Inhibitors of HSP90 in melanoma

Cancer statistics, 2019

(2019) Rebecca L. Siegel et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Induced cross-resistance of BRAFV600E melanoma cells to standard chemotherapeutic dacarbazine after chronic PLX4032 treatment

(2019) Sarah Erdmann et al.   Scientific Reports

Role of miRNAs in Melanoma Metastasis

(2019) Anna Gajos-Michniewicz et al.   Cancers

Targeting the ERK Signaling Pathway in Melanoma

(2019) Paola Savoia et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The Potential of Targeting P53 and HSP90 Overcoming Acquired MAPKi-Resistant Melanoma

(2019) Chi-Che Hsieh et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

Cross-talk between receptor tyrosine kinases AXL and ERBB3 regulates invadopodia formation in melanoma cells

(2019) Or-Yam Revach et al.   CANCER RESEARCH

17-Aminogeldanamycin selectively diminishes IRE1α-XBP1s pathway activity and cooperatively induces apoptosis with MEK1/2 and BRAFV600E inhibitors in melanoma cells of different genetic subtypes

(2019) Aleksandra Mielczarek-Lewandowska et al.   APOPTOSIS

Many ways to resistance: How melanoma cells evade targeted therapies

(2019) Ines Kozar et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

HDAC Inhibitors Exert Anti-Myeloma Effects through Multiple Modes of Action

(2019) Yoichi Imai et al.   Cancers

Plasticity of Drug-Naïve and Vemurafenib- or Trametinib-Resistant Melanoma Cells in Execution of Differentiation/Pigmentation Program

(2019) Malgorzata Czyz et al.   Journal of Oncology

Regulation of the Hsp90 system

(2018) Siyuan Sima et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Combined BRAF and HSP90 inhibition in patients with unresectableBRAFV600E mutant melanoma

(2018) Zeynep Eroglu et al.   CLINICAL CANCER RESEARCH

Heat shock protein 90 inhibitor enhances apoptosis by inhibiting the AKT pathway in thermal-stimulated SK-MEL-2 human melanoma cell line

(2018) Min Kyung Shin et al.   JOURNAL OF DERMATOLOGICAL SCIENCE

Wnt-signaling enhances neural crest migration of melanoma cells and induces an invasive phenotype

(2018) Tobias Sinnberg et al.   Molecular Cancer

Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors

(2018) Alireza Azimi et al.   Molecular Systems Biology

17-AAG inhibits vemurafenib-associated MAP kinase activation and is synergistic with cellular immunotherapy in a murine melanoma model

(2018) Sandeep S. Joshi et al.   PLoS One

A LY-15, a novel cyclic pentapeptide that inhibits B16 cell proliferation and migration and induces cell apoptosis

(2018) Xuan Wang et al.   Oncology Letters

A switch point in the molecular chaperone Hsp90 responding to client interaction

(2018) Daniel Andreas Rutz et al.   Nature Communications

Discovery of new molecular entities able to strongly interfere with Hsp90 C-terminal domain

(2018) Stefania Terracciano et al.   Scientific Reports

Management of Metastatic Melanoma in 2018

(2018) Howard L. Kaufman et al.   JAMA Oncology

Reversal of Resistance in Targeted Therapy of Metastatic Melanoma: Lessons Learned from Vemurafenib (BRAFV600E-Specific Inhibitor)

(2018) Antoni Torres-Collado et al.   Cancers

Anti-PD-1 and Anti-CTLA-4 Therapies in Cancer: Mechanisms of Action, Efficacy, and Limitations

(2018) Judith A. Seidel et al.   Frontiers in Oncology

The HSP90 Family: Structure, Regulation, Function, and Implications in Health and Disease

(2018) Abdullah Hoter et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Results from phase II trial of HSP90 inhibitor, STA-9090 (ganetespib), in metastatic uveal melanoma

(2018) Shalin Shah et al.   MELANOMA RESEARCH

Bad Company: Microenvironmentally Mediated Resistance to Targeted Therapy in Melanoma

(2018) Filipe V Almeida et al.   Pigment Cell & Melanoma Research

Oncogenic PI3K/AKT promotes the step-wise evolution of combination BRAF/MEK inhibitor resistance in melanoma

(2018) Mal Irvine et al.   Oncogenesis

Hsp90 and Hsp70 chaperones: Collaborators in protein remodeling

(2018) Olivier Genest et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Whole-exome sequencing reveals novel genetic variants associated with diverse phenotypes of melanoma cells

(2018) Mariusz L. Hartman et al.   MOLECULAR CARCINOGENESIS

A mechanism for cancer-associated inactivation of NQO1 due to P187S and its reactivation by the consensus mutation H80R

(2017) Inés G. Muñoz et al.   FEBS LETTERS

First-in-human study of the epichaperome inhibitor PU-H71: clinical results and metabolic profile

(2017) Giovanna Speranza et al.   INVESTIGATIONAL NEW DRUGS

Molecular testing for BRAF mutations to inform melanoma treatment decisions: a move toward precision medicine

(2017) Liang Cheng et al.   MODERN PATHOLOGY

Histone deacetylase activity mediates acquired resistance towards structurally diverse HSP90 inhibitors

(2017) Ryan C. Chai et al.   Molecular Oncology

Whole-genome landscapes of major melanoma subtypes

(2017) Nicholas K. Hayward et al.   NATURE

VISTA is an inhibitory immune checkpoint that is increased after ipilimumab therapy in patients with prostate cancer

(2017) Jianjun Gao et al.   NATURE MEDICINE

The HSP90 chaperone machinery

(2017) Florian H. Schopf et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Phenotype-based variation as a biomarker of sensitivity to molecularly targeted therapy in melanoma

(2017) Kerem M. Senses et al.   MedChemComm

HSP90 inhibition enhances cancer immunotherapy by upregulating interferon response genes

(2017) Rina M. Mbofung et al.   Nature Communications

Induction of Hsp70 in tumor cells treated with inhibitors of the Hsp90 activity: A predictive marker and promising target for radiosensitization

(2017) Vladimir A. Kudryavtsev et al.   PLoS One

HSP90 is a promising target in gemcitabine and 5-fluorouracil resistant pancreatic cancer

(2016) Tarik Ghadban et al.   APOPTOSIS

Mechanisms of Hsp90 regulation

(2016) C. Prodromou   BIOCHEMICAL JOURNAL

Hsp90: Friends, clients and natural foes

(2016) Sharad Verma et al.   BIOCHIMIE

Wnt/β-catenin signaling in melanoma: Preclinical rationale and novel therapeutic insights

(2016) Gongda Xue et al.   CANCER TREATMENT REVIEWS

PU-H71, a novel Hsp90 inhibitor, as a potential cancer-specific sensitizer to carbon-ion beam therapy

(2016) Huizi Keiko Li et al.   JOURNAL OF RADIATION RESEARCH

Loss of cohesin complex components STAG2 or STAG3 confers resistance to BRAF inhibition in melanoma

(2016) Che-Hung Shen et al.   NATURE MEDICINE

Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma

(2016) Jesse M. Zaretsky et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Ig V H complementarity-determining region 3-containing Rb9 peptide, inhibits melanoma cells migration and invasion by interactions with Hsp90 and an adhesion G-protein coupled receptor

(2016) Natalia Girola et al.   PEPTIDES

Enhancing the evaluation of PI3K inhibitors through 3D melanoma models

(2016) Batool Shannan et al.   Pigment Cell & Melanoma Research

2-phenylethynesulphonamide (PFT-μ) enhances the anticancer effect of the novel hsp90 inhibitor NVP-AUY922 in melanoma, by reducing GSH levels

(2016) Andree Yeramian et al.   Pigment Cell & Melanoma Research

Melanoma and the Unfolded Protein Response

(2016) Erin Sykes et al.   Cancers

NAD(P)H:Quinone Oxidoreductase-1 Expression Sensitizes Malignant Melanoma Cells to the HSP90 Inhibitor 17-AAG

(2016) Shuya Kasai et al.   PLoS One

Membrane-bound heat shock proteins facilitate the uptake of dying cells and cross-presentation of cellular antigen

(2015) Haiyan Zhu et al.   APOPTOSIS

Synthesis and biological evaluation of geldanamycin analogs against human cancer cells

