Pharmacological Inhibition of EZH2 by ZLD1039 Suppresses Tumor Growth and Pulmonary Metastasis in Melanoma Cells in vitro and in vivo.

[1]  J. Burke,et al.  Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas. , 2022, Blood reviews.

[2]  Chengyuan Liang,et al.  Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. , 2022, Journal of medicinal chemistry.

[3]  S. Wen,et al.  Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. , 2022, Journal of medicinal chemistry.

[4]  A. Lallas,et al.  European consensus-based interdisciplinary guideline for melanoma. Part 1: Diagnostics: Update 2022. , 2022, European journal of cancer.

[5]  D. Hanahan Hallmarks of Cancer: New Dimensions. , 2022, Cancer discovery.

[6]  Chunying Li,et al.  Signal pathways of melanoma and targeted therapy , 2021, Signal Transduction and Targeted Therapy.

[7]  B. Teicher,et al.  Evaluation of an EZH2 inhibitor in patient-derived orthotopic xenograft models of pediatric brain tumors alone and in combination with chemo- and radiation therapies , 2021, Laboratory Investigation.

[8]  W. De,et al.  EZH2-mediated epigenetic suppression of lncRNA PCAT18 predicts a poor prognosis and regulates the expression of p16 by interacting with miR-570a-3p in gastric cancer , 2021, Journal of Cancer.

[9]  A. Mai,et al.  Polycomb Repressive Complex 2 Modulation through the Development of EZH2–EED Interaction Inhibitors and EED Binders , 2021, Journal of medicinal chemistry.

[10]  Peng Huang,et al.  Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. , 2021, Journal of medicinal chemistry.

[11]  Kaixian Chen,et al.  Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. , 2021, Journal of medicinal chemistry.

[12]  Lidan Zhang,et al.  The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor. , 2021, Chemical communications.

[13]  Xiuli Wu,et al.  Design and Synthesis of EZH2-Based PROTACs to Degrade the Complex for Targeting the Noncatalytic Activity of EZH2. , 2021, Journal of medicinal chemistry.

[14]  A. Jemal,et al.  Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries , 2021, CA: a cancer journal for clinicians.

[15]  K. Flaherty,et al.  Cobimetinib plus atezolizumab in BRAFV600 wild-type melanoma: primary results from the randomized phase 3 IMspire170 study. , 2020, Annals of oncology : official journal of the European Society for Medical Oncology.

[16]  S. Stacchiotti,et al.  Tazemetostat for advanced epithelioid sarcoma: current status and future perspectives. , 2020, Future oncology.

[17]  Yong Xia,et al.  Repurposing of Antipsychotic Trifluoperazine for Treating Brain Metastasis, Lung Metastasis and Bone Metastasis of Melanoma by Disrupting Autophagy Flux. , 2020, Pharmacological research.

[18]  Clare Gregson,et al.  Targeting PRC2 for the treatment of cancer: an updated patent review (2016 - 2020) , 2020, Expert opinion on therapeutic patents.

[19]  Z. Werb,et al.  Concepts of extracellular matrix remodelling in tumour progression and metastasis , 2020, Nature Communications.

[20]  G. Salles,et al.  Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial. , 2020, The Lancet. Oncology.

[21]  S. Shiva,et al.  Mitochondrial electron transport chain: Oxidative phosphorylation, oxidant production, and methods of measurement , 2020, Redox biology.

[22]  K. Tew,et al.  Oxidative Stress in Cancer. , 2020, Cancer cell.

[23]  Sheridan M. Hoy Tazemetostat: First Approval , 2020, Drugs.

[24]  Friederike Hoffmann,et al.  H3K27me3 and EZH2 expression in melanoma: relevance for melanoma progression and response to immune checkpoint blockade , 2020, Clinical Epigenetics.

[25]  A. Laganà,et al.  Discovery of a first-in-class EZH2 selective degrader , 2019, Nature Chemical Biology.

[26]  Xiuli Wu,et al.  Repurposing of the Anti-helminthic Drug Niclosamide to Treat Melanoma and Pulmonary Metastasis via the STAT3 Signaling Pathway. , 2019, Biochemical pharmacology.

