The equivalent inducibility by the different compounds is in agreement with the modeling data that show similar distances to the key amino acids in the AR LBP of the mutated LNCaP AR.
Similar results were obtained when estimating the contributions made by the different compounds of root-zone respiration in the sink-limited plants on the second day in the cuvette experiments based on data from Fig. 3.
To compare inhibition by the different compounds, rates were calculated from the time period between first detection of PT pore opening in the absence of inhibitor (vertical arrow, Figure 2A) and the attainment of a 0.24 unit change in absorbance (horizontal arrow; corresponding to an approximate half-maximal absorbance change).
Determination of relative induction by the different compounds showed a 23.7 ± 5.0-fold induction after exposure to DHT, a 24.4 ± 5.1-fold induction with 50 50 TBECH-γδ, a 25.5 ± 1.3-fold induction with 25:75 TBECH-γδ, an 8.4 ± 1.2-fold induction with TBECH-αβ, and a 2.4 ± 0.3-fold induction with TBECH-β.
By comparing the activities of the different compounds against wild-type RT and the resistant enzymes carrying the single mutations Lys103Asn, Leu100Ile, and Tyr181Ile (K103N, L100I, and Y181I), we found that one compound (RS1914) dissociated from the mutated enzymes almost 10-fold slower than from the wild type RT.
The inhibition constants (K i) of CA II were determined in vitro for the different compounds by assaying CA-catalyzed CO2 hydration activity.
Specimens of the different compounds were manufactured by a hot pressing process.
Identification of the different compounds was made by comparing their retention time and UV spectra with those of pure standards.
At present, the relative risk of precipitating renal failure by using the different compounds is unsettled.
To investigate whether the effects of the inhibitors in the acidification assays were paralleled by inhibition of bone resorption by human osteoclasts, the different compounds were tested in a dose-response, again using Bafilomycin A1 as a positive control (figure 4H) [ 27, 28].
To further understand the biological pathways upregulated by these different compounds we performed an Ingenuity Pathway Analysis (IPA), focusing on the MCF7 IGF1R cell line using both time points (Venn diagram Fig. 3a).
