Inibidores de tirosino quinase na leucemia mieloide crônica

Lopes, Nei R; Abreu, Maria Theresa Cerávolo Laguna

doi:10.1590/s1516-84842009005000089

Cited by 13 publications

(30 citation statements)

References 22 publications

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“…This reduces tumoral proliferation, and also causes the blocking of the various cellular signaling routes activated by the protein. Imatinib has shown long-lasting effects during the chronic phase of CML [4] ; however the same results have not been obtained when the treatment was used in more advanced phases of the disease, such as the acute phase and the blast crisis [11] .…”

Section: Imatinibmentioning

confidence: 97%

“…Compounds based on 2-phenylaminopyrimidine show high inhibitory potential towards the BCR-ABL gene, acting specifically to block energy transfer to the tyrosine kinase domain, while not inhibiting other tyrosine kinases such as those of the Src kinase family and the T315I mutation of Abl [4] . Imatinib and nilotinib belong to this group of drugs.…”

Section: Compounds Based On 2-phenylaminopyrimidinementioning

confidence: 99%

“…These compounds are inhibitors of the Src family of kinases, which also show inhibitory properties towards Abl, but are not able to inhibit the T315I mutation of Abl [4] . Members of this group of drugs include dasatinib, bosutinib, AP23464, and PD166326.…”

Section: Src/abl Inhibiting Compoundsmentioning

confidence: 99%

“…The inhibitors that are competitive to the ATP binding site can be divided into two subclasses: compounds based on 2-phenylaminopyrimidine, and Src-Abl inhibitors. Inhibitors that do not use the ATP binding site, considered ATP-non-competitive, have been developed to inhibit phosphorylation of the T315I mutation of the BCR-ABL gene, since it has been shown that the competitive inhibitors remain unable to perform this function [4] .…”

mentioning

confidence: 99%

“…Meanwhile, the effects of these medicines can vary between patients, and with the specific spectrum of kinases on which they act, since the drugs also affect other kinases involved in the activation of immune effector cells [4,5] .…”

mentioning

confidence: 99%

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Immunological implications of the use of tyrosine kinase inhibitors in chronic myeloid leukemia

et al. 2012

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Background: The treatment of chronic myeloid leukemia (CML) employs drugs known as tyrosine kinase inhibitors (TKIs). Comparative analyses of the effects of different TKIs has shown that these substances can reduce the immunogenicity of leukemic cells, and prejudice anti-tumoral immunity. Once the TKIs differ in terms of their direct influence on cells of the immunological system, the objective of this work was therefore to analyze alterations in the immunological systems of CML patients using different TKI drugs. Methodology/Principal findings:A review of the literature revealed that imatinib is considered to be the new paradigm for treatment of CML; however, use of this drug can result in inhibition of activation of immune system cells and development of resistance. Second and third generation TKIs can be used in the treatment of patients resistant to imatinib, but can have immunosuppressor effects. Nilotinib is more effective than imatinib in recently-diagnosed patients, however at high doses can induce myelosuppression and diminish cytokine production. Dasatinib was found to induce a rapid full cytogenetic response, with heightened in vivo immune-stimulation, in contrast to an immunosuppression observed in vitro. The mutated T315I phenotype of CML only shows a response to treatment with inhibitors that do not compete with ATP, involving aurora kinases that control mitosis, progression of the cellular cycle, and apoptosis induction. MK0457, which is able to act in the presence of the mutation, presents important bone marrow toxicity, while in small doses danusertib has shown anti-proliferative and pro-apoptotic activity against a wide spectrum of BCR-ABL-positive cells.Conclusions/Significance: Selection of the most suitable tyrosine kinase inhibitor in patients showing positive to the BCR-ABL mutation requires previous analysis of the phenotype and the influence of the TKI on the immunological system.

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Section: Imatinibmentioning

confidence: 97%

Section: Compounds Based On 2-phenylaminopyrimidinementioning

confidence: 99%

Section: Src/abl Inhibiting Compoundsmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Immunological implications of the use of tyrosine kinase inhibitors in chronic myeloid leukemia

et al. 2012

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Molecular biology as a tool for the treatment of cancer

Anna¹,

Ferreira²,

Soares³

et al. 2018

Clin Exp Med

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Cancer is a genetic disease characterized by uncontrolled cell growth and metastasis. Cancer can have a number of causes, such the activation of oncogenes, the inactivation of tumor-suppressing genes, mutagenesis provoked by external factors, and epigenetic modifications. The development of diagnostic tools and treatments using a molecular biological approach permits the use of sensitive, low-cost, noninvasive tests for cancer patients. Biomarkers can be used to provide rapid, personalized oncology, in particular the molecular diagnosis of chronic myeloid leukemia, and gastric, colon, and breast cancers. Molecular tests based on DNA methylation can also be used to direct treatments or evaluate the toxic effects of chemotherapy. The adequate diagnosis, prognosis, and prediction of the response of cancer patients to treatment are essential to ensure the most effective therapy, reduce the damaging effects of treatment, and direct the therapy to specific targets, and in this context, molecular biology has become increasingly important in oncology. In this brief review, we will demonstrate the fundamental importance of molecular biology for the treatment of three types of cancer-chronic myeloid leukemia, hereditary diffuse gastric cancer, and astrocytomas (sporadic tumors of the central nervous system). In each of these three models, distinct biological mechanisms are involved in the transformation of the cells, but in all cases, molecular biology is fundamental to the development of personalized analyses for each patient and each type of neoplasia, and to guarantee the success of the treatment.

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Expressão dos genes da via de sinalização celular hippo e aurora quinases na leucemia mielóide crônica

Marsola¹

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Inibidores de tirosino quinase na leucemia mieloide crônica

Cited by 13 publications

References 22 publications

Immunological implications of the use of tyrosine kinase inhibitors in chronic myeloid leukemia

Immunological implications of the use of tyrosine kinase inhibitors in chronic myeloid leukemia

Molecular biology as a tool for the treatment of cancer

Expressão dos genes da via de sinalização celular hippo e aurora quinases na leucemia mielóide crônica

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