(2015) Yan-ping Li et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Genomic Classification of Cutaneous Melanoma

(2015) Rehan Akbani et al.   CELL

NF-κB Regulation of c-FLIP Promotes TNFα-Mediated RAF Inhibitor Resistance in Melanoma

(2015) Yongping Shao et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

XL888 Limits Vemurafenib-Induced Proliferative Skin Events by Suppressing Paradoxical MAPK Activation

(2015) Manali Phadke et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Novel cyclic pentapeptide H-15 induces differentiation and inhibits proliferation in murine melanoma B16 cells

(2015) YUNJIANG LIU et al.   Oncology Letters

Melanoma

(2015) Dirk Schadendorf et al.   Nature Reviews Disease Primers

The HSP90 Inhibitor Ganetespib Radiosensitizes Human Lung Adenocarcinoma Cells

(2015) Roberto Gomez-Casal et al.   Cancers

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

Client Proteins and Small Molecule Inhibitors Display Distinct Binding Preferences for Constitutive and Stress-Induced HSP90 Isoforms and Their Conformationally Restricted Mutants

(2015) Thomas L. Prince et al.   PLoS One

Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition

(2015)   Oncotarget

Posttranslational modification and conformational state of Heat Shock Protein 90 differentially affect binding of chemically diverse small molecule inhibitors

(2015) Kristin Beebe et al.   Oncotarget

Targeting Aerobic Glycolysis and HIF-1α Expression Enhance Imiquimod-induced Apoptosis in Cancer Cells

(2015) Shi-Wei Huang et al.   Oncotarget

ABCB5 Maintains Melanoma-Initiating Cells through a Proinflammatory Cytokine Signaling Circuit

(2014) B. J. Wilson et al.   CANCER RESEARCH

Oncogenic BRAF induces chronic ER stress condition resulting in increased basal autophagy and apoptotic resistance of cutaneous melanoma

(2014) M Corazzari et al.   CELL DEATH AND DIFFERENTIATION

An artificial HSE promoter for efficient and selective detection of heat shock pathway activity

(2014) Viktoria Ortner et al.   CELL STRESS & CHAPERONES

First-in-Human Phase I Dose Escalation Study of a Second-Generation Non-Ansamycin HSP90 Inhibitor, AT13387, in Patients with Advanced Solid Tumors

(2014) G. I. Shapiro et al.   CLINICAL CANCER RESEARCH

Phase I dose-escalation studies of SNX-5422, an orally bioavailable heat shock protein 90 inhibitor, in patients with refractory solid tumours

(2014) Jeffrey R. Infante et al.   EUROPEAN JOURNAL OF CANCER

Hsp90 inhibitor as a sensitizer of cancer cells to different therapies (Review)

(2014) Zuzana Sol�rov� et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Potential diagnostic significance of HSP90, ACS/TMS1, and L-plastin in the identification of melanoma

(2014) Allen G. Strickler et al.   MELANOMA RESEARCH

Evaluating Melanoma Drug Response and Therapeutic Escape with Quantitative Proteomics

(2014) Vito W. Rebecca et al.   MOLECULAR & CELLULAR PROTEOMICS

Overcoming Acquired BRAF Inhibitor Resistance in Melanoma via Targeted Inhibition of Hsp90 with Ganetespib

(2014) J. Acquaviva et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of HSP90 by AT13387 Delays the Emergence of Resistance to BRAF Inhibitors and Overcomes Resistance to Dual BRAF and MEK Inhibition in Melanoma Models

(2014) T. Smyth et al.   MOLECULAR CANCER THERAPEUTICS

Heat shock protein 90 promotes epithelial to mesenchymal transition, invasion, and migration in colorectal cancer

(2014) Ganji Purnachandra Nagaraju et al.   MOLECULAR CARCINOGENESIS

Comparative effects of SNX-7081 and SNX-2112 on cell cycle, apoptosis and Hsp90 client proteins in human cancer cells

(2014) XIAO WANG et al.   ONCOLOGY REPORTS

Natural Compounds' Activity against Cancer Stem-Like or Fast-Cycling Melanoma Cells

