Fig. 1: Influence of LZNV on the thermostability and function of YePEPT. | Communications Chemistry

Fig. 1: Influence of LZNV on the thermostability and function of YePEPT.

From: Peptide transporter structure reveals binding and action mechanism of a potent PEPT1 and PEPT2 inhibitor

Fig. 1

a Thermal shift assay using YePEPTWT and YePEPTK314A, and LZNV. The Ti-values of YePEPTWT and YePEPTK314A were determined at different concentrations of LZNV (200 µM, 400 µM and 800 µM). ΔTi-values at specified LZNV concentrations were calculated by subtraction of the Ti-value in the absence of LZNV. Data points represent mean ± SD of at least three independent experiments. b Kinetics of [3H]Ala-Ala uptake in E. coli cells transformed with the YePEPTK314A construct. Data points represent uptake of [3H]Ala-Ala normalised to Vmax ± SEM of three independent experiments, each at least in triplicate. c IC50 determination of YePEPTK314A for LZNV by heterologous competition. Data points represent uptake of [3H]Ala-Ala normalised to the uninhibited signal ± SEM of three independent experiments, each at least in triplicates. Numbers in brackets below Km- and IC50-values represent 95% confidence intervals. If not visible, error bars are smaller than symbols.

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