Non-small cell lung cancer adenocarcinoma in the past decade has targeted therapies as the cornerstone for therapy. In specific patients with epidermal growth factor receptor mutation have three different therapy approaches with the tyrosine kinase inhibitors: erlotinib, gefitinib and afatinib. Nowadays we can use tyrosine kinase inhibitors as second line treatment for squamous cell carcinoma. ...

background: genistein is a soya isoflavone, which is found naturally in legumes, such as soybeans and chickpeas. radiation–induced free radicals in turn impair the antioxidative defense mechanism, leading to an increased membrane lipid peroxidation that results in damage of the membrane bound enzyme and may lead to damage or death of cell. hence, the lipid peroxidation is a good biomarker of da...

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....

The selectivity of Janus kinase inhibitors (JAKis) is still a matter debate, as no JAKi specific for only one (JAK) isoform. Currently approved JAKis in rheumatoid arthritis (RA) all inhibit JAK1, which an effective therapeutic target RA. Although selective JAK1 inhibition seems not to decrease drug efficacy, may modify the safety profile this class. Indeed, balance benefit and risk inhibiting ...

Background and Objective: Targeting KIT PDGFRA with traditional tyrosine kinase inhibitors (TKIs) such as imatinib, sunitinib regorafenib has revolutionized the treatment prognosis of patients diagnosed locally advanced metastatic gastrointestinal stromal tumors (GISTs) but resistance to those therapies represents a major challenge in management progression disease after third line. In this rev...

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,...

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...

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-...