Metastatic Melanoma: Insights Into the Evolution of the Treatments and Future Challenges

Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance

(2016) Michaël Cerezo et al.   CANCER CELL

Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells

(2016) Zhen Li et al.   CANCER LETTERS

Ras Conformational Ensembles, Allostery, and Signaling

(2016) Shaoyong Lu et al.   CHEMICAL REVIEWS

Metastatic Melanoma – A Review of Current and Future Treatment Options

(2015) E Maverakis et al.   ACTA DERMATO-VENEREOLOGICA

Recent progress on MAP kinase pathway inhibitors

(2015) David E. Uehling et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The role of JAK/STAT signalling in the pathogenesis, prognosis and treatment of solid tumours

(2015) S J Thomas et al.   BRITISH JOURNAL OF CANCER

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

Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma

(2015) Maria Romina Girotti et al.   CANCER CELL

Genomic Classification of Cutaneous Melanoma

(2015) Rehan Akbani et al.   CELL

Reorienting the immune system in the treatment of cancer by using anti-PD-1 and anti-PD-L1 antibodies

(2015) Troels H. Borch et al.   DRUG DISCOVERY TODAY

BRAF and MEK inhibition in melanoma

(2015) Lesly A Dossett et al.   Expert Opinion On Drug Safety

Nivolumab plus ipilimumab in the treatment of advanced melanoma

(2015) Katy K. Tsai et al.   Journal of Hematology & Oncology

Discovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells

(2015) James R. Henry et al.   JOURNAL OF MEDICINAL CHEMISTRY

The multi-faceted roles of the PI3K-AKT pathway in melanoma

(2015) Michael A Davies   Journal of Translational Medicine

Pembrolizumab versus investigator-choice chemotherapy for ipilimumab-refractory melanoma (KEYNOTE-002): a randomised, controlled, phase 2 trial

(2015) Antoni Ribas et al.   LANCET ONCOLOGY

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

Nivolumab in Previously Untreated Melanoma without BRAF Mutation

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

Pembrolizumab versus Ipilimumab in Advanced Melanoma

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

Combined Nivolumab and Ipilimumab or Monotherapy in Untreated Melanoma

(2015) James Larkin et al.   NEW ENGLAND JOURNAL OF MEDICINE

NF-kB2 induces senescence bypass in melanoma via a direct transcriptional activation of EZH2

(2015) G M De Donatis et al.   ONCOGENE

Endoplasmic Reticulum Stress-Activated Cell Reprogramming in Oncogenesis

(2015) E. Chevet et al.   Cancer Discovery

Beyond BRAF: where next for melanoma therapy?

(2014) I V Fedorenko et al.   BRITISH JOURNAL OF CANCER

Mechanism and consequences of RAF kinase activation by small-molecule inhibitors

(2014) M Holderfield et al.   BRITISH JOURNAL OF CANCER

Loss of NF1 in Cutaneous Melanoma Is Associated with RAS Activation and MEK Dependence

(2014) Moriah H. Nissan et al.   CANCER RESEARCH

Dabrafenib and Trametinib, Alone and in Combination for BRAF-Mutant Metastatic Melanoma

(2014) A. M. Menzies et al.   CLINICAL CANCER RESEARCH

Non-BRAF-targeted therapy, immunotherapy, and combination therapy for melanoma

(2014) Sara Tomei et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

New RAF kinase inhibitors in cancer therapy

(2014) Juan Martin-Liberal et al.   EXPERT OPINION ON PHARMACOTHERAPY

Strategies for modern biomarker and drug development in oncology

(2014) Alan D Smith et al.   Journal of Hematology & Oncology

Targeted therapy by combined inhibition of the RAF and mTOR kinases in malignant spindle cell neoplasm harboring the KIAA1549-BRAF fusion protein

(2014) Vivek Subbiah et al.   Journal of Hematology & Oncology

Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase

(2014) Yongqi Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase Ib/II, open-label, dose-escalation study of LGX818, an oral selective BRAF inhibitor, in combination with MEK162, an oral MEK1/2 inhibitor, in patients with BRAF V600-dependent advanced solid tumors: preliminary results

(2014) Richard Kefford et al.   Journal of Translational Medicine

Acquired and intrinsic resistance in cancer immunotherapy

(2014) Sander Kelderman et al.   Molecular Oncology

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics

(2014) Apirat Chaikuad et al.   Nature Chemical Biology

The clinical development of MEK inhibitors

(2014) Yujie Zhao et al.   Nature Reviews Clinical Oncology

Targeting RAS–ERK signalling in cancer: promises and challenges

(2014) Ahmed A. Samatar et al.   NATURE REVIEWS DRUG DISCOVERY

Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma

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

Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma

(2014) Georgina V. Long et al.   Nature Communications

Treatment of BRAF-Mutant Melanoma: The Role of Vemurafenib and Other Therapies

(2013) S Jang et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

B-Raf mutation: A key player in molecular biology of cancer

(2013) M.A. Rahman et al.   EXPERIMENTAL AND MOLECULAR PATHOLOGY

Molecular biology of normal melanocytes and melanoma cells

(2013) Bizhan Bandarchi et al.   JOURNAL OF CLINICAL PATHOLOGY

B-Raf and the inhibitors: from bench to bedside

(2013) Tiangui Huang et al.   Journal of Hematology & Oncology

Stat3-Targeted Therapies Overcome the Acquired Resistance to Vemurafenib in Melanomas

