Articles with the keyword: 


Protein Kinase CK2: new perspectives of an old kinase
yarmoluk submitted, created time 1 month 4 weeks (www.discover8.com)
Protein Kinase CK2: new perspectives of an old kinase
Design of specific small molecules that are able to block (inhibit) function of macromolecular targets responsible for the development of certain disorder is the “classic” and most widely used approach in modern drug therapeutics, e.g., in cancer treatment 


Blocking enzyme could help in rare blood cancer
jerry submitted, created time 2 months 3 days (www.reuters.com)
An enzyme that fights some kinds of cancers may foster the growth of a rare type of leukemia that affects babies, U.S. researchers said on Wednesday in a finding that may lead to new drugs for the hard-to-treat disease. There is also talk of applications in Alzheimer's and diabetes.
The enzyme is called glycogen synthase kinase, or GSK3, and blocking it might be an effective way to treat this type of leukemia--for which chemotherapy is characteristically ineffective. Existing drugs used for bipolar disease seem to do a shaky but effective job. 


Researchers unveil vital key to cancer
sea-maid submitted, created time 3 months 2 weeks (www.manchester.ac.uk)
University of Manchester scientists have uncovered the 3D structure of Mps1 – a protein that regulates the number of chromosomes during cell division and thus has an essential role in the prevention of cancer – which will lead to the design of safer and more effective therapies. 
ROCO Kinase Activity Is Controlled by Internal GTPase Function
jerry submitted, created time 5 months 4 days (stke.sciencemag.org)
GTPases have long been known to control the activities of downstream protein kinases. Now this paper shows that the kinase activity of one of these ROCO proteins depends on whether guanosine diphosphate or guanosine triphosphate (GTP) is bound and that the activity is controlled by the adjacent GTPase, which suggests a novel mechanism of intrinsic control. 


Survival of Cancer Cells Is Maintained by EGFR Independent of Its Kinase Activity
jerry submitted, created time 5 months 3 weeks (www.cancercell.org)
Expression of the epidermal growth factor receptor (EGFR), a receptor tyrosine kinase associated with cell proliferation and survival, is overactive in many tumors of epithelial origin. Blockade of the kinase activity of EGFR has been used for cancer therapy; however, by itself, it does not seem to reach maximum therapeutic efficacy. We report here that in human cancer cells, the function of kinase-independent EGFR is to prevent autophagic cell death by maintaining intracellular glucose level through interaction and stabilization of the sodium/glucose cotransporter 1 (SGLT1). 


DNA Damage Signals for p53 Pulses
jerry submitted, created time 5 months 4 weeks (www.sciencedirect.com)
A major challenge of systems biology is to understand how network topology affects protein dynamics in living cells. A new study show that p53 pulses are driven by pulses in the upstream signaling kinases, ATM and Chk2, and that a negative feedback mediated by the phosphatase Wip1 is essential for maintaining the uniform shape of p53 pulses. 
jerry submitted, created time 6 months 2 days (ajp.amjpathol.org)
The hepatocyte growth factor (HGF)/Met signaling system is essential for liver development, homeostasis, and function. In this study, the researchers took advantage of a liver-specific, Met-conditional knockout mouse generated in their laboratory to address the molecular mechanisms of HGF/Met signaling in adult liver progenitor cell (oval cell) biology. It reveals a critical, functional role for Met in oval cell survival through an autocrine mechanism. 


The IB kinase – a bridge between inflammation and cancer
davidd submitted, created time 8 months 2 weeks (www.nature.com)
A potential link between inflammation and cancer has been suspected for over a century, but the exact molecular mechanisms connecting the two remained nebulous. The review proposed that NF-B transcription factors regulated via the IB kinase (IKK) complex play a critical role in coupling inflammation and cancer and have set out to test this hypothesis in mouse models of cancer. 
yarmoluk submitted, created time 8 months 2 weeks (www.discover8.com)
Continuing the protein kinase research, OTAVA keeps discovering new promising inhibitors - ProHit compounds. These sets of compounds are offered to academic institutions and pharmaceutical companies which are interested in their further evaluation. 
OTAVA offers new Death-Associated Protein Kinase 2 (DAPK-2) focused Library.
yarmoluk submitted, created time 1 year 1 day (www.discover8.com)
The library was prepared on the base of Otava and Life Chemicals Stock Collections (about 500,000 compounds total) using receptor-based virtual screening.
Design of the focused libraries consists in Lipinsky/Veber rules filtering and flexible docking in a protein target of certain enzyme family. Further computational analysis for the presence of critical receptor-ligand hydrogen bond(s) and docking score refinement makes our focused libraries good starting point for drug discovery purposes 


An analysis of expression patterns of genes encoding proteins with catalytic activities
saury submitted, created time 1 year 4 months (www.biomedcentral.com)
”The 662 expression patterns discussed here comprised gene products with activities associated with catalysis. Preliminary analysis of these data revealed that a significant number of genes encoding housekeeping functions such as biosynthesis and catabolism were expressed regionally, so they could be used as tissue-specific gene markers. They found no difference in tissue specificity between mRNAs encoding housekeeping functions and those encoding components of signal transduction pathways, as exemplified by the kinases.“ 
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