The gene family of protein phosphatases is a rich but under-exploited source therapeutically validated drug targets modulating signal transduction pathways. Unlike the kinase family, research and development activities have not yet yielded any approved small-molecule drugs against phosphatase. Approximately 20 years ago, phosphatase was classified as undruggable intractable. This primarily due ...

a series of 42 pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinaseinhibitors regarded as promising antitumor agents to complement the existing therapies, wassubjected to a three-dimensional quantitative activity relationship (3d qsar). different qsarmethods, comparative molecular field analysis (comfa), comfa region focusing, andcomparative molecular similarity indices an...

The UL97-encoded protein kinase (pUL97) of human cytomegalovirus (HCMV) plays a critical role in the control of virus replication. Deletion of the UL97 gene results in a drastic reduction in the replication efficiency. Although the exact function of pUL97 remains unclear and its sensitivity to specific inhibitors is speculative, protein kinase inhibitors of the indolocarbazole class are effecti...

antiproliferative protein (app) isolated from conditioned media of two androgen-independent prostatic carcinoma cell lines, pc3 and du-145 was shown to inhibit selectively cell proliferation of androgen-dependent prostate cancer cell line lncap in a dose dependent manner. this protein was further purified with hplc using hydrophobic interaction column (phenyl 5pw) and was used to study the modu...

Background: All cellular events depend upon the DNA synthesis and gene expression involving complex interplay between ligands such as interleukins and interferons, with various cell membrane receptors. These ligand-receptors interactions transmit signals within the cell via numerous signal transduction pathways to affect gene expression. Janus kinase/signal transducer and activator of transcrip...

Epithelioid glioblastoma is a rare and aggressive variant of that common in children young adults. This frequently has BRAF V600E mutation, recent years, this often treated with mitogen-activated protein kinase inhibitors. An 18-year-old female initially presented headaches vomiting. They were diagnosed an epithelioid temozolomide chemoradiotherapy. Upon progression, they had to redo surgery th...

We have identified a strain of Streptomyces in which aerial hyphae formation appears to be especially sensitive to inhibition by protein kinase inhibitors. Using this assay, a number of bacterial cultures have been screened and novel inhibitors of eukaryotic protein kinases have been identified. Since M. tuberculosis possesses multiple eukaryotic-like protein kinase genes, we tested the active ...

The specificities of 28 commercially available compounds reported to be relatively selective inhibitors of particular serine/threonine-specific protein kinases have been examined against a large panel of protein kinases. The compounds KT 5720, Rottlerin and quercetin were found to inhibit many protein kinases, sometimes much more potently than their presumed targets, and conclusions drawn from ...