(2013) Fang Liu et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

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

Effects of Raf Dimerization and Its Inhibition on Normal and Disease-Associated Raf Signaling

(2013) Alyson K. Freeman et al.   MOLECULAR CELL

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

(2013) Georgia Hatzivassiliou et al.   NATURE

Hepatotoxicity with Combination of Vemurafenib and Ipilimumab

(2013) Antoni Ribas et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Challenging resistance mechanisms to therapies for metastatic melanoma

(2013) Lucio Tentori et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

(2013) Tara R. Rheault et al.   ACS Medicinal Chemistry Letters

MAP Kinase Pathway Alterations in BRAF-Mutant Melanoma Patients with Acquired Resistance to Combined RAF/MEK Inhibition

(2013) N. Wagle et al.   Cancer Discovery

Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors

(2013) E. J. Morris et al.   Cancer Discovery

The Molecular Chaperone GRP78/BiP in the Development of Chemoresistance: Mechanism and Possible Treatment

(2013) Corinna Roller et al.   Frontiers in Pharmacology

A systematic review of worldwide incidence of nonmelanoma skin cancer

(2012) A. Lomas et al.   BRITISH JOURNAL OF DERMATOLOGY

The Role of the PI3K-AKT Pathway in Melanoma

(2012) Michael A. Davies   CANCER JOURNAL

Abstract 3790: Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor

(2012) Darrin D. Stuart et al.   CANCER RESEARCH

A Comprehensive Survey of Ras Mutations in Cancer

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

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

(2012) Axel Hauschild et al.   LANCET

ERK Inhibition Overcomes Acquired Resistance to MEK Inhibitors

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

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Improved Survival with MEK Inhibition in BRAF-Mutated Melanoma

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Safety and Activity of Anti–PD-L1 Antibody in Patients with Advanced Cancer

(2012) Julie R. Brahmer et al.   NEW ENGLAND JOURNAL OF MEDICINE

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

(2012) Kenneth D. Rice et al.   ACS Medicinal Chemistry Letters

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

(2011) John C. Stellwagen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

(2011) A. G. Gilmartin et al.   CLINICAL CANCER RESEARCH

IL-2 family cytokines: new insights into the complex roles of IL-2 as a broad regulator of T helper cell differentiation

(2011) Wei Liao et al.   CURRENT OPINION IN IMMUNOLOGY

BRAFV600E: Implications for Carcinogenesis and Molecular Therapy

(2011) E. R. Cantwell-Dorris et al.   MOLECULAR CANCER THERAPEUTICS

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

(2011) Poulikos I. Poulikakos et al.   NATURE

Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma

(2011) Sergey I Nikolaev et al.   NATURE GENETICS

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

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

Ipilimumab plus Dacarbazine for Previously Untreated Metastatic Melanoma

(2011) Caroline Robert et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate)

(2011) Hiroyuki Abe et al.   ACS Medicinal Chemistry Letters

Efficacy and safety of ipilimumab monotherapy in patients with pretreated advanced melanoma: a multicenter single-arm phase II study

(2010) S. J. O'Day et al.   ANNALS OF ONCOLOGY

Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy

(2010) K H T Paraiso et al.   BRITISH JOURNAL OF CANCER

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

RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models

(2010) H. Yang et al.   CANCER RESEARCH

A Phase II Study of PD-0325901, an Oral MEK Inhibitor, in Previously Treated Patients with Advanced Non-Small Cell Lung Cancer

(2010) E. B. Haura et al.   CLINICAL CANCER RESEARCH

Interleukin-2 Receptor Signaling: At the Interface between Tolerance and Immunity

(2010) Thomas R. Malek et al.   IMMUNITY

Review: Ultraviolet radiation and skin cancer

(2010) Deevya L. Narayanan et al.   INTERNATIONAL JOURNAL OF DERMATOLOGY

From basic research to clinical development of MEK1/2 inhibitors for cancer therapy

(2010) Christophe Frémin et al.   Journal of Hematology & Oncology

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

(2010) Georgia Hatzivassiliou et al.   NATURE

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

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

Improved Survival with Ipilimumab in Patients with Metastatic Melanoma

(2010) F. Stephen Hodi et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Immune Checkpoint Proteins: A New Therapeutic Paradigm for Cancer—Preclinical Background: CTLA-4 and PD-1 Blockade

(2010) Jeffrey Weber   SEMINARS IN ONCOLOGY

Melanocytes in development and cancer

(2009) Audrey Uong et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Final Version of 2009 AJCC Melanoma Staging and Classification

(2009) Charles M. Balch et al.   JOURNAL OF CLINICAL ONCOLOGY

A dimerization-dependent mechanism drives RAF catalytic activation

(2009) Thanashan Rajakulendran et al.   NATURE

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

Cell death and endoplasmic reticulum stress: disease relevance and therapeutic opportunities

(2008) Inki Kim et al.   NATURE REVIEWS DRUG DISCOVERY

Understanding Signaling Cascades in Melanoma

(2008) Pablo Lopez-Bergami et al.   PHOTOCHEMISTRY AND PHOTOBIOLOGY

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