Identifying novel protein kinase inhibitors

design and synthesis of novel (e)-2-(4-fluorophenyl)-2-(hydroxyimino)-1-(2-(methylthio)pyrimidin-4-yl)ethanone as potential protein kinase inhibitors and identifying cytotoxic effect

Endogenous Protein Kinase Inhibitors

A thermostable inhibition of ATP:protein phosphotransferase (EC 2.7.1.37) (protein kinase) which is present in crude tissue extracts has been resolved by gel chromatography (Sephadex G-100) into two molecular forms. These two forms will be referred to as type I and type II inhibitor. The type I inhibitor (M, = 24,000) is specific for CAMP-dependent protein kinase and corresponds to the inhibito...

New protein kinase inhibitors.

Background: The stomach is an infrequent site of breast cancer metastasis. It may prove very difficult to distinguish a breast cancer metastasis to the stomach from a primary gastric cancer on the basis of clinical, endoscopic, radiological and histopathological features. It is important to make this distinction as the basis of treatment for breast cancer metastasis to the stomach is usually wi...

Rho Kinase Inhibitors as a Novel Treatment for Glaucoma and Ocular Hypertension

In an elegant example of bench-to-bedside research, a hypothesis that cells in the outflow pathway actively regulate conventional outflow resistance was proposed in the 1990s and systematically pursued, exposing novel cellular and molecular mechanisms of intraocular pressure (IOP) regulation. The critical discovery that pharmacologic manipulation of the cytoskeleton of outflow pathway cells dec...

Monitoring of protein kinase inhibitors

Several mechanisms may influence the enhanced glucose uptake in cancer cells, including upregulation of glucose transporters, increase in the hexokinase activity and the protein kinase B, also called Akt, which appears to play key role in the control of glucose metabolism together with proteins which are involved in the signal cascade pathway, such as the mammalian target of rapamycin (mTOR). I...