Journal: Communications biology

Article Title: The PAR2 inhibitor I-287 selectively targets Gα q and Gα 12/13 signaling and has anti-inflammatory effects.

doi: 10.1038/s42003-020-01453-8

Figure Lengend Snippet: Fig. 5 I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways. a, b Impact of increasing concentrations of I-287 (15 min) on DAG production (a) and PKC activation (b) induced after 1 (DAG) or 5 (PKC) min stimulation with an EC80 concentration of hTrypsin or SLIGKV-NH2 in HEK293 cells co-expressing hPAR2 and the indicated unimolecular BRET2-based biosensors. Results are expressed as ΔBRET in % of the response induced by EC80 of respective agonists in the absence of I-287 (mean ± SEM; n = 4–5). c Impact of increasing concentrations of I-287 (30 min) on intracellular Ca2+ mobilization induced by an EC80 concentration of hTrypsin or SLIGKV-NH2 in HEK293 cells endogenously expressing hPAR2. Results are expressed as % of the response induced by respective agonists in the absence of I-287 (mean ± SEM; n = 3-4). d Impact of I-287 (10 µM, 30 min) on hPAR2-promoted SRF-RE reporter gene activation induced after 6 h stimulation with hTrypsin (10 U/mL) or SLIGKV-NH2 (100 µM) in HEK293 cells expressing hPAR2. FBS (10%) was used as control. Results are expressed as % of the response induced by respective agonists in the absence of I-287 (mean ± SEM; n = 3–5; unpaired t-test: *p < 0.05 and **p < 0.01 compared to respective control cells, ns: nonsignificant). e, f Kinetics of FAK and ERK1/2 phosphorylation in HEK293 cells expressing hPAR2 and pretreated with DMSO or I-287 (10 µM, 30 min) before stimulation with hTrypsin (1 U/mL) or SLIGKV-NH2 (100 µM) at the indicated times. Representative immunoblots of FAK and ERK1/2 phosphorylation are shown. Western blots were quantified and expressed as the ratio of phosphorylated protein level (P-FAK or P-ERK1/2) normalized over total protein (t-FAK or t-ERK1/2; mean ± SEM; n = 3–5; two-way ANOVA followed by Tukey’s post hoc test: *p < 0.05, **p < 0.01, and ***p < 0.001 compared to DMSO-treated cells at the respective time).

Article Snippet: Plasmids. hPAR2 cDNA plasmid was purchased from Origen (IBD90.1 clone; catalog number SC322345), where the serine in position 291 has been mutated in threonine (S291T) to reproduce the hPAR2 phenotype observed in HEK293 and HCT 116 cells.

Techniques: Activation Assay, Protein-Protein interactions, Concentration Assay, Expressing, Control, Phospho-proteomics, Western Blot

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: PAR2 expression level in lung cancer cells transfected either with pcDNA3-PAR2 or PAR2 shRNA. (A) PAR2 expression level after A549 cells were transfected with pcDNA3-PAR2; (B) PAR2 expression level after H1299 cells were transfected with pcDNA3-PAR2; (C) PAR2 expression level after A549 cells were transfected with PAR2 shRNA; (D) PAR2 expression level after H1299 cells were transfected with PAR2 shRNA.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Expressing, Transfection, shRNA

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: Overexpression PAR2 promoted growth of lung cancer cells with or without paclitaxel. (A–D) The growth of A549 cells with or without paclitaxel after transfection with pcDNA3-PAR2; (E–H) The growth of H1299 cells with or without paclitaxel after transfection with pcDNA3-PAR2.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Over Expression, Transfection

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: Knockdown PAR2 decreased growth of lung cancer cells with or without paclitaxel. (A–D) The growth of A549 cells with or without paclitaxel after transfection with PAR2 shRNA; (E–H) The growth of H1299 cells with or without paclitaxel after transfection with PAR2 shRNA.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Knockdown, Transfection, shRNA

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: PAR2 inhibited paclitaxel-associated apoptosis in lung cancer cells. (A) Caspase 3/7 activity in A549 cell transfected with pcDNA3-PAR2; (B) Caspase 3/7 activity in H1299 cell transfected with pcDNA3-PAR2; (C–F) Bcl-2 and BAX expression in A549 and H1299 cells.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Activity Assay, Transfection, Expressing

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: PAR2 played essential roles in invasion and migration of lung cancer cells. (A, B) up-regulation of PAR2 increased migration and invasion of A549 cells. (C, D) down-regulation of PAR2 decreaased migration and invasion of A549 cells. (E, F) up-regulation of PAR2 increased migration and invasion of H1299 cells. (G, H) down-regulation of PAR2 decreased migration and invasion of H1299 cells.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Migration

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: PAR2 altered PTEN/AKT protein expression in lung cancer cells. (A–C) Impact of up-regulation of PAR2 on expression of p-AKT, AKT and PTEN in A549 and H1299 cells. (D–F) Impact of down-regulation of PAR2 on expression of p-AKT, AKT and PTEN in A549 and H1299 cells.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Expressing

Journal: Future Science OA

Article Title: PAR2 regulates proliferation, migration of lung cancer and chemotherapy sensitivity by involving PTEN pathway

doi: 10.1080/20565623.2025.2535221

Figure Lengend Snippet: PAR2 expression in human lung cancer tissue. (A) PAR2 levels in different stage of lung cancer tissue and normal lung tissue. (B) Immunohistochemical studies for Ki-67 and PTEN on different levels of PAR2 in lung tissue.

Article Snippet: Human PAR2 sandwich enzyme-linked immunosorbent assay (ELISA) kit (Novus Biologicals, USA) was used to detect serum PAR2 level according to the manufacture’s instructions.

Techniques: Expressing, Immunohistochemical staining