Reductions in Organic Chemistry

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Cancer epigenetics: tumor heterogeneity, plasticity of stem-like states, and drug resistance. Mol Cell. Epigenetic alterations in acute myeloid leukemias. FEBS J. Minucci S, Pelicci PG. Histone deacetylase inhibitors and the promise of epigenetic and more treatments for cancer. Epigenetic treatment of myelodysplastic syndromes and acute myeloid leukemias. Curr Med Chem. Rius M, Lyko F.

Conventional Cancer Treatment

Epigenetic cancer therapy: rationales, targets and drugs. Epigenetic protein families: a new frontier for drug discovery. Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders. Holoch D, Moazed D. RNA-mediated epigenetic regulation of gene expression. Perspectives on the mechanism of transcriptional regulation by long non-coding RNAs. Transcriptional targeting by microRNA-polycomb complexes: a novel route in cell fate determination.

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Characteristics of the solid tumors

Epigenetic role of miRNAs in normal and leukemic hematopoiesis. FDA approval summary: vorinostat for treatment of advanced primary cutaneous T-cell lymphoma. Panobinostat plus bortezomib and dexamethasone versus placebo plus bortezomib and dexamethasone in patients with relapsed or relapsed and refractory multiple myeloma: a multicentre, randomised, double-blind phase 3 trial. Lancet Oncol. J Clin Oncol. Epigenetics in focus: pathogenesis of myelodysplastic syndromes and the role of hypomethylating agents. Crit Rev Oncol Hematol.

Vorinostat, a histone deacetylase inhibitor, combined with pelvic palliative radiotherapy for gastrointestinal carcinoma: the Pelvic Radiation and Vorinostat PRAVO phase 1 study. Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors.


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Clin Cancer Res. Phase I trial of histone deacetylase inhibition by valproic acid followed by the topoisomerase II inhibitor epirubicin in advanced solid tumors: a clinical and translational study. A phase I pharmacokinetic and pharmacodynamic study of CHR, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. DNA methyltransferase inhibitor, zebularine, delays tumor growth and induces apoptosis in a genetically engineered mouse model of breast cancer.

Mol Cancer Ther. Mol Oncol. Chronic oral administration of CI a phase 1 study. Invest New Drugs. Undevia SD. A phase I study of the oral combination of CI, a putative histone deacetylase inhibitor, and capecitabine. Ann Oncol. Reactivation of tumor suppressor genes by the cardiovascular drugs hydralazine and procainamide and their potential use in cancer therapy.

Molecular modeling and molecular dynamics studies of hydralazine with human DNA methyltransferase 1. Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells. EMBO J.


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Lane A, Chabner B. Histone deacetylase inhibitors in cancer therapy. Phase I trial of a new schedule of romidepsin in patients with advanced cancers.

1. Introduction

Karahoca M, Momparler RL. Clin Epigenetics.

A proof-of-principle study of epigenetic therapy added to neoadjuvant doxorubicin cyclophosphamide for locally advanced breast cancer. PLoS One. A phase II study of epigenetic therapy with hydralazine and magnesium valproate to overcome chemotherapy resistance in refractory solid tumors. A double-blind, placebo-controlled, randomized phase III trial of chemotherapy plus epigenetic therapy with hydralazine valproate for advanced cervical cancer. Preliminary results 1.

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Press Releases

Combination epigenetic therapy has efficacy in patients with refractory advanced non-small cell lung cancer. Cancer Discov. Cancer Chemother Pharmacol. Gerson SL. MGMT: its role in cancer aetiology and cancer therapeutics. Marks PA. Discovery and development of SAHA as an anticancer agent. Phase I-II study of vorinostat plus paclitaxel and bevacizumab in metastatic breast cancer: evidence for vorinostat-induced tubulin acetylation and Hsp90 inhibition in vivo. Breast Cancer Res Treat.

Milestones in Cancer Research and Discovery - National Cancer Institute

Molecular and biologic analysis of histone deacetylase inhibitors with diverse specificities. Phase I study of epigenetic modulation with 5-azacytidine and valproic acid in patients with advanced cancers. First-in-human, pharmacokinetic and pharmacodynamic phase i study of resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. Oral Oncol. A pilot phase II study of valproic acid for treatment of low-grade neuroendocrine carcinoma.

Combination therapy with vidaza and entinostat suppresses tumor growth and reprograms the epigenome in an orthotopic lung cancer model. Cancer Res. Phase II trial of the histone deacetylase inhibitor belinostat in women with platinum resistant epithelial ovarian cancer and micropapillary LMP ovarian tumours. Eur J Cancer. Epigenetic resensitization to platinum in ovarian cancer.

Bibliographic Information

Phase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group study. Phase 1 clinical trial of the novel proteasome inhibitor marizomib with the histone deacetylase inhibitor vorinostat in patients with melanoma, pancreatic and lung cancer based on in vitro assessments of the combination.

Diaz LA, Bardelli A. Liquid biopsies: genotyping circulating tumor DNA. Histone acetylation and histone deacetylase activity of magnesium valproate in tumor and peripheral blood of patients with cervical cancer. A phase I study.