The protein encoded by this gene is a potent, tight-binding inhibitor of several G1 CDKs, arresting the cells in G1 when overexpressed [41].
5 This gene contains three exons and encodes p57 KIP2), a potent tight-binding inhibitor of several G1 cyclin/Cdk complexes (cyclin E-CDK2, cyclin D2-CDK4, and cyclin A-CDK2).
CDKN1C codifies for CDKN1C/KIP2, a nuclear protein and potent tight-binding inhibitor of several cyclin/Cdk complexes, playing a role in maintenance of the nonproliferative state of cells.
Indeed, pemetrexed and its polyglutamates are potent, tight-binding inhibitors of folate-dependent enzymes, including thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT) and show activity against a wide variety of solid tumours, including bladder cancer (Calvert, 2004).
It is a potent, tight-binding, non-competitive MEK inhibitor with an median inhibitory concentration (IC50) of 14.1 nmol L−1 against purified MEK1 with no observed inhibition at 10 μmol L−1 against >40 other serine/threonine kinases (Davies et al, 2007; Yeh et al, 2007).
Not only is O'Brien tasked with replacing Joe Paterno, the iconic Penn State coach who died this month, but he must also buy a house, recruit players and figure out how to stymie the N.F.L.'s most dangerous pass rush while dealing with an ankle injury to one of his most potent playmakers, tight end Rob Gronkowski.
Brazilian officials are right to worry about the impact of foreign capital flows, but their emphasis on controls and fear of raising rates have distracted them from a more potent tool: tighter fiscal policy.Ms Rousseff's government brags about its fiscal squeeze.
This modest chemical change results in a very significant and unexpected shift in the selectivity of COX inhibition, creating a molecule that is a highly potent, slow, tight-binding inhibitor of COX-2 lacking significant COX-1 inhibitory activity.
Based on this, studies by the research team of Chiron/ University of Washingtonidentified a diphenyl-acetylene-containing hydroxamic acid compound CHIR-090 (Fig. 5), a very potent, slow, tight-binding inhibitor against both E. coli and P. aeruginosa LpxC (McClerren et al., 2005; Barb et al., b).
Conclusions: VEGF alone is twice as potent in interrupting tight junctions in an endothelial cell monolayer as Ang-2.
The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli PDF (KI∗= 4.4nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC = 2 4 μg/mL).