[27]  R. Sullivan,et al.  Atezolizumab plus cobimetinib and vemurafenib in BRAF-mutated melanoma patients , 2019, Nature Medicine.

[28]  A. Vincent-Salomon,et al.  EZH1/2 function mostly within canonical PRC2 and exhibit proliferation-dependent redundancy that shapes mutational signatures in cancer , 2019, Proceedings of the National Academy of Sciences.

[29]  E. Jordanova,et al.  Overexpression of EZH2 in conjunctival melanoma offers a new therapeutic target , 2018, The Journal of pathology.

[30]  Liang-Chih Liu,et al.  EZH2 promotes migration and invasion of triple-negative breast cancer cells via regulating TIMP2-MMP-2/-9 pathway. , 2018, American journal of cancer research.

[31]  Jing Cai,et al.  EZH2-mediated epigenetic silencing of TIMP2 promotes ovarian cancer migration and invasion , 2017, Scientific Reports.

[32]  Ming Yan,et al.  A covalently bound inhibitor triggers EZH2 degradation through CHIP‐mediated ubiquitination , 2017, The EMBO journal.

[33]  I. Makhoul,et al.  Role of EZH2 histone methyltrasferase in melanoma progression and metastasis , 2016, Cancer biology & therapy.

[34]  Yuquan Wei,et al.  Selective inhibition of EZH2 by ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast cancer , 2016, Scientific Reports.

[35]  C. Roberts,et al.  Targeting EZH2 in cancer , 2016, Nature Medicine.

[36]  Nathan L. Avaritt,et al.  Quantitative Histone Mass Spectrometry Identifies Elevated Histone H3 Lysine 27 (Lys27) Trimethylation in Melanoma* , 2015, Molecular & Cellular Proteomics.

[37]  T. Horvath,et al.  Mitochondrial ROS Signaling in Organismal Homeostasis , 2015, Cell.

[38]  Lidan Zhang,et al.  Design, synthesis and biological evaluation of novel 1-methyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinolins as potential EZH2 inhibitors , 2015 .

[39]  R. Dummer,et al.  The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors , 2015, Nature Communications.

[40]  P. Hersey,et al.  EZH2: an emerging role in melanoma biology and strategies for targeted therapy , 2015, Pigment cell & melanoma research.

[41]  D. Fisher,et al.  The melanoma revolution: From UV carcinogenesis to a new era in therapeutics , 2014, Science.

[42]  P. Schumacker,et al.  Mitochondrial ROS in cancer: initiators, amplifiers or an Achilles' heel? , 2014, Nature Reviews Cancer.

[43]  Yasunori Sato,et al.  Immunostaining for Polycomb Group Protein EZH2 and Senescent Marker p16INK4a May Be Useful to Differentiate Cholangiolocellular Carcinoma From Ductular Reaction and Bile Duct Adenoma , 2014, The American journal of surgical pathology.

[44]  Y. Sakamoto,et al.  Enhancer of Zeste Homolog 2 (EZH2) Promotes Progression of Cholangiocarcinoma Cells by Regulating Cell Cycle and Apoptosis , 2013, Annals of Surgical Oncology.

[45]  Y. Wan,et al.  H3K9me-enhanced DNA hypermethylation of the p16INK4a gene: an epigenetic signature for spontaneous transformation of rat mesenchymal stem cells. , 2013, Stem cells and development.

[46]  A. Sivachenko,et al.  A Landscape of Driver Mutations in Melanoma , 2012, Cell.

[47]  Benjamin E. Gross,et al.  The cBio cancer genomics portal: an open platform for exploring multidimensional cancer genomics data. , 2012, Cancer discovery.

[48]  Norma I Rodríguez-Malavé,et al.  MicroRNAs in B cell development and malignancy , 2012, Journal of Hematology & Oncology.

[49]  Yong Jiang,et al.  Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27) , 2012, Proceedings of the National Academy of Sciences.

[50]  D. Reinberg,et al.  The Polycomb complex PRC2 and its mark in life , 2011, Nature.

[51]  J. Massagué,et al.  G1 cell-cycle control and cancer , 2004, Nature.

[52]  A. Hauschild,et al.  Improved overall survival in melanoma with combined dabrafenib and trametinib. , 2015, The New England journal of medicine.