human glypican  (Sino Biological)

Journal: Acta Pharmaceutica Sinica. B

Article Title: GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

doi: 10.1016/j.apsb.2025.02.037

Figure Lengend Snippet: The GLTAC strategy for targeted membrane protein degradation. (A) The GLTAC molecule, consisting of a GPC3-targeting ligand, a POI-binding ligand, and a linker, hijacks the GPC3 receptor to induce the internalization and lysosomal degradation of POI. (B) Chemical structure of PD-L1 GLTACs.

Article Snippet: The recombinant human GPC3 protein (ABclonal, Cat No. RP00138) or PD-L1 protein (ABclonal, Cat No. RP00068) powder was diluted to a concentration of 200 nmol/L with PBS and added to the corresponding centrifuge tube.

Techniques: Membrane, Binding Assay

Journal: Acta Pharmaceutica Sinica. B

Article Title: GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

doi: 10.1016/j.apsb.2025.02.037

Figure Lengend Snippet: GPC3-mediated endocytosis and lysosomal trafficking using a probe conjugating GPC3-targeting peptide with photosensitizer. (A) Schematic diagram of the internalization of probe 8b mediated by GPC3. (B) GPC3 protein expression level in HepG2 cells. (C) Cellular uptake of probe 8b (2 μmol/L) in HepG2 cells using confocal laser scanning. (D) Colocalization of probe 8b (red) with the lysosome marker (green) in HepG2 cells. (E) Colocalization of probe 8b (red) with the lysosome marker (green) by 3D fluorescence confocal assay. Pearson coefficient R = 0.84. For C–E, Scale bar = 10 μm.

Article Snippet: The recombinant human GPC3 protein (ABclonal, Cat No. RP00138) or PD-L1 protein (ABclonal, Cat No. RP00068) powder was diluted to a concentration of 200 nmol/L with PBS and added to the corresponding centrifuge tube.

Techniques: Expressing, Marker, Fluorescence, Confocal Assay

Journal: Acta Pharmaceutica Sinica. B

Article Title: GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

doi: 10.1016/j.apsb.2025.02.037

Figure Lengend Snippet: PD-L1 degradation activities of GLTACs. (A) PD-L1 degradation activity of compounds WP0 and WP1 in HepG2 cells. Data are presented as mean ± SD ( n = 3). ∗∗ P < 0.01, ∗∗∗ P < 0.001, ∗∗∗∗ P < 0.0001, ns, not significant. (B) Representative confocal micrographs of the PD-L1 degradation activity of compound WP0 (3 μmol/L) in HepG2 cells. Scale bar = 10 μm. (C) GPC3 and PD-L1 protein expression levels in Caco2 cells. (D) PD-L1 degradation activity of compounds WP0 and WP1 in Caco2 cells. Data are presented as mean ± SD ( n = 3). ∗ P < 0.1, ∗∗∗ P < 0.001, ∗∗∗∗ P < 0.0001, ns, not significant. Uncropped blot images for A and D are shown in . The red numbers in A and D represent the percentage of PD-L1 remaining relative to the control.

Article Snippet: The recombinant human GPC3 protein (ABclonal, Cat No. RP00138) or PD-L1 protein (ABclonal, Cat No. RP00068) powder was diluted to a concentration of 200 nmol/L with PBS and added to the corresponding centrifuge tube.

Techniques: Activity Assay, Expressing, Control

Journal: Acta Pharmaceutica Sinica. B

Article Title: GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

doi: 10.1016/j.apsb.2025.02.037

Figure Lengend Snippet: Degradation mechanisms of PD-L1 GLTAC. (A) Time-dependent degradation activity of compound WP0 (3 μmol/L) in HepG2 cells. (B) PD-L1 protein level in HepG2 cells. Cells were pretreated with lysosome inhibitor BafA (100 nmol/L), BMS-202 (1 μmol/L), TJ12P1 (1 μmol/L), or proteasome inhibitor MG132 (100 nmol/L), followed by treatment with WP0 (1 μmol/L). (C) GPC3 and PD-L1 protein expression levels in MDA-MB-231 cells. (D) Degradation activity of WP0 on PD-L1 protein in MDA-MB-231 cells. Uncropped blot images for A, B and D are shown in . The red numbers in A, B and D represent the percentage of PD-L1 remaining relative to the control.

Article Snippet: The recombinant human GPC3 protein (ABclonal, Cat No. RP00138) or PD-L1 protein (ABclonal, Cat No. RP00068) powder was diluted to a concentration of 200 nmol/L with PBS and added to the corresponding centrifuge tube.

Techniques: Activity Assay, Expressing, Control

Journal: Acta Pharmaceutica Sinica. B

Article Title: GPC3-mediated lysosome-targeting chimeras (GLTACs) for targeted degradation of membrane proteins

doi: 10.1016/j.apsb.2025.02.037

Figure Lengend Snippet: Binding of GLTAC WP0 with GPC3 and PD-L1 and the formation of ternary complex. (A) Binding of compound WP0 (5 μmol/L) with GPC3 and PD-L1 verified by CETSA. (B) Binding affinity of compound WP0 with GPC3 and PD-L1 measured by MST assay. Data were represented as mean ± SD ( n = 3). (C) Colocalization of GPC3 and PD-L1 induced by compound WP0 (3 μmol/L) by confocal microscopy. Scale bar = 10 μm. (D) Compound WP0 (5 μmol/L) induced the PD-L1- WP0 -GPC3 ternary complex formation. Uncropped blot images for A and D are shown in .

Article Snippet: The recombinant human GPC3 protein (ABclonal, Cat No. RP00138) or PD-L1 protein (ABclonal, Cat No. RP00068) powder was diluted to a concentration of 200 nmol/L with PBS and added to the corresponding centrifuge tube.

Techniques: Binding Assay, Confocal Microscopy