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New pharmacological interventions influencing food intake regulation
Špolcová, Andrea ; Čabala, Radomír (advisor) ; Podlipná, Radka (referee)
NEW PHARMACOLOGICAL INTERVENTIONS INFLUENCING FOOD INTAKE REGULATION Author: Bc. Andrea Špolcová ABSTRACT Prolactin-releasing peptide (PrRP) identified as an endogenous ligand of the orphan receptor GPR10 was originally found to stimulate the secretion of prolactin (PRL) both in vitro and in vivo. PrRP-mediated PRL secretion was later questioned and is not currently considered to be the primary function of PrRP. The fact that both PrRP and GPR10 knock-out mice are hyperphagic and develop late-onset obesity proves the unique anorexigenic properties of PrRP. Designing and evaluation of PrRP analog(s) with selective anorexigenic properties and searching for PrRP antagonists would contribute to finding the mechanism and possible treatment of obesity and metabolic syndrome. In our recent published study (Maixnerová et al., Peptides (2011)), the PrRP receptor was immunodetected and characterized by saturation binding in three rodent tumor pituitary cell lines. Two naturally occurring analogs, PrRP31 and PrRP20, showed comparable potency in binding, cell signaling and prolactin release in pituitary RC-4B/C cells, as well as caused food intake decrease after intracerebroventricular administration in fasted mice. In the present study, analogs of PrRP20 with C-terminal Phe amide derivatives with modified aromatic...
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New pharmacological interventions influencing food intake regulation
Špolcová, Andrea ; Čabala, Radomír (advisor) ; Podlipná, Radka (referee)
NEW PHARMACOLOGICAL INTERVENTIONS INFLUENCING FOOD INTAKE REGULATION Author: Bc. Andrea Špolcová ABSTRACT Prolactin-releasing peptide (PrRP) identified as an endogenous ligand of the orphan receptor GPR10 was originally found to stimulate the secretion of prolactin (PRL) both in vitro and in vivo. PrRP-mediated PRL secretion was later questioned and is not currently considered to be the primary function of PrRP. The fact that both PrRP and GPR10 knock-out mice are hyperphagic and develop late-onset obesity proves the unique anorexigenic properties of PrRP. Designing and evaluation of PrRP analog(s) with selective anorexigenic properties and searching for PrRP antagonists would contribute to finding the mechanism and possible treatment of obesity and metabolic syndrome. In our recent published study (Maixnerová et al., Peptides (2011)), the PrRP receptor was immunodetected and characterized by saturation binding in three rodent tumor pituitary cell lines. Two naturally occurring analogs, PrRP31 and PrRP20, showed comparable potency in binding, cell signaling and prolactin release in pituitary RC-4B/C cells, as well as caused food intake decrease after intracerebroventricular administration in fasted mice. In the present study, analogs of PrRP20 with C-terminal Phe amide derivatives with modified aromatic...
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Specific binding of prolactin-releasing peptide analogues in pituitary cells
Maixnerová, Jana ; Špolcová, Andrea ; Matyšková, Resha ; Blechová, Miroslava ; Veselá, Iva ; Železná, Blanka ; Maletínská, Lenka
We report specific binding of 125I-PrRP31 to the following cell lines: GH3 cells (rat – somatotrophs), AtT20 cells (mouse – adenocorticotrophs) and RC-4B/C cells (rat- somatotrophs, lactrophs, adenocortitrophs and gonadotrophs). These results will serve as a basic knowledge for future structure-activity studie sof PrRP.
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