Imatinib is an orally administered tyrosine kinase inhibitor which inhibits the Bcr-Abl protein-tyrosine kinase with high selectivity. Imatinib is rapidly absorbed from the gut, after oral intake and has an almost absolute bioavailability of 98%. The metabolism of imatinib is mediated by the cytochrome P450 (CYP) isoenzymes in the liver and gut wall. CGP74588 is a major active metabolite of ima...

Recently, anti-cancer targeting drugs are directed against specific molecules and signaling pathways. These agents have reasonable specificity, efficacy less side effects. Tyrosine kinases, which play an essential role in growth factor regulation, significant targets this type of therapy. Synthesized numerous tyrosine-kinase inhibitors (TKIs), such as substituted indolin-2-ones, effective anti-...

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...

Background: When Staphylococcus aureus is grown in the presence of high concentration of external glucose, this sugar is phosphorylated by glucokinase (glkA) to form glucose-6-phosphate. This product subsequently enters into anabolic phase, which favors biofilm formation. The presence of ROK (repressor protein, open reading frame, sugar kinase) motif, phosphate-1 and -2 sites, and tyrosine kina...

Dominant mutations or DNA amplification of tyrosine kinases are rare among the oncogenic alterations implicated in prostate cancer. We demonstrate that castration-resistant prostate cancer (CRPC) in men exhibits increased tyrosine phosphorylation, raising the question of whether enhanced tyrosine kinase activity is observed in prostate cancer in the absence of specific tyrosine kinase mutation ...

Suppression of Akt (Protein kinase B) has been implicated in schizophrenia, the effect which has been documented to be reversed by tyrosine phosphatase inhibition. T hus, present study has been designed to study the effect of sodium orthovanadate, a tyrosine phosphatase inhibitor, on protracted methionine administration induced schizophrenia like behavior in rats.   Schizophrenia...

Chemotherapy-induced peripheral neuropathy (CIPN) is a well-documented toxicity leading to dose limitation. Ibrutinib an oral Bruton’s Tyrosine Kinase (BTK) inhibitor approved for treating chronic lymphocytic lymphoma. The most common neurological side effects of include headache and dizziness. Herein, we report as dose-limiting manifestation treatment.

This work presents a simple, low-cost and reusable label-free method for detecting protein tyrosine kinase activity using a tyrosinase-based amperometric biosensor (tyrosine kinase biosensor). This method is based on the observation that phosphorylation can block the tyrosinase-catalyzed oxidation of tyrosine or tyrosyl residue in peptides. Therefore, the activity of p60c-src protein tyrosine k...