Equilibrium studies of a fluorescent tacrolimus binding to surfactant protein A

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dc.contributor.authorCañadas, O
dc.contributor.authorSáenz, A
dc.contributor.authorOrellana Moraleda, Guillermo
dc.contributor.authorCasals Carro, María Cristina
dc.date.accessioned2024-01-15T11:31:30Z
dc.date.available2024-01-15T11:31:30Z
dc.date.issued2005-05-01
dc.description.abstractTacrolimus (FK506) is a hydrophobic immunosuppressive agent used in kidney, liver, and lung transplantation. The objective of this study was to characterize the binding of FK506 to surfactant protein A (SP-A), an abundant lipoprotein found in the alveolar fluid that functions as part of the innate immune system in the lung. We have synthesized a novel derivative of FK506 in which a dansyl moiety was covalently bound via cadaverine to the C22 position of the FK506 molecule (DNS-FK). Using the fluorescence and anisotropy properties of DNS-FK, we demonstrated that tacrolimus avidly binds to SP-A with an apparent equilibrium association constant (K(app)) of 10(7)M(-1) and a Gibbs binding free energy of -40 kJ mol(-1)K(-1). Derivatization of FK506 at the C22 position did not block FK506 binding to the cytosolic immunophilin FK506-binding protein (FK-BP) or human serum albumin (HSA), both used as controls of tacrolimus-binding proteins. K(app) for FK-BP/DNS-FK and HSA/DNS-FK complexes were 1.5 x 10(7) and 10(7