Non-ATP-Mimetic Organometallic Protein Kinase Inhibitor

Non-ATP-Mimetic Organometallic Protein Kinase Inhibitor

Organometallic Pyridylnaphthalimide Complexes as Protein Kinase Inhibitors.

A new metal-containing scaffold for the design of protein kinase inhibitors is introduced. Key feature is a 3-(2-pyridyl)-1,8-naphthalimide "pharmacophore chelate ligand" which is designed to form two hydrogen bonds with the hinge region of the ATP-binding site and is at the same time capable of serving as a stable bidentate ligand through C-H-activation at the 4-position of the electron-defici...

An organometallic protein kinase inhibitor pharmacologically activates p53 and induces apoptosis in human melanoma cells.

Unlike other tumors, melanomas harbor wild-type (WT) p53 but exhibit impaired p53-dependent apoptosis. The mechanisms for the impaired p53 activation are poorly understood but may be linked to the high expression of the p53 suppressor Mdm2, which is found in >50% of melanoma lesions. Here, we describe an organometallic glycogen synthase kinase 3beta (GSK3beta) inhibitor (DW1/2) as a potent acti...

An organometallic inhibitor for glycogen synthase kinase 3.

Replacing natural products with kinetically inert metal complexes may lead to a new class of therapeutics in which a metal center plays the role of an innocent bystander, organizing the orientation of the organic ligands in the receptor space. As an example of this approach, a ruthenium complex is described that copies the binding mode of indolocarbazole protein kinase inhibitors and serves as ...

THE EFFECT OF THEOPHYLLINE ON THE KINETICS OF cAMP-DEPENDENT PROTEIN KINASE CATALYTIC SUBUNIT, cAMP, PROTEIN KINASE INHIBITOR AND THEIR RELATIONSHIP IN LUNG TISSUE

We have investigated the effect of theophylline on the kinetics of the catalytic subunit of protein kinase and related factors in lung tissue. The results show that the point of highest concentration of the C subunit of protein kinase which is active in casein phosphorylation is at 3h of incubation time, but in the presence of 100 Ilg/ InL and 10µg/mL theophylline, this is shifted to I.S an...