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  • selective
  • In the presence of TKI the binding of ATP is blocked, phosphorylation is prevented and Bcr-Abl expressing cells either have a selective growth disadvantage or undergo apoptotic cell death. (wikipedia.org)
  • Cancer
  • Cyclophosphamide is a prescription medicine used alone, or in combination with other medications to treat several types of cancer including lymphoma, leukemia, ovarian, and breast cancer. (rxwiki.com)
  • Skin cancer and leukemia , which can be fatal, have been reported in patients receiving long-term hydroxyurea for conditions other than sickle cell anemia. (rxwiki.com)
  • Vánky, F. (1976), "Properties of the K562 cell line, derived from a patient with chronic myeloid leukemia", International Journal of Cancer, 18 (4): 421-31, doi:10.1002/ijc.2910180405, PMID 789258 Andersson, L.C. (wikipedia.org)
  • Chronic myelogenous leukemia (CML) is a cancer of the white blood cells. (wikipedia.org)
  • Even though the first Bcr-Abl TK inhibitor was named "the magic bullet" to cure cancer by TIME magazine, a second generation of Bcr-Abl TKI was subsequently developed to combat the initial resistance that emerged. (wikipedia.org)
  • As Musashi2 is involved in the generation of hematopoietic cells, it is also linked with cancer pathologies: It has been found that MSI2 plays an important role in myeloid leukemia. (wikipedia.org)
  • kinase domain
  • Since then crystallographic studies have revealed that imatinib binds to the kinase domain of Abl only when the domain adopts the inactive or "closed" conformation. (wikipedia.org)
  • This is due to the replacement of the myristoylated cap region, which when present induces a conformational change rendering the kinase domain inactive, with a truncated portion of the BCR protein. (wikipedia.org)
  • Proteins
  • Since ABL activates a number of cell cycle-controlling proteins and enzymes, the result of the BCR-Abl fusion is to speed up cell division. (wikipedia.org)
  • blast crisis
  • Blast crisis is diagnosed if any of the following are present in a patient with CML: >20% myeloblasts or lymphoblasts in the blood or bone marrow Large clusters of blasts in the bone marrow on biopsy Development of a chloroma (solid focus of leukemia outside the bone marrow) The only curative treatment for CML is a bone marrow transplant or an allogeneic stem cell transplant. (wikipedia.org)
  • KBM-7 cells were derived from a 39-year-old man with chronic myeloid leukemia in blast crisis. (wikipedia.org)
  • adherence
  • However, another study suggests that bcr:abl over-expression may actually increase cell adherence to cell culture plastic. (wikipedia.org)
  • kinases
  • It is an ATP-competitive Bcr-Abl tyrosine-kinase inhibitor with an additional inhibitory effect on SRc family kinases (including Src, Lyn and Hck). (wikipedia.org)
  • Although the BCR region also expresses serine/threonine kinases, the tyrosine kinase function is very relevant for drug therapy. (wikipedia.org)
  • Different inhibitors have been designed to target different kinases: inhibition of BCR/ABl constitutes the basis of the functioning of drugs like imatinib inhibition of FLT3 is carried out by drugs like lestaurtinib inhibition of JAK2 is carried out by the drug CYT387, which was successful in preclinical trials and is currently undergoing clinical trials. (wikipedia.org)
  • phosphorylation
  • In the presence of TKI the binding of ATP is blocked, phosphorylation is prevented and Bcr-Abl expressing cells either have a selective growth disadvantage or undergo apoptotic cell death. (wikipedia.org)
  • activates
  • Since ABL activates a number of cell cycle-controlling proteins and enzymes, the result of the BCR-Abl fusion is to speed up cell division. (wikipedia.org)
  • Nilotinib
  • The importance of early and deeper molecular responses on the risk of progression and blast crisis has been proven in the DASISION and ENESTnd trials leading to the approval of both dasatinib and nilotinib as first line TKIs along with imatinib in both the National Comprehensive Cancer Network (NCCN) and European Leukemia Net (ELN) guidelines. (rbhh.org)
  • genes
  • Alterations in the expression of cytoskeletal regulatory genes and migration properties of BCP represent early events in the evolution of the disease, from the preleukemic phase to the clinical onset, and suggest new strategies for effective eradication of leukemia. (aacrjournals.org)
  • Bosutinib
  • The positive opinion for bosutinib was based on data from Study 200, a global, single-arm, open-label, multi-cohort, Phase 1/2 study of bosutinib in more than 500 patients with Ph+ CML with separate cohorts for chronic, accelerated and blast phase disease previously treated with one or more prior TKIs. (biospace.com)
  • We are very pleased with this positive recommendation on bosutinib by the CHMP. (biospace.com)
  • Bosutinib is an oral, once-daily, kinase inhibitor, which limits cancer cell growth by inhibiting the Abl and Src signaling pathways.4 Bosutinib was first approved as BOSULIF® in the United States (U.S.) in September 2012 for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance, or intolerance to prior therapy. (biospace.com)
  • subsequently
  • The patient was subsequently tested by RQ-PCR for BCR-ABL on a six-monthly basis [November 2012 (0.00%), March 2013 (0.069%), October 2013 (0.062%), January 2014 (0.008%), September 2014 (0.0024%), December 2015 (0.00%), and June 2016 (0.00%)] ( Figure 1 ). (rbhh.org)
  • Even though the first Bcr-Abl TK inhibitor was named "the magic bullet" to cure cancer by TIME magazine, a second generation of Bcr-Abl TKI was subsequently developed to combat the initial resistance that emerged. (wikipedia.org)