Source Name: 2024_Bergeron
Literature Information
Literature Title | Analogs of Cyclic Peptide Mortiamide-D From Marine Fungi Have Improved Membrane Permeability and Kill Drug-Resistant Melanoma Cells |
Doi | 10.1002/pep2.24380 |
Research Group |
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Data Number | 3 |
Minimum Molecular Weight | 804.0 |
Maximum Molecular Weight | 847.1 |
Assay Information 1
Assay Type | PAMPA |
Permeability Type | logPapp |
Membrane Measurement Direction (Exclude PAMPA) | - |
Assay Detail | Assays were performed according to the manufacturer instructions for using the BD Gentest precoated PAMPA plate system (BD Biosciences). Peptides 1–3 were prepared at 50 μM in PBS with 1% (v/v) DMSO, then added to the apical side of the precoated PAMPA plate wells, and incubated for 4 h at 37°C, 5% CO2. |
Assay Information 2
Assay Type | Caco2 |
Permeability Type | logPapp |
Membrane Measurement Direction (Exclude PAMPA) | Apical to Basolateral (AB) |
Assay Detail | Permeability assays were performed as previously described. Caco-2 cells were grown in DMEM supplemented with 10% (v/v) fetal bovine serum, 1% (v/v) nonessential amino acids, 100 units/ mL of penicillin and 100 mg/mL of streptomycin, with culture flasks incubated at 37°C with 5% CO2. Cells were plated at 3 × 105 cells/well in Transwell 12- well plates (Corning) in DMEM supplezzmented with 10% (v/v) FBS, 1% (v/v) nonessential amino acids, 0.4 μg/mL puromycin and cultivated for 8–10 days. Transepithelial/ endothelial electrical resistance (TEER) was measured to confirm the integrity of the Caco-2 cell monolayer for the assay (>400 Ω). Peptides 1–3 were prepared at 50 μM in Hanks balanced salt solution (HBSS) with 50 μM lucifer yellow, then added to the apical side of Caco-2 cell monolayers, and incubated for 90 min at 37°C, 5% CO2, with orbital shaking at 55 rpm. |