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  • transcriptional
  • BTB and CNC homology 2 (Bach2) is a transcriptional repressor that is required for the formation of the germinal center (GC) and reactions, including class switch recombination and somatic hypermutation of Ig genes in B cells, within the GC. (jimmunol.org)
  • miRNAs represent an abundant class of small, non-coding RNAs involved in global post-transcriptional regulation and, consequently, play an integral role at multiple steps in carcinogenesis, including cell cycle progression, proliferation, apoptosis, invasion, and metastasis. (frontiersin.org)
  • We describe the characterization of the transcriptional inhibitor class in terms of kinase inhibition profile, cellular mode of action, and selectivity for transformed cells. (rcsb.org)
  • A structural selectivity rationale was used to optimize potency and biopharmaceutical properties and led to the development of a transcriptional inhibitor, 3,4-dimethyl-5-[2-(4-piperazin-1-yl-phenylamino)-pyrimidin-4-yl]-3H-thiazol-2-one, with anticancer activity in animal models. (rcsb.org)
  • By antagonizing Mdm2, a negative regulator of the p53 tumor suppressor, ARF triggers a p53-dependent transcriptional response that diverts incipient cancer cells to undergo growth arrest or apoptosis. (aacrjournals.org)
  • degradation
  • In both fungi and metazoans, it is well established that CKI degradation at the G1-to-S transition releases CDK activity, which in turn is required to enter S phase. (plantcell.org)
  • 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)
  • toxicities
  • Three recent reviews provide comprehensive recommendations for the management of cancer treatment-related toxicity, including the ESMO guideline on diagnosis, treatment, and follow-up for immunotherapy toxicity, recommendations for potential CDK 4/6 inhibitor-related toxicities and drug interactions in breast cancer, and an update to ASCO antiemetics guidelines. (primeoncology.org)
  • Recommendations for Management of Potential CDK 4/6 Inhibitor-Related Toxicities and Drug Interactions in Breast Cancer. (primeoncology.org)
  • This class of therapy is associated with a unique, but easily manageable toxicity profile, primarily comprised of hematologic toxicities, including neutropenia. (primeoncology.org)
  • This review summarizes the current literature regarding the safety and efficacy of CDK 4/6 inhibitors in HR-positive, HER2-negative breast cancer and discusses strategies to manage the toxicities and drug interactions associated with these agents. (primeoncology.org)
  • Ibrance
  • That continuous dosing is something Lilly believes could give the drug an advantage of rival inhibitors in the same space, including Pfizer's Ibrance and Novartis' Kisqali. (biospace.com)
  • accumulation
  • Finally, we show that multiprotein complex formation involving p45 SKP2 -CUL‐1 and p19 SKP1 is governed, in part, by periodic, S phase‐specific accumulation of the p45 SKP2 subunit and by the p45 SKP2 ‐bound cyclin A-CDK2. (embopress.org)
  • transcriptionally
  • The defensive functions promoted by LGOoe in sepals overlap with functions recently shown to be transcriptionally activated by hyperimmune cpr5 mutants in a LGO-dependent manner. (frontiersin.org)
  • suppress
  • Pre-menopausal patients also have been treated with hormone therapy and CDK4/6 inhibitors, in addition to drugs that suppress ovarian production of estrogen, but there previously was a lack of data to confirm the utility of this approach, explained Tripathy. (mdanderson.org)
  • cancer
  • The examined inhibitors were effective in stopping the growth of lung cancer by targeting anaphase catastrophe. (mdanderson.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)
  • 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)
  • Cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors in combination with hormone therapy have recently become a standard treatment for hormone receptor (HR)-positive and HER2-negative breast cancer based on their significant clinical benefit. (primeoncology.org)
  • A new class of oral drugs for treating the most common type of breast cancer, known as cyclin-dependent kinase (CDK) inhibitors, appears to have fewer adverse events and side effects for most patients compared to other treatments. (medshadow.org)
  • Some of the non-biological drugs, known as Cyclin-dependent kinase (CDK) inhibitors, are currently being tested for use in cancer treatment. (thefreedictionary.com)
  • Three CDK4/6 inhibitors have been approved by the Food and Drug Administration (FDA) for combination treatment with standard hormone therapies, known as aromatase inhibitors, in post-menopausal women with advanced HR+ breast cancer. (mdanderson.org)
  • 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)
  • Non‐selective CDK inhibitors showed disappointing results in the clinic due to lack of efficacy across different cancer types and excessive toxicity. (embopress.org)
  • The Company is also developing ME-344, a novel mitochondrial inhibitor currently in an investigator-sponsored study in combination with bevacizumab for the treatment of HER2-negative breast cancer. (yahoo.com)
  • reduction
  • A strain of S. cerevisiae over-expressing mevalonate kinase was used to establish conditions for reduction of background interference. (ebscohost.com)
  • Indication
  • 15. MONACON # Product Company Phas e Pharmacological Class WW 2022 Sales ($m) NPV ($bn) Indication 1 Ocrevus Roche Filed Anti-CD20 Mab 3,962 16,965 MS 2 Dupilumab Sanofi Ph. (slideshare.net)