Search Results - "Sinnamon, Robert H."
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Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
Published in Nature chemical biology (01-03-2014)“…Allosteric small-molecule inhibitors of the p53-induced oncogenic phosphatase Wip1 bind at a ‘flap’ subdomain near the catalytic site. Inhibitor GSK2830371…”
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Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions
Published in PloS one (03-07-2013)“…Mitogen-Activated Protein Kinase (MAPK) pathway activation has been implicated in many types of human cancer. BRAF mutations that constitutively activate MAPK…”
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Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase
Published in Journal of medicinal chemistry (11-08-2016)“…Undecaprenyl pyrophosphate synthase (UppS) is an essential enzyme in bacterial cell wall synthesis. Here we report the discovery of Staphylococcus aureus UppS…”
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C-terminal region of USP7/HAUSP is critical for deubiquitination activity and contains a second mdm2/p53 binding site
Published in Archives of biochemistry and biophysics (15-11-2010)“…► Deletion of the N-terminal TRAF-like domain of USP7 has no effect on USP7 mediated deubiquitination of Ub n-mdm2 and Ub n-p53. ► Amino acids 208–1102 were…”
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A Biochemical Rationale for the Anticancer Effects of Hsp90 Inhibitors: Slow, Tight Binding Inhibition by Geldanamycin and Its Analogues
Published in Proceedings of the National Academy of Sciences - PNAS (16-05-2006)“…Heat shock protein (Hsp)90 is emerging as an important therapeutic target for the treatment of cancer. Two analogues of the Hsp90 inhibitor geldanamycin are…”
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Cocktailed fragment screening by X‐ray crystallography of the antibacterial target undecaprenyl pyrophosphate synthase from Acinetobacter baumannii
Published in Acta crystallographica. Section F, Structural biology communications (01-01-2020)“…Direct soaking of protein crystals with small‐molecule fragments grouped into complementary clusters is a useful technique when assessing the potential of a…”
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Characterization of PI3K class IA isoforms with regulatory subunit p55α using a scintillation proximity assay
Published in Analytical biochemistry (15-12-2008)“…Differential activation of the phosphoinositide 3-kinase (PI3K)/AKT pathway has been linked to cancer. Activation occurs through gene amplification and…”
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Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85α–p110α fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors
Published in Protein expression and purification (01-10-2010)“…Phosphoinositide 3-kinases have been targeted for therapeutic research because they are key components of a cell signaling cascade controlling proliferation,…”
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9
Characterization of PI3K class IA isoforms with regulatory subunit p55alpha using a scintillation proximity assay
Published in Analytical biochemistry (15-12-2008)“…Differential activation of the phosphoinositide 3-kinase (PI3K)/AKT pathway has been linked to cancer. Activation occurs through gene amplification and…”
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Journal Article -
10
Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors
Published in Protein expression and purification (01-10-2010)“…Phosphoinositide 3-kinases have been targeted for therapeutic research because they are key components of a cell signaling cascade controlling proliferation,…”
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11
Effects of oncogenic p110alpha subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase
Published in Biochemical journal (15-01-2008)“…The PIK3CA gene, encoding the p110alpha catalytic subunit of Class IA PI3Ks (phosphoinositide 3-kinases), is frequently mutated in many human tumours. The…”
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