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  • covalent
  • Using a covalent inhibitor of cyclin-dependent kinase 7 (CDK7) to disrupt the transcription of amplified MYCN in neuroblastoma cells, we demonstrate downregulation of the oncoprotein with consequent massive suppression of MYCN-driven global transcriptional amplification. (nih.gov)
  • These epigenetic regulatory mechanisms include covalent modifications of histones, ATP hydrolysis-dependent chromatin remodeling activities, substitutions of the core (major) histones with their related variant (minor) histones, and DNA methylation. (sigmaaldrich.com)
  • Ribociclib
  • The addition of ribociclib, an inhibitor of the cell cycle, to standard hormone therapy significantly improved progression-free survival (PFS) in pre-menopausal patients with advanced hormone receptor-positive (HR+) breast cancer, according to results of the MONALEESA-7 Phase III clinical trial led by researchers at The University of Texas MD Anderson Cancer Center . (mdanderson.org)
  • The trial results, presented today at the 2017 San Antonio Breast Cancer Symposium by Debu Tripathy, M.D. , chair of Breast Medical Oncology , also show a greater overall response rate (ORR), a delay in patient-reported quality-of-life (QOL) deterioration and manageable treatment side effects with ribociclib compared to hormone therapy alone. (mdanderson.org)
  • Patients were randomized to receive either ribociclib (335) or placebo (337) in combination with tamoxifen or a nonsteroidal aromatase inhibitor (NSAI), and goserelin, an ovarian suppression drug. (mdanderson.org)
  • However, there has been no study to investigate effects of a selective CDK 4/6 inhibitor, Ribociclib (LEE011), in thyroid cancer. (yonsei.ac.kr)
  • assay
  • Here we introduce a simple screening system based on zFRase activity as a primary readout and a following robust invasion assay and lysosomal distribution analysis for the identification of compounds that can inhibit ErbB2‐induced invasion. (pubmedcentralcanada.ca)
  • cancers
  • This has resulted in the conclusion that most, if not all, cancers exhibit one or more cell cycle defects ( Sherr, 1996 ), and that effective cancer therapy will require restoring normal cell cycle control. (aspetjournals.org)
  • While "targeted therapy" has made significant progress in treatment of blood cancers, we continue to treat DLBCL with standard chemotherapy regimens, which are associated with significant side effects and high rate of failure. (lls.org)
  • genes
  • We used a systematic gain-of-function approach to identify genes whose upregulation confers resistance to the PI3K inhibitor BYL719 in breast cancer cells. (aacrjournals.org)
  • Among the validated resistance genes, Proviral Insertion site in Murine leukemia virus (PIM) kinases conferred resistance by maintaining downstream PI3K effector activation in an AKT-independent manner. (aacrjournals.org)
  • Clinical
  • Viral Therapy of Cancer illustrates this point very well with almost the entire gamut of bioscience and clinical expertise represented by the contributors. (spotidoc.com)
  • Eventually, we hope this work can define MMSC markers in clinical samples and to use this knowledge to develop a novel therapy to prevent MM relapse. (lls.org)
  • We also observed increased PIM expression and activity in a subset of breast cancer biopsies with clinical resistance to PI3K inhibitors. (aacrjournals.org)
  • One of these highly active anti-cancer agents was CCT68127, a pre-clinical stage CDK2/9 inhibitor developed by Cyclacel Pharmaceuticals, Inc. It offers an innovative approach to combating aneuploid cancer cells - those that contain abnormal numbers of chromosomes. (mdanderson.org)
  • Study findings were replicated using Cyclacel's clinical stage next-generation CDK2/9 inhibitor, CYC065, and were published in the Feb. 10 online issue of the Journal of the National Cancer Institute (JNCI). (mdanderson.org)
  • cancer therapy
  • This essay focuses on one well-studied epigenetic control, histone (de)acetylation, and the recent development of cancer therapy aiming at altering the balance of histone and protein acetylation. (sigmaaldrich.com)
  • Therefore, selective inactivation of FGFRs is an important strategy for cancer therapy. (biomedcentral.com)
  • Cancer therapy is one of the fastest growing segments in the pharmaceutical industry, which itself is undergoing a major shift from conventional chemotherapy and radiotherapy to specific agents aimed at targeting abnormalities that are specific to cancer cells. (biomedcentral.com)
  • CCT68127 and CYC065, currently in a Phase I study, are the next-generation drugs being developed in the line of CDK cancer therapy inhibitors. (mdanderson.org)
  • mechanisms
  • These creative ways to develop CDK inhibitors are presented along with crystal structures of these agents complexed with CDK2 to highlight differences in their binding sites and mechanisms of action. (aspetjournals.org)
  • antiapoptotic
  • By combining anti-inflammatory, antiapoptotic and pro-proliferative functions, A20-based therapies could be beneficial in prevention and treatment of FHF. (garvan.org.au)
  • cells
  • B) Dose-response curves of NB cells treated as in (A) with the reversible CDK7 inhibitor THZ1R. (nih.gov)
  • In addition, a p53-independent branch of the DNA damage checkpoint is activated that involves the Chk1 kinase and arrests cells solely before mitosis ( 1 ). (aacrjournals.org)
  • development
  • The purpose of this review is to provide a broad overview of the development of various classes of CDK inhibitors. (aspetjournals.org)
  • The current review focuses on the aberrant hepatoepigenetics events that play important roles in hepatocarcinogenesis and their utilities in the development of HCC therapy. (hindawi.com)
  • Gene Therapy
  • 2. Gene Therapy. (spotidoc.com)
  • This new therapy was born out of the new biology, termed gene therapy and presented the biomedical community with the possibility of a quantum change in therapeutics. (spotidoc.com)
  • Gene therapy represents the ultimate multidisciplinary activity. (spotidoc.com)
  • The book focuses on cancer and the use of viruses, both as vectors and as therapeutic agents, the latter strategy having grown out of the early days of gene therapy when viral vectors seemed to be the only possible way forward. (spotidoc.com)
  • control
  • Using the well‐established and clinically relevant ErbB1 and ErbB2 inhibitor lapatinib as a positive control, we studied their ability to inhibit ErbB2‐induced invasion in 3‐dimensional Matrigel cultures. (pubmedcentralcanada.ca)
  • breast cancer
  • This is the first study that tells us we can reliably use CDK inhibitors in pre-menopausal patients, which represent about 20 percent of all breast cancer patients in the U.S.," said Tripathy. (mdanderson.org)