Journal: EJNMMI Radiopharmacy and Chemistry

Article Title: Preclinical validations of [ 18 F]FPyPEGCBT- c (RGDfK): a 18 F-labelled RGD peptide prepared by ligation of 2-cyanobenzothiazole and 1,2-aminothiol to image angiogenesis

doi: 10.1186/s41181-016-0019-z

Figure Lengend Snippet: Displacement of [ 125 I]echistatin by FPyPEGCBT- c (RGDfK). U-87 MG and SKOV-3 cancer cells were co-incubated for 1 h in 96-well plates with 370 Bq/well [ 125 I]echistatin and a concentration range (10 −9 to 10 −4 M) of FPyPEGCBT- c (RGDfK) or c (RGDfV). After lysis, the cell-associated radioactivity was measured in a γ-counter. Means ± SD of three independent experiments conducted in quadruplicate well were fitted by nonlinear regression using GraphPad Prism and R 2 fitting correlation coefficients are shown ( a ). IC 50 values ± SD are also shown ( b )

Article Snippet: On the day of the experiment, the cells were washed twice with binding buffer (20 mM Tris pH 7.4, 150 mM NaCl, 2 mM CaCl 2 , 1 mM MgCl 2 , 1 mM MnCl 2 , 0.1 % BSA), then co-incubated for 1 h at 37 °C in binding buffer with 370 Bq/well [ 125 I]echistatin (Perkin Elmer, Schwerzenbach, Switzerland) and a concentration range (10 −9 to 10 −4 M) of FPyPEGCBT- c (RGDfK) or c (RGDfV) (PeptaNova, Sandhausen, Germany) as a reference peptide.

Techniques: Incubation, Concentration Assay, Lysis, Radioactivity

Journal: EJNMMI Radiopharmacy and Chemistry

Article Title: Preclinical validations of [ 18 F]FPyPEGCBT- c (RGDfK): a 18 F-labelled RGD peptide prepared by ligation of 2-cyanobenzothiazole and 1,2-aminothiol to image angiogenesis

doi: 10.1186/s41181-016-0019-z

Figure Lengend Snippet: Uptake of [ 18 F]FPyPEGCBT- c (RGDfK) in cancer cells. U-87 MG and SKOV-3 cells were incubated with 100 kBq/mL [ 18 F]FPyPEGCBT- c (RGDfK) for 15 to 120 min at 37 or 4 °C ( a ). Cells were also co-treated with 10 −4 M c (RGDfV) for 1 h ( b ). Uptake of [ 18 F]FPyPEGCBT- c (RGDfK) was also evaluated after 1 h of incubation with cells with selective siRNA-mediated knocked down of α V , β 1 , β 3 or β 5 integrin subunits and indicated combinations ( c ). Depletions were verified by immunoblotting using specific antibodies as compared to untransfected cells (Unt) and to an irrelevant depletion of luciferase (si Luc). After incubation, cells were lysed and the cell-associated radioactivity was measured in a γ-counter. Data are means ± SD of at least three independent experiments performed in quadruplicate well. Statistical differences were analysed with the one-way ANOVA test followed by Dunnett’s post hoc test as compared to 37 °C controls ( b ) or to si Luc ( c ); # p < 0.001

Article Snippet: On the day of the experiment, the cells were washed twice with binding buffer (20 mM Tris pH 7.4, 150 mM NaCl, 2 mM CaCl 2 , 1 mM MgCl 2 , 1 mM MnCl 2 , 0.1 % BSA), then co-incubated for 1 h at 37 °C in binding buffer with 370 Bq/well [ 125 I]echistatin (Perkin Elmer, Schwerzenbach, Switzerland) and a concentration range (10 −9 to 10 −4 M) of FPyPEGCBT- c (RGDfK) or c (RGDfV) (PeptaNova, Sandhausen, Germany) as a reference peptide.