(2014) Malgorzata Sztiller-Sikorska et al.   PLoS One

Gene Expression Profiling Identifies Microphthalmia-Associated Transcription Factor (MITF) and Dickkopf-1 (DKK1) as Regulators of Microenvironment-Driven Alterations in Melanoma Phenotype

(2014) Mariusz L. Hartman et al.   PLoS One

A novel cyclic pentapeptide, H-10, inhibits B16 cancer cell growth and induces cell apoptosis

(2014) GENG ZHANG et al.   Oncology Letters

Low MITF/AXL ratio predicts early resistance to multiple targeted drugs in melanoma

(2014) Judith Müller et al.   Nature Communications

The Immune Microenvironment Confers Resistance to MAPK Pathway Inhibitors through Macrophage-Derived TNF 

(2014) M. P. Smith et al.   Cancer Discovery

The Double-Edged Sword: Conserved Functions of Extracellular Hsp90 in Wound Healing and Cancer

(2014) Michael Hance et al.   Cancers

Hsp90 inhibition by PU-H71 induces apoptosis through endoplasmic reticulum stress and mitochondrial pathway in cancer cells and overcomes the resistance conferred by Bcl-2

(2013) Cindy Gallerne et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Targeting MAPK pathway in melanoma therapy

(2013) Yabin Cheng et al.   CANCER AND METASTASIS REVIEWS

Tanespimycin and Tipifarnib Exhibit Synergism in Inducing Apoptosis in Melanoma Cell Lines From Later Stages of Tumor Progression

(2013) Anna Bentke et al.   CANCER INVESTIGATION

Sustained IRE1 and ATF6 signaling is important for survival of melanoma cells undergoing ER stress

(2013) Kwang Hong Tay et al.   CELLULAR SIGNALLING

Resistance to BRAF-targeted therapy in melanoma

(2013) Ryan J. Sullivan et al.   EUROPEAN JOURNAL OF CANCER

Oncogenic Activation of MEK/ERK Primes Melanoma Cells for Adaptation to Endoplasmic Reticulum Stress

(2013) Amanda Croft et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Inhibition of Wee1, AKT, and CDK4 Underlies the Efficacy of the HSP90 Inhibitor XL888 in an In Vivo Model of NRAS-Mutant Melanoma

(2013) H. E. Haarberg et al.   MOLECULAR CANCER THERAPEUTICS

The road to maturation: somatic cell interaction and self-organization of the mammalian oocyte

(2013) Rong Li et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Activity of the Heat Shock Protein 90 Inhibitor Ganetespib in Melanoma

(2013) Xinqi Wu et al.   PLoS One

The Role of the PI3K-AKT Pathway in Melanoma

(2012) Michael A. Davies   CANCER JOURNAL

Hsps are up-regulated in melanoma tissue and correlate with patient clinical parameters

(2012) Christopher Shipp et al.   CELL STRESS & CHAPERONES

The HSP90 Inhibitor XL888 Overcomes BRAF Inhibitor Resistance Mediated through Diverse Mechanisms

(2012) K. H. T. Paraiso et al.   CLINICAL CANCER RESEARCH

NF-κB as potential target in the treatment of melanoma

(2012) Gabriele Madonna et al.   Journal of Translational Medicine

Systematic Identification of the HSP90 Regulated Proteome

(2012) Zhixiang Wu et al.   MOLECULAR & CELLULAR PROTEOMICS

Melanoma exosomes educate bone marrow progenitor cells toward a pro-metastatic phenotype through MET

(2012) Héctor Peinado et al.   NATURE MEDICINE

The heat shock protein 90 inhibitor SNX-2112 inhibits B16 melanoma cell growth in vitro and in vivo

(2012) Yi-Fei Wang   ONCOLOGY REPORTS

Charged linker sequence modulates eukaryotic heat shock protein 90 (Hsp90) chaperone activity

(2012) S. Tsutsumi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

NAD(P)H:quinone oxidoreductase 1 (NQO1) in the sensitivity and resistance to antitumor quinones

(2011) David Siegel et al.   BIOCHEMICAL PHARMACOLOGY

Post-translational modifications of Hsp90 and their contributions to chaperone regulation

(2011) Mehdi Mollapour et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

A novel C-terminal HSP90 inhibitor KU135 induces apoptosis and cell cycle arrest in melanoma cells

(2011) Abbas K. Samadi et al.   CANCER LETTERS

SNX-2112, an Hsp90 inhibitor, induces apoptosis and autophagy via degradation of Hsp90 client proteins in human melanoma A-375 cells

(2011) Kai-Sheng Liu et al.   CANCER LETTERS

The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer

(2011) Brent Graham et al.   CANCER SCIENCE

HSP90: The Rosetta stone for cellular protein dynamics?

