title: In vitro evaluation of leptin fragments activity on the ob receptor.
abstract: In an attempt to identify regions in the leptin molecule responsible for its bioactivity, we tested six related-leptin peptide fragments denoted: Ac-hLEP(23-47)-NH(2) (I), Ac-hLEP(48-71)-NH(2) (II), Ac-hLEP(72-88)-NH(2) (III), Ac-hLEP(92-115)-NH(2) (IV), Ac-[Ser(117)]-hLEP(116-140)-NH(2) (V), Ac-hLEP(141-164)-NH(2) (VI) and their correspondent disulfide bridged dimer forms. The activity of the fragments was evaluated in comparision to leptin, by their ability to interact with leptin receptor using a cytosensor microphysiometer. Our results indicated that the fragments IV and V and [D-Leu(4)]-OB(3) and its human sequence analog were recognized by leptin receptor present in HP-75 cells, in agreement with the results obtained by other workers, validating that this region of the molecule contain the functional epitope of the leptin molecule.
authors.affiliation: Natural and Human Science Center, Federal University of ABC, Santo André, SP, Brazil. vani.junior@ufabc.edu.br
authors.forename: Vani Xavier
authors.initials: VX
authors.lastname: de Oliveira
authors.forename: Marcos Antonio
authors.initials: MA
authors.lastname: Fázio
authors.forename: Edson Lucas
authors.initials: EL
authors.lastname: Santos
authors.forename: João Bosco
authors.initials: JB
authors.lastname: Pesquero
authors.forename: Antonio
authors.initials: A
authors.lastname: Miranda
mesh_terms: D000595:Amino Acid Sequence; D002460:Cell Line; D002942:Circular Dichroism; D019281:Dimerization; D000939:Epitopes / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology; D005110:Extracellular Space / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D020738:Leptin / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology*; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology; D020836:Protein Structure, Quaternary; D054411:Receptors, Leptin / Q000187:drug effects* / Q000378:metabolism
chemical_list: D000939:Epitopes; C515448:LEPR protein, human; D020738:Leptin; D010446:Peptide Fragments; D054411:Receptors, Leptin