fgfr2  (Carna Inc)

Journal: The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology

Article Title: Circular RNA circSmad4 controls pulmonary fibrosis

doi: 10.4196/kjpp.25.123

Figure Lengend Snippet: (A) Relative expression levels of miR-671-5p after treatment with the si-circSmad4 ± TGF-β1 (n = 8–9 per group). (B) Relative Fgfr2 mRNA expression levels after treatment with the si-circSmad4 ± TGF-β1 (n = 8–9 per group). p-values were determined using Tukey’s HSD test following one-way ANOVA. All data are presented as mean ± SEM. *p ≤ 0.05; **p ≤ 0.01; ****p ≤ 0.0001.

Article Snippet: FGFR2-IN-1 (HY-145230; MedChemExpress) was used as a selective FGFR2 inhibitor and dissolved in dimethyl sulfoxide to the desired concentrations.

Techniques: Expressing

Journal: The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology

Article Title: Circular RNA circSmad4 controls pulmonary fibrosis

doi: 10.4196/kjpp.25.123

Figure Lengend Snippet: (A) Relative miR-671-5p amount in NIH3T3 treated with TGF-β1 (n = 6 per group). (B) Relative mRNA levels of fibrosis-related genes ( Acta2, Col1a1, Col3a1, Ctgf ) under the indicated combinations of miR-671-5p mimic and TGF-β1 (n = 6 per group). (C) Collagen concentrations measured in the culture medium (Media collagen) and the matrix-associated fraction (Matrix collagen) transfected with miR-671-5p mimic in NIH3T3 cells (n = 8 per group). (D) Relative Fgfr2 mRNA expression levels in NIH3T3 fibroblasts treated with TGF-β1 (n = 6 per group). (E) Effect of miR-671-5p mimic on TGF-β1-induced in Fgfr2 mRNA expression (n = 6 per group). (F) Effect of si-circSMAD4 on TGF-β1-induced increase in Fgfr2 mRNA expression (n = 6 per group). (G) Changes in the expression of Acta2, Col1a1, Ctgf, Fibronectin-1 ( Fn1 ) in NIH3T3 cells under FGFR2-IN-1 and TGF-β1 treatments (n = 7 per group). p-values were determined using Tukey’s HSD test following one-way ANOVA. All data are presented as mean ± SEM. ns, not significant. *p ≤ 0.05; **p ≤ 0.01; ***p ≤ 0.001; ****p ≤ 0.0001.

Article Snippet: FGFR2-IN-1 (HY-145230; MedChemExpress) was used as a selective FGFR2 inhibitor and dissolved in dimethyl sulfoxide to the desired concentrations.

Techniques: Transfection, Expressing

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: Chemical structures of selective FGFR2 inhibitors 1 – 4 .

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques:

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: The binding mode of FGFR2 inhibitor 2 (PDB: 8STG) with FGFR2 and the predicted binding model of new FGFR2 inhibitor PLW1 with FGFR2 are shown. Hydrogen bonds were indicated by yellow dashed lines.

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques: Binding Assay

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: PLW559 covalently binds to FGFR2 kinase. (A) Antiproliferative effects of PLW559 and PLW14N against BaF3-FGFR1, BaF3-FGFR2 and parental BaF3 cell lines; (B) Docking results of PLW559 with FGFR2; (C) Deconvoluted intact mass spectra of unmodified FGFR2 (top) and PLW559 -labeled FGFR2 (bottom), acquired with 1 μg of protein; (D) Higher energy collision-induced dissociation (HCD) MS/MS spectrum of the [M + 2H] 2+ ion at m/z 1251.581, derived from the human FGFR2 peptide PLGEGCFGQVVMAEAVGIDK containing one modified site. Predicted b- and y-type ions (partial list) are indicated above and below the peptide sequence, respectively.