(2011) Diane C. DeZwaan et al.   CELL CYCLE

mTOR signaling in protein homeostasis

(2011) Crystal S. Conn et al.   CELL CYCLE

The Novel HSP90 Inhibitor, IPI-493, Is Highly Effective in Human Gastrostrointestinal Stromal Tumor Xenografts Carrying Heterogeneous KIT Mutations

(2011) G. Floris et al.   CLINICAL CANCER RESEARCH

A Phase I Study of PF-04929113 (SNX-5422), an Orally Bioavailable Heat Shock Protein 90 Inhibitor, in Patients with Refractory Solid Tumor Malignancies and Lymphomas

(2011) A. Rajan et al.   CLINICAL CANCER RESEARCH

A Phase I Study of the Heat Shock Protein 90 Inhibitor Alvespimycin (17-DMAG) Given Intravenously to Patients with Advanced Solid Tumors

(2011) Simon Pacey et al.   CLINICAL CANCER RESEARCH

Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90

(2011) Kamalika Moulick et al.   Nature Chemical Biology

High-Content, High-Throughput Analysis of Cell Cycle Perturbations Induced by the HSP90 Inhibitor XL888

(2011) Susan K. Lyman et al.   PLoS One

Phase I Evaluation of STA-1474, a Prodrug of the Novel HSP90 Inhibitor Ganetespib, in Dogs with Spontaneous Cancer

(2011) Cheryl A. London et al.   PLoS One

Macrocyclic Inhibitors of Hsp90

(2010) Victoria A. Johnson et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Preclinical Antitumor Activity of the Orally Available Heat Shock Protein 90 Inhibitor NVP-BEP800

(2010) Andrew J. Massey et al.   MOLECULAR CANCER THERAPEUTICS

A New Geldanamycin Analogue from Streptomyces hygroscopicus

(2010) Hao Zhang et al.   MOLECULES

HSP90 and its inhibitors (Review)

(2010) Naomoto   ONCOLOGY REPORTS

Bcl-2 Regulates HIF-1α Protein Stabilization in Hypoxic Melanoma Cells via the Molecular Chaperone HSP90

(2010) Daniela Trisciuoglio et al.   PLoS One

Cytotoxic sugar analogues of an optimized novobiocin scaffold

(2010) Alison C. Donnelly et al.   MedChemComm

Geldanamycin and its anti-cancer activities

(2009) Yayoi Fukuyo et al.   CANCER LETTERS

Acquired Resistance to 17-Allylamino-17-Demethoxygeldanamycin (17-AAG, Tanespimycin) in Glioblastoma Cells

(2009) N. Gaspar et al.   CANCER RESEARCH

Inhibition of heat shock protein 90 sensitizes melanoma cells to thermosensitive ferromagnetic particle-mediated hyperthermia with low Curie temperature

(2009) Aki Ito et al.   CANCER SCIENCE

A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6–dependent B cell lymphomas

(2009) Leandro C Cerchietti et al.   NATURE MEDICINE

NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis

(2008) S. A. Eccles et al.   CANCER RESEARCH

Phase II Trial of 17-Allylamino-17-Demethoxygeldanamycin in Patients with Metastatic Melanoma

(2008) D. B. Solit et al.   CLINICAL CANCER RESEARCH

153 POSTER IPI-493, a potent, orally bioavailable Hsp90 inhibitor of the ansamycin class

(2008) J. Lee et al.   EJC SUPPLEMENTS

Pigmentation and skin-cancer risk

(2008) Kyle Vogan   NATURE REVIEWS GENETICS