Techniques: Incubation, Western Blot, Luciferase, Radioactivity

Journal: EJNMMI Radiopharmacy and Chemistry

Article Title: Preclinical validations of [ 18 F]FPyPEGCBT- c (RGDfK): a 18 F-labelled RGD peptide prepared by ligation of 2-cyanobenzothiazole and 1,2-aminothiol to image angiogenesis

doi: 10.1186/s41181-016-0019-z

Figure Lengend Snippet: Biodistribution of [ 18 F]FPyPEGCBT- c (RGDfK) in nude mice bearing U-87 MG or SKOV-3 subcutaneous tumours. Mice intravenously injected with 3–5 MBq [ 18 F]FPyPEGCBT- c (RGDfK) were sacrificed and indicated organs were collected after uptake times of 30, 60 or 120 min ( a ). For the blocking experiments, mice were injected intravenously with 20 mg/kg of c (RGDfV) 5 min prior to [ 18 F]FPyPEGCBT- c (RGDfK) injection and indicated organs were collected after 60 min of uptake ( b ). [ 18 F]FPyPEGCBT- c (RGDfK) uptake in the indicated organs was quantified in a γ-counter and expressed as percentages of the injected dose per gram (%ID/g) ( a , b ). Tumours-to-blood and Tumours-to-muscle %ID/g ratios were also determined for the uptake time course of [ 18 F]FPyPEGCBT- c (RGDfK) ( c ) and the blocked experiment ( d ). Data are means ± SD ( n ≥ 7) and statistical differences were analysed with the one-way ANOVA test followed by Dunnett’s post hoc test as compared with 0.5 h uptake time ( c ) or with non-blocked 1 h uptake time ( d ); * p < 0.05, ** p < 0.01, # p < 0.001

Article Snippet: On the day of the experiment, the cells were washed twice with binding buffer (20 mM Tris pH 7.4, 150 mM NaCl, 2 mM CaCl 2 , 1 mM MgCl 2 , 1 mM MnCl 2 , 0.1 % BSA), then co-incubated for 1 h at 37 °C in binding buffer with 370 Bq/well [ 125 I]echistatin (Perkin Elmer, Schwerzenbach, Switzerland) and a concentration range (10 −9 to 10 −4 M) of FPyPEGCBT- c (RGDfK) or c (RGDfV) (PeptaNova, Sandhausen, Germany) as a reference peptide.

Techniques: Injection, Blocking Assay

Journal: EJNMMI Radiopharmacy and Chemistry

Article Title: Preclinical validations of [ 18 F]FPyPEGCBT- c (RGDfK): a 18 F-labelled RGD peptide prepared by ligation of 2-cyanobenzothiazole and 1,2-aminothiol to image angiogenesis

doi: 10.1186/s41181-016-0019-z

Figure Lengend Snippet: MicroPET/CT images of [ 18 F]FPyPEGCBT- c (RGDfK) in nude mice bearing subcutaneous tumours. Coronal sections of representative microPET/CT images of nude mice bearing subcutaneous U-87 MG ( a , left ) and SKOV-3 ( a , right ) tumours after an uptake time of [ 18 F]FPyPEGCBT- c (RGDfK) of 60 ± 10 min. Tumours are outlined by dashed circles. Similar experiments were performed with injections of a blocking c (RGDfV) peptide 5 min prior to the tracer ( b ). c Mean SUV of [ 18 F]FPyPEGCBT- c (RGDfK) in U-87 MG and SKOV-3 tumours at indicated times (top graph) as well as in the 60 min-blocked experiment ( bottom graph ). d Tumours-to-blood and Tumours-to-muscle SUV ratios were also determined for the uptake time course of [ 18 F]FPyPEGCBT- c (RGDfK) ( top graph ) and the blocked experiment ( bottom graph ). Data are means ± SD ( n ≥ 5). Statistical differences were analysed with the one-way ANOVA test followed by Dunnett’s post hoc test as compared with 0.5 h uptake time ( c , d , top graphs ) or with non-blocked 1 h uptake time ( c , d , bottom graphs ); * p < 0.05, # p < 0.001

Article Snippet: On the day of the experiment, the cells were washed twice with binding buffer (20 mM Tris pH 7.4, 150 mM NaCl, 2 mM CaCl 2 , 1 mM MgCl 2 , 1 mM MnCl 2 , 0.1 % BSA), then co-incubated for 1 h at 37 °C in binding buffer with 370 Bq/well [ 125 I]echistatin (Perkin Elmer, Schwerzenbach, Switzerland) and a concentration range (10 −9 to 10 −4 M) of FPyPEGCBT- c (RGDfK) or c (RGDfV) (PeptaNova, Sandhausen, Germany) as a reference peptide.

Techniques: Blocking Assay

Journal: Frontiers in Molecular Neuroscience

Article Title: Ototoxicity: a high risk to auditory function that needs to be monitored in drug development

doi: 10.3389/fnmol.2024.1379743

Figure Lengend Snippet: Drug candidates in clinical development for drug induced hearing loss.

Article Snippet: ORC-13661A , Oricula Therapeutics , DIHL Aminoglycosides , oral , , Phase 1.

Techniques: Binding Assay