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3.
Figure 2

Figure 2. Inhibition of PC6 activity by small molecule compounds.. From: Small Molecule Proprotein Convertase Inhibitors for Inhibition of Embryo Implantation.

The data are expressed as percent reduction of PC6 activity based on the rate of substrate hydrolysis relative to the control. Each value represents mean ± SEM of at least two independent experiments.

Huiting Ho, et al. PLoS One. 2013;8(12):e81380.
4.
Figure 4

Figure 4. Inhibition of decidualization of HESCs.. From: Small Molecule Proprotein Convertase Inhibitors for Inhibition of Embryo Implantation.

(A) Inhibition of decidualization by the five compounds at 10 µM using prolactin as the decidual marker. (B) Dose-dependent inhibition of decidualization by compound 1o using prolactin as the decidual marker. (C) Confirmation of decidualization inhibition by compound 1o with an additional decidual marker, IGFBP-1. The data are expressed as percentage reductions relative to control (no inhibitors). Each value represents mean ± SEM of three independent experiments. *P<0.05; **P<0.01

Huiting Ho, et al. PLoS One. 2013;8(12):e81380.
5.
Figure 6

Figure 6. Compound 1o reduces the cleavage of pro-intergrin-αV into its heavy chain.. From: Small Molecule Proprotein Convertase Inhibitors for Inhibition of Embryo Implantation.

(A) Representative western blot showing the pro-integrin-αV (∼170 kDa) and the heavy chain (130 kDa). (B) Densitometric analysis of the heavy chain of integrin-αV. Densitometric analysis was not performed for pro-integrin-αV as the signals were too weak to be accurately determined. Data were normalized to GAPDH and control and expressed as the mean ± SEM (n = 3). *P<0.05.

Huiting Ho, et al. PLoS One. 2013;8(12):e81380.
6.
Figure 5

Figure 5. (A) Representative micrograph of JAR spheroids attached to endometrial epithelial cell line Ishikawa monolayer.. From: Small Molecule Proprotein Convertase Inhibitors for Inhibition of Embryo Implantation.

(B) Inhibition of the receptivity of endometrial epithelial cell line Ishikawa to JAR spheroids by compound 1o in a dose-dependent fashion. The data are expressed as the attachment ratio relative to control. Each bar indicates the mean ± SEM of three independent experiments. *P<0.05; **P<0.01.

Huiting Ho, et al. PLoS One. 2013;8(12):e81380.
7.
Figure 3

Figure 3. Putative binding modes of compounds 1g and 1o in the active site of hPC6.. From: Small Molecule Proprotein Convertase Inhibitors for Inhibition of Embryo Implantation.

hPC6 is depicted as a molecular surface colored by electrostatic potential (red – regions of negative potential, blue – regions of positive potential), selected residues of the S1–S6, S1′ sub-pockets and catalytic triad are shown as sticks. The Ca2+ cation close to the active site is shown as a magenta sphere (labelled as Ca) and the coordinated waters as small red spheres (labelled as H2O). The location of sub-pockets S1–S6 and S1′ are indicated. Electrostatic/hydrogen bonds/polar contacts are indicated by black dashed lines. (A) Binding mode of compound 1g (green colored sticks). The four guanidino moieties are located in S1, S2 and S4 sub-pockets and near the catalytic triad (D172, H213, S385). (B) Binding mode of compound 1o (yellow colored sticks). The four guanidino moieties are located in the S1, S2 and S3 sub-pockets and near the catalytic triad (D172, H213, S385).

Huiting Ho, et al. PLoS One. 2013;8(12):e81380.

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