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C50 values were estimated for each peptide as the peptide concentration required for half maximal stabilization of HLA-A2.
The C50 value was calculated for each peptide as the peptide concentration required for half maximal stabilization of HLA-A2.
The Tm values derived from all of our biophysical experiments are presented in Table 2, which documents the dose-dependent stabilization of CTA1 by PBA: although PBA conferred some thermal stability to the secondary and tertiary structures of CTA1 at 1 and 10 µM concentrations, the maximal stabilization of CTA1 was obtained with 100 µM PBA.
This process is required for maximal stabilization of TAp63 in female germ cells, and the subsequent death of these cells, after exposure to a genotoxic stress in vivo.
Blood was obtained in the morning (7.00 a.m. to 8.00 a.m.; in the fasting state) after a 25-minute rest at slight or no stasis from the antecubital vein into CTAD tubes, which contain four anticoagulants, sodium citrate, theophylline, adenosine, and dipyridamole (Vacutainers, Becton-Dickinson), to obtain maximal stabilization of platelets, and then placed into the ice/water bath.
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The di-peptides also stabilized the 4xUb-Luc reporter in MDA-MB-231 cells with EC50 values that tracked closely with their in vitro 20S β5 potencies (Table 2), although the maximal stabilization effects of approx. 100-fold were lower than those observed for bortezomib (Table 2), other boronates (J.L. Blank, unpublished work) and covalent inhibitors, such as salinosporamide A [ 15].
We measured the changes in melting temperature (Δ Tm) upon varying the concentration of added foldamer or macrocyle (Δ Tm in presence of 1 μ m ligand in Table 1; concentrations for maximal stabilization in Table 2; full melting profiles in the Supporting Information).
However, the DNA melting profiles in the presence of 9 (see Supporting Information) show that this foldamer exhibited formidable selectivity for G-quadruplexes over duplex DNA, even though maximal stabilization occurred above 1 μ m.
In respect to g-As2Se3-based media, this can be achieved due to doping with small amount of Ga (or alternatively, In), allowing stabilization of optimal compound with maximal Ga content, but still in glassy state [14 18].
After initial stabilization of her clinical state with maximal supportive care, she then started to deteriorate clinically, with signs of cardiovascular collapse and no signs of obvious neurological recovery.
The maximal current amplitude was increased several fold due to stabilization of the activated-open state.
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