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Binding of 3H-melatonin to calmodulin.

dc.creatorBenítez-King, G
dc.creatorHuerto-Delgadillo, L
dc.creatorAntón-Tay, F.
dc.date.accessioned2017-06-29T04:16:46Z
dc.date.available2017-06-29T04:16:46Z
dc.date.issued1993es_ES
dc.identifier164es_ES
dc.identifier.issn0024-3205es_ES
dc.identifier.urihttp://repositorio.inprf.gob.mx/handle/123456789/4858
dc.identifier.urihttps://doi.org/10.1016/0024-3205(93)90670-Xes_ES
dc.language.isoenges_ES
dc.relation53 (3) 201-207 p.es_ES
dc.relationversión del editores_ES
dc.rightsacceso cerradoes_ES
dc.titleBinding of 3H-melatonin to calmodulin.es_ES
dc.typearticlees_ES
dc.contributor.affiliationInstituto Mexicano de Psiquiatría, Departamento de Neurofarmacología, D.F.es_ES
dc.relation.jnabreviadoLIFE SCIes_ES
dc.relation.journalLife Scienceses_ES
dc.identifier.placeEnglandes_ES
dc.date.published1993es_ES
dc.identifier.organizacionInstituto Mexicano de Psiquiatríaes_ES
dc.description.abstractotrodiomaStudies in melatonin mechanism of action have suggested that one of them could be the binding of the hormone to calmodulin. We assessed calmodulin-melatonin binding by combining liposome incorporation of calmodulin with separation of free and bound 3H-Melatonin by a rapid ultrafiltration method. Specific binding to calmodulin was saturable, reversible, Ca(++)-dependent, ligand selective, and showed high affinity. Saturation as well as association-dissociation studies revealed that 3H-Melatonin binds to a single site on the calmodulin molecule with a Kd of 188 pM and a total binding capacity Bmax of 35 pM/ug of calmodulin. Displacement experiments showed that the relative order of potency of some compounds for inhibition of 3H-Melatonin was as follows: Melatonin > 6-chloromelatonin > 6-hydroxymelatonin > luzindole > trifluoperazine. The results explain our previously reported melatonin effects such as cytoskeletal rearrangements, inhibition of calmodulin dependent phosphodiesterase activity as well as the modification of Ca(++)-calmodulin electrophoretic mobility. The high affinity of melatonin binding to calmodulin suggests that the hormone is able to modulate cell activity by intracellularly binding to calmodulin at physiologically ranges. Melatonin-calmodulin binding could modulate many intracellular Ca++ functions and thus, the set-point for cell activity will follow the rhythmic circulating levels of the pineal hormone. Moreover, since calmodulin and melatonin are phylogenetically well preserved compounds, their interaction may represent a primary mechanism for both the regulation and the synchronization of cell physiologyes_ES


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