Lipid nanocapsules (LNCs) represent a stable, biocompatible and worthwhile drug delivery system, demonstrating significant potential as gene/drug delivery platforms for cancer therapy. Imatinib, a potent tyrosine kinase inhibitor, has revolutionized the therapy of malignancies resulting from abnormal tyrosine kinase activity. However, its Clinical effectiveness in cancer treatment is h...

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...

EGFR-TKIs (tyrosine kinase inhibitor) can effectively improve the survival rate of NSCLC patients with EGFR sensitive mutations. However, concomitant alterations along mutations often affect effect EGFR-TKIs. The genome characteristic co-mutation is great significance for guiding clinical treatment. In this study, we first reported genetic characteristics EGFR/RB1/TP53 co-variation in Chinese n...

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...

BE-23372M, a new protein tyrosine kinase inhibitor, has been obtained as a reddish orange solid. The compound, C17H12O6, HRFAB-MS: m/z 312.0625 (M)+, is an acidic substance, showing UV (MeOH) lambda max (epsilon) 266 (8,800), 426 nm (20,400), and IR (KBr)vmax 1752(C = O) and 3298(OH) cm-1. The structure of BE-23372M, (E)-3-(3,4-dihydroxybenzylidene)-5-(3,4-dihydroxyphenyl)-2(3H)-fur anone, has ...

  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 trea...

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...

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 ...

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...