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques: Labeling, Tandem Mass Spectroscopy, Derivative Assay, Modification, Sequencing

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: PLW559 selectively inhibits FGFR2 kinase activity. (A) Selectivity profile of PLW559 against a panel of 76 tyrosine kinases, presented as a heat map; (B) Kinases exhibiting the highest inhibition rates by PLW559 at 1 μM; (C) IC 50 values of PLW559 against FGFR1-4. Pan-FGFR inhibitor TAS120 was included as a positive control and its IC 50 values against FGFR1-4 were 0.793, 0.5634, 0.8203, and 2.724 nM, respectively.

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques: Activity Assay, Inhibition, Positive Control

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: PLW559 suppresses FGFR2 signalling and selectively inhibits FGFR2-driven cancer cell proliferation. (A) Inhibition of FGFR2-mediated signalling in SNU-16 cells. SNU-16 cells were treated with PLW559 for 1 h before lysis and subsequent Western-blot analysis. GAPDH served as the loading control; (B) Antiproliferative activity of PLW559 and PLW14N against cancer cell lines. Cell proliferation was assessed using the CCK-8 assay after 72 h of treatment with compound or 0.2% DMSO.

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques: Inhibition, Lysis, Western Blot, Control, Activity Assay, CCK-8 Assay

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: 2 H -pyrazolo[3,4- d ]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors

doi: 10.1080/14756366.2026.2647526

Figure Lengend Snippet: PLW559 selectively induces apoptosis of FGFR2-overexpressed cancer cells. Apoptosis was analysed in A204 (A) and SNU-16 (B) cells following treatment with the indicated concentrations of PLW559 for 48 h. Cells were stained with Annexin V and 7-AAD and analysed by flow cytometry; representative flow cytometry plots were shown. Quantitative summaries of the flow cytometry results are presented in bar charts (C and D).

Article Snippet: PLW559 was preincubated with FGFR1, FGFR2, FGFR3 or FGFR4 kinase (Carna Biosciences) and substrate peptide (Peptide30, GL) in 50 mmol/L HEPES, pH 7.5, 10 mmol/L MgCl 2 , 1 mmol/L EGTA, 0.01% Brij-35, 2 mmol/L DTT, and 0.05% BSA for 30 min at room temperature.

Techniques: Staining, Flow Cytometry

Journal: The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology

Article Title: Circular RNA circSmad4 controls pulmonary fibrosis

doi: 10.4196/kjpp.25.123

Figure Lengend Snippet: (A) Relative miR-671-5p amount in NIH3T3 treated with TGF-β1 (n = 6 per group). (B) Relative mRNA levels of fibrosis-related genes ( Acta2, Col1a1, Col3a1, Ctgf ) under the indicated combinations of miR-671-5p mimic and TGF-β1 (n = 6 per group). (C) Collagen concentrations measured in the culture medium (Media collagen) and the matrix-associated fraction (Matrix collagen) transfected with miR-671-5p mimic in NIH3T3 cells (n = 8 per group). (D) Relative Fgfr2 mRNA expression levels in NIH3T3 fibroblasts treated with TGF-β1 (n = 6 per group). (E) Effect of miR-671-5p mimic on TGF-β1-induced in Fgfr2 mRNA expression (n = 6 per group). (F) Effect of si-circSMAD4 on TGF-β1-induced increase in Fgfr2 mRNA expression (n = 6 per group). (G) Changes in the expression of Acta2, Col1a1, Ctgf, Fibronectin-1 ( Fn1 ) in NIH3T3 cells under FGFR2-IN-1 and TGF-β1 treatments (n = 7 per group). p-values were determined using Tukey’s HSD test following one-way ANOVA. All data are presented as mean ± SEM. ns, not significant. *p ≤ 0.05; **p ≤ 0.01; ***p ≤ 0.001; ****p ≤ 0.0001.

Article Snippet: FGFR2-IN-1 (HY-145230; MedChemExpress) was used as a selective FGFR2 inhibitor and dissolved in dimethyl sulfoxide to the desired concentrations.

Techniques: Transfection, Expressing