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Synthesis and characterization of fluorescent cobalamin (CobalaFluor) derivatives for imaging.
TLDR
Fluorescent derivatives of cobalamin have been prepared by linking fluorophore NHS-ester with beta-(3-aminopropyl)cobalamin to form fluorescent cobalam conjugates (CobalaFluors) that are potentially suitable for the in vitro and in vivo imaging of transcobalamin receptors on cancer cells.
Molecular Imaging of GLUT1 and GLUT5 in Breast Cancer: A Multitracer Positron Emission Tomography Imaging Study in Mice
TLDR
The results highlight the importance of detailed biochemical studies on GLUT protein expression levels in combination with PET imaging studies for functional characterization of GLUTs in BC and suggest that tumor uptake of fructose metabolism-targeting radiotracers 1-[18F]FDF, 6-deoxy-6-fluoro-d-glucose, and 1-[ 18F]FDAM does not correlate with GLUT5 mRNA levels but is linked toGLUT5 protein levels.
Comprehensive in vitro characterization of PD-L1 small molecule inhibitors
TLDR
This work reports the rigorous and systematic in vitro characterization of a selected set of potent PD-1/PD-L1 macrocyclic peptide and small-molecule inhibitors from Bristol-Myers Squibb (BMS) and a peptidomimetic small- molecule inhibitor from Aurigene (Aurigene-1) using a series of biochemical and cell-based assays.
Structures reveal details of small molecule binding to cardiac troponin.
Advances in the Nazarov cyclization.
TLDR
Three principal subtopics are considered: stereocontrol, domino or cascade reactions initiated by the Nazarov cyclization, and alternative substrates (including versions of the 'metallo-Nazarov' reaction).
Equilibrium and kinetic analyses of the interactions between vitamin B(12) binding proteins and cobalamins by surface plasmon resonance.
TLDR
The affinities determined for protein-ligand interaction, using the solution competition and direct binding assays, are comparable, demonstrating that surface plasmon resonance provides a versatile way to study the molecular recognition properties of vitamin B(12) binding proteins.
Interrupting the Nazarov reaction: domino and cascade processes utilizing cyclopentenyl cations.
The Nazarov reaction entails the electrocyclic closure of a conjugated pentadienyl cation to furnish a cyclopentenyl cation. In its conventional protocol, this intermediate is allowed to undergo
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