Cocaine- and amphetamine-regulated transcript (CART) peptide specific binding in pheochromocytoma cells PC12
| Autor: | Jiřina Slaninová, Resha Matyšková, Lenka Maletínská, Jana Maixnerová, Eva Sloncova, Blanka Železná, Renata Haugvicová, Tomáš Elbert |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Cart medicine.medical_specialty Time Factors Cellular differentiation Cell Adrenal Gland Neoplasms PC12 cell line Nerve Tissue Proteins Pheochromocytoma Binding Competitive Models Biological PC12 Cells Cocaine and amphetamine regulated transcript Iodine Radioisotopes Eating Mice chemistry.chemical_compound immune system diseases Iodine Isotopes Internal medicine Nerve Growth Factor mental disorders medicine Animals Binding site Neurons Pharmacology Dose-Response Relationship Drug Chemistry Cell Membrane virus diseases Cell Differentiation Biological activity Peptide Fragments Rats Mice Inbred C57BL Kinetics Phenotype Endocrinology medicine.anatomical_structure nervous system Cell culture hormones hormone substitutes and hormone antagonists Protein Binding |
| Zdroj: | European Journal of Pharmacology. 559:109-114 |
| ISSN: | 0014-2999 |
| Popis: | CART (cocaine- and amphetamine-regulated transcript) peptides have been studied for ten years. We report specific binding of 125I-CART(61-102) to the rat adrenal pheochromocytoma PC12 cell line, both intact cells and cell membranes. Saturation binding to intact plated cells resulted in Kd of 0.48 ± 0.16 nM and Bmax of 2228 ± 529 binding sites/cell. 125I-CART(61-102) was also bound to PC12 cells differentiated using nerve growth factor to the neuronal phenotype with non-specific binding below 20%, and Kd of 1.90 ± 0.27 nM and Bmax of 11194 ± 261 binding sites/cell. In competitive binding experiments, CART(61-102), CART(55-102) and di-iodinated CART(61-102) were bound to PC12 cell membranes with Ki in low nM range; their affinity to intact non-differentiated and differentiated cells was in low 10− 8 M range. In order to prove that iodination did not eliminate the pharmacological properties of CART, we tested the biological activity of di-iodinated CART(61-102). It decreased food intake in in vivo feeding experiment on fasted mice in a dose of 1 μg/mouse to the same extent as CART(61-102) in a dose of 0.5 μg/mouse. |
| Databáze: | OpenAIRE |
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