background: the secondary genetic changes other than the promyelocytic leukemia-retinoic acid receptor (pml-rara) fusion gene may contribute to the acute promyelocytic leukemogenesis. chromosomal alterations and mutation of flt3 (fms-like tyrosine kinase 3) tyrosine kinase receptor are the frequent genetic alterations in acute myeloid leukemia. however, the prognostic significance of flt3 mutat...

introduction: tyrosine kinase inhibitors (tkis) were the first drugs to use an intracellular signaling molecule as a therapeutic target. unresponsiveness to tkis limits therapeutic options, making allogeneic hematopoietic stem cell transplantation (hsct) the only option leading to molecular remission. objectives: to characterize cml patients unresponsive to first- and/or second-generation tki t...

introduction: gastrointestinal stromal tumors (gists) are the most common mesenchymal neoplasms of the gastrointestinal tract. gist has been shown to over-express c-kit (cd117), the receptor tyrosine kinase. imatinib (sti571 or glivec) is a new type of tyrosine kinase inhibitor that selectively inhibits various tyrosine kinases and has been successfully used to treat gist. in this study we have...

introduction: the secondary genetic changes other than the pml-rara fusion gene may contribute to the acute promyelocytic leukemogenesis. chromosomal alterations and mutation of flt3 tyrosine kinase receptor are the frequent genetic alterations in acute myeloid leukemia (aml). however, the prognostic significance of flt3 mutations in acute promyelocytic leukemia (apl) is not firmly established....

OBJECTIVE Somatic mutations in the epidermal growth factor receptor gene are associated with a therapeutic response to epidermal growth factor receptor tyrosine kinase inhibitors such as gefitinib and erlotinib in patients with non-small cell lung cancer. Although the safety profile of these drugs is favorable, a small proportion of patients with EGFR mutation-positive non-small cell lung cance...

Gefitinib is a selective tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) used for the treatment malignant neoplasms. The most frequent skin complication during gefitinib therapy an acneiform papulopustular eruption, usually distributed in seborrheic areas but occasionally widespread. We report patient with erosive pustular dermatosis scalp, neutrophil-mediated disease prese...

BACKGROUND The tyrosine kinase inhibitors (TKI) sunitinib and imatinib were shown to induce macrocytosis in patients with renal cell cancer (RCC) and gastrointestinal stromal tumors (GIST), presumably through inhibition of the c-KIT dependent signaling pathway of erythroid progenitor cells of the bone marrow. PATIENTS AND METHODS Hematology charts of patients with RCC, breast cancer (BC), GIS...

lung cancer is still diagnosed in advanced stage and most patients do not have the opportunity for surgical treatment. although in the recent years new diagnostic equipment is available such as the radial and linear endobronchial ultrasound (ebus) and electromagnetic fiberoptic bronchoscopy. however; novel targeted therapies with tyrosine kinase inhibitors of second generation and immunotherapy...

mpns including a heterogeneous group of clonal or oligoclonal hamtopathies characterized by proliferation and accumulation of mature myeloid cells. jak2 tyrosine kinase mutation is the most common molecular lesion identified in 90% of cases. jak2 is involved in epo signaling pathway, and mutations in it lead to epo-independent spontaneous phosphorylation. most tyrosine kinase inhibitors (tki) a...

Src is a non-receptor tyrosine kinase (TK) whose involvement in cancer, including glioblastoma (GBM), has been extensively demonstrated. In this context, we started from our in-house library of pyrazolo[3,4-d]pyrimidines that are active as and/or Bcr-Abl TK inhibitors and performed lead optimization study to discover new generation derivative suitable for targeting. We synthesized 19 compounds,...