY

The discovery and development of sorafenib for the treatment of thyroid cancer

(2015) Peter T White et al.   Expert Opinion on Drug Discovery

MEK + CDK4 a regimen for non-BRAF V6000 melanoma

(2015) Jeff Sosman   Journal of Translational Medicine

Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial

(2015) Georgina V Long et al.   LANCET

AKT Antagonist AZD5363 Influences Estrogen Receptor Function in Endocrine-Resistant Breast Cancer and Synergizes with Fulvestrant (ICI182780) In Vivo

(2015) R. Ribas et al.   MOLECULAR CANCER THERAPEUTICS

Minireview: Were the IGF Signaling Inhibitors All Bad?

(2015) Heather Beckwith et al.   MOLECULAR ENDOCRINOLOGY

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

Improved Overall Survival in Melanoma with Combined Dabrafenib and Trametinib

(2015) Caroline Robert et al.   NEW ENGLAND JOURNAL OF MEDICINE

AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer

(2015) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

Improved antitumor activity of immunotherapy with BRAF and MEK inhibitors in BRAF V600E melanoma

(2015) Siwen Hu-Lieskovan et al.   Science Translational Medicine

Increased CD271 expression by the NF-kB pathway promotes melanoma cell survival and drives acquired resistance to BRAF inhibitor vemurafenib

(2015) Abdelali Lehraiki et al.   Cell Discovery

Trametinib with or without Vemurafenib in BRAF Mutated Non-Small Cell Lung Cancer

(2015) Monika Joshi et al.   PLoS One

Mutations and Deregulation of Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR Cascades

(2015) James Andrew McCubrey et al.   Oncotarget

BRAF vs RAS oncogenes: Are mutations of the same pathway equal? Differential signalling and therapeutic implications

(2015) Eftychia Oikonomou et al.   Oncotarget

Pharmacodynamic Characterization of the Efficacy Signals Due to Selective BRAF Inhibition with PLX4032 in Malignant Melanoma

(2015) William D. Tap et al.   NEOPLASIA

Integrated Genomic Characterization of Papillary Thyroid Carcinoma

(2014) Nishant Agrawal et al.   CELL

Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion-Positive Cancer

(2014) R. Katayama et al.   CLINICAL CANCER RESEARCH

Panitumumab versus cetuximab in patients with chemotherapy-refractory wild-type KRAS exon 2 metastatic colorectal cancer (ASPECCT): a randomised, multicentre, open-label, non-inferiority phase 3 study

(2014) Timothy J Price et al.   LANCET ONCOLOGY

Safety and efficacy of vemurafenib in BRAFV600E and BRAFV600K mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study

(2014) Grant A McArthur et al.   LANCET ONCOLOGY

The Capable ABL: What Is Its Biological Function?

(2014) J. Y. J. Wang   MOLECULAR AND CELLULAR BIOLOGY

Genomic classification of the RAS network identifies a personalized treatment strategy for lung cancer

(2014) Nader N. El-Chaar et al.   Molecular Oncology

Combined BRAF and MEK Inhibition versus BRAF Inhibition Alone in Melanoma

(2014) Georgina V. Long et al.   NEW ENGLAND JOURNAL OF MEDICINE

Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma

(2014) James Larkin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Nilotinib is associated with a reduced incidence of BCR-ABL mutations vs imatinib in patients with newly diagnosed chronic myeloid leukemia in chronic phase

(2013) A. Hochhaus et al.   BLOOD

Trametinib: First Global Approval

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

Targeting the RAS oncogene

(2013) Asami Takashima et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Pertuzumab, trastuzumab, and docetaxel for HER2-positive metastatic breast cancer (CLEOPATRA study): overall survival results from a randomised, double-blind, placebo-controlled, phase 3 study

(2013) Sandra M Swain et al.   LANCET ONCOLOGY

MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study

(2013) Paolo A Ascierto et al.   LANCET ONCOLOGY

PDGFRA alterations in cancer: characterization of a gain-of-function V536E transmembrane mutant as well as loss-of-function and passenger mutations

(2013) A I Velghe et al.   ONCOGENE

BCL2A1is a lineage-specific antiapoptotic melanoma oncogene that confers resistance to BRAF inhibition

(2013) Rizwan Haq et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Response to Cabozantinib in Patients with RET Fusion-Positive Lung Adenocarcinomas

(2013) Alexander Drilon et al.   Cancer Discovery

Vessel co-option in primary human tumors and metastases: an obstacle to effective anti-angiogenic treatment?

