title: [Tyrosine kinase inhibitors (TKI): a new revolution in the treatment of chronic myeloid leukemia (CML)].
abstract: Chronic myeloid leukemia (CML) is a clonal myeloproliferative neoplasia associated with the t(9,22)(q34:q11) reciprocal translocation, also known as Philadelphia chromosome (Ph). As a result of such abnormality, a chimeric gene (bcr-abl) is produced that is translated into a chimeric protein (BCR-ABL), a constitutively activated tyrosine kinase. Major cell dysfunctions result from this abnormal kinase activity, including increased proliferation and reduced apoptosis. Based on the structure of BCR-ABL, several molecules have been designed that inhibit its kinase activity. Five such molecules have already been brought into the clinic for the treatment of Ph+ CML patients. Good results have been obtained in terms of patients' remission rates and quality of life. Some major problems, however, have been observed. Firstly, a significant proportion of patients develop resistance to the drugs; secondly, it is clear that such drugs affect most of the leukemic cells, but do not eliminate leukemia stem cells. Thus, important CML-related challenges remain to be solved in the near future.
authors.affiliation: Unidad de Investigación Médica en Enfermedades Oncológicas, Hospital de Oncología, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social (IMSS), México, D.F. hmayaniv@prodigy.net.mx.
authors.forename: Sócrates
authors.initials: S
authors.lastname: Avilés-Vázquez
authors.forename: Antonieta
authors.initials: A
authors.lastname: Chávez-González
authors.forename: Héctor
authors.initials: H
authors.lastname: Mayani
mesh_terms: D001549:Benzamides / Q000627:therapeutic use; D019008:Drug Resistance, Neoplasm; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy*; D010879:Piperazines / Q000627:therapeutic use; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000627:therapeutic use
chemical_list: D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases