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...

Erk1/Erk2 MAP kinases are key regulators of cell behaviour and their activation is generally associated with tyrosine kinase signalling. However, TGF-beta stimulation also activates Erk MAP kinases through an undefined mechanism, albeit to a much lower level than receptor tyrosine kinase stimulation. We report that upon TGF-beta stimulation, the activated TGF-beta type I receptor (TbetaRI) recr...

Growth hormone receptor (GHR) forms a complex with a tyrosine kinase, suggesting involvement of a ligand-activated tyrosine kinase in intracellular signaling by growth hormone (GH). Here we identify JAK2, a nonreceptor tyrosine kinase, as a GHR-associated tyrosine kinase. Immunological approaches were used to establish GH-dependent complex formation between JAK2 and GHR, activation of JAK2 tyro...

In a high proportion of human carcinomas overexpression of the EGFR (epidermal growth factor receptor), a receptor tyrosine kinase, represents a potential target for cancer treatment. EGFR is induced to dimerize through ligand binding which activates the tyrosine kinase activity of the receptor. This catalyses the transfer of ATP's gamma-phosphate to hydroxyl groups of tyrosine residues on the ...

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...

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,...

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...

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...

Increasing evidence supports the hypothesis that tannic acid, a plant polyphenol, exerts anticarcinogenic activity in chemically induced cancers. In the present study, tannic acid was found to strongly inhibit tyrosine kinase activity of epidermal growth factor receptor (EGFr) in vitro (IC50 = 323 nM). In contrast, the inhibition by tannic acid of p60(c-src) tyrosine kinase (IC50 = 14 microM) a...

INTRODUCTION Non-small-cell lung cancer harboring an activated epidermal growth factor receptor mutation exhibits a good response to epidermal growth factor receptor-tyrosine kinase inhibitors; however, clinicians often experience treatment failure following the development of resistance to epidermal growth factor receptor-tyrosine kinase inhibitor. CASE PRESENTATION We here report a case of ...