(2013) Tom Donnem et al.   Cancer Medicine

Epidermal growth factor receptor (EGFR) inhibitors and derived treatments

(2012) R. Dziadziuszko et al.   ANNALS OF ONCOLOGY

A Comprehensive Survey of Ras Mutations in Cancer

(2012) I. A. Prior et al.   CANCER RESEARCH

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial

(2012) José Baselga et al.   LANCET

Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial

(2012) Axel Hauschild et al.   LANCET

Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial

(2012) George D Demetri et al.   LANCET

Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial

(2012) James Chih-Hsin Yang et al.   LANCET ONCOLOGY

Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial

(2012) Rafael Rosell et al.   LANCET ONCOLOGY

Oncogenic NRAS signaling differentially regulates survival and proliferation in melanoma

(2012) Lawrence N Kwong et al.   NATURE MEDICINE

RASMutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors

(2012) Fei Su et al.   NEW ENGLAND JOURNAL OF MEDICINE

Dasatinib or imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: 2-year follow-up from a randomized phase 3 trial (DASISION)

(2011) H. M. Kantarjian et al.   BLOOD

c-Raf, but Not B-Raf, Is Essential for Development of K-Ras Oncogene-Driven Non-Small Cell Lung Carcinoma

(2011) Rafael B. Blasco et al.   CANCER CELL

EGFR Exon 19 Insertions: A New Family of Sensitizing EGFR Mutations in Lung Adenocarcinoma

(2011) M. He et al.   CLINICAL CANCER RESEARCH

Sorafenib-induced premalignant and malignant skin lesions

(2011) Victoria L. Williams et al.   INTERNATIONAL JOURNAL OF DERMATOLOGY

Biomarker Analyses and Final Overall Survival Results From a Phase III, Randomized, Open-Label, First-Line Study of Gefitinib Versus Carboplatin/Paclitaxel in Clinically Selected Patients With Advanced Non–Small-Cell Lung Cancer in Asia (IPASS)

(2011) Masahiro Fukuoka et al.   JOURNAL OF CLINICAL ONCOLOGY

Long-Term Androgen Ablation and Docetaxel Up-Regulate Phosphorylated Akt in Castration Resistant Prostate Cancer

(2011) Takeo Kosaka et al.   JOURNAL OF UROLOGY

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

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

C-Raf Is Required for the Initiation of Lung Cancer by K-Ras G12D

(2011) Florian A. Karreth et al.   Cancer Discovery

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

(2010) Tianjun Zhou et al.   Chemical Biology & Drug Design

Genetic analysis of Ras signalling pathways in cell proliferation, migration and survival

(2010) Matthias Drosten et al.   EMBO JOURNAL

Sorafenib: a clinical and pharmacologic review

(2010) Renuka Iyer et al.   EXPERT OPINION ON PHARMACOTHERAPY

Dermatofibrosarcoma protuberans-derived fibrosarcoma: Clinical history, biological profile and sensitivity to imatinib

(2010) Silvia Stacchiotti et al.   INTERNATIONAL JOURNAL OF CANCER

Trastuzumab in combination with chemotherapy versus chemotherapy alone for treatment of HER2-positive advanced gastric or gastro-oesophageal junction cancer (ToGA): a phase 3, open-label, randomised controlled trial

(2010) Yung-Jue Bang et al.   LANCET

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

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

(2010) E. W. Joseph et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oncogenic Braf Induces Melanocyte Senescence and Melanoma in Mice

(2009) Nathalie Dhomen et al.   CANCER CELL

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

Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer

(2009) Tetsuya Mitsudomi et al.   FEBS Journal

BrafV600E cooperates with Pten loss to induce metastatic melanoma

(2009) David Dankort et al.   NATURE GENETICS

Class I PI3K in oncogenic cellular transformation

(2008) L Zhao et al.   ONCOGENE