FLP-Mediated Activations and Reductions of CO2 and CO
|Author||Ashley, AE; O'Hare, D;|
|Key phrase||Carbon dioxide Carbon monoxide Energy Frustrated Lewis pair Fuels Hydrogenations Sequestration Small molecule activation|
Monocyclic β-lactams are selective, mechanism-based inhibitors of rhomboid intramembrane proteases.
|Abstract||Rhomboids are relatively recently discovered intramembrane serine proteases that are conserved throughout evolution. They have a wide range of biological functions, and there is also much speculation about their potential medical relevance. Although rhomboids are weakly inhibited by some broad-spectrum serine protease inhibitors, no potent and specific inhibitors have been identified for these enzymes, which are mechanistically distinct from and ... [truncated at 450 characters in length]|
|Author||Pierrat, OA; Strisovsky, K; Christova, Y; et al|
|Key phrase||Amino Acid Sequence Animals COS Cells Cercopithecus aethiops Chromatography, High Pressure Liquid Cloning, Molecular Escherichia coli Fluorescent Dyes Gene Expression High-Throughput Screening Assays Kinetics Membrane Proteins Mice Molecular Sequence Data Monobactams Quantitative Structure-Activity Relationship Recombinant Fusion Proteins Serine Proteases Serine Proteinase Inhibitors Small Molecule Libraries Species Specificity Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization Substrate Specificity|
Minitags for small molecules: detecting targets of reactive small molecules in living plant tissues using 'click chemistry'
|Author||Kaschani, F; Verhelst, SHL; van Swieten, PF; et al|
|Key phrase||click chemistry small molecule E-64 papain-like cysteine protease proteasome MG132|
Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.
|Abstract||Human cells utilize a variety of complex DNA repair mechanisms in order to combat constant mutagenic and cytotoxic threats from both exogenous and endogenous sources. The RecQ family of DNA helicases, which includes Bloom helicase (BLM), plays an important function in DNA repair by unwinding complementary strands of duplex DNA as well as atypical DNA structures such as Holliday junctions. Mutations of the BLM gene can result in Bloom syndrome, an ... [truncated at 450 characters in length]|
|Author||Rosenthal, AS; Dexheimer, TS; Gileadi, O; et al|
|Key phrase||ADME BLM BS Bloom helicase Bloom syndrome DMF HR HTS Inhibitor MLM NADPH PBS PEPPSITM-IPr SAR SCE Small molecule [1,3-Bis(2,6-Diisopropylphenyl)imidazole-2-ylidene](3-chloropyridyl)palladium(II)chloride absorption, distribution, metabolism and excretion dimethylformamide high throughput screen homologous recombination mouse liver microsomes nicotinamide adenine dinucleotide phosphate phosphate buffered saline sister chromatid exchanges structure activity relationship|
A multi-functional imaging approach to high-content protein interaction screening.
|Abstract||Functional imaging can provide a level of quantification that is not possible in what might be termed traditional high-content screening. This is due to the fact that the current state-of-the-art high-content screening systems take the approach of scaling-up single cell assays, and are therefore based on essentially pictorial measures as assay indicators. Such phenotypic analyses have become extremely sophisticated, advancing screening enormously ... [truncated at 450 characters in length]|
|Author||Matthews, DR; Fruhwirth, GO; Weitsman, G; et al|
|Key phrase||Biosensing Techniques Cell Line, Tumor Fluorescence Polarization Fluorescence Resonance Energy Transfer Green Fluorescent Proteins Humans Luminescent Proteins Photons Protein Interaction Domains and Motifs Proteins Receptors, CXCR4 Sensitivity and Specificity Small Molecule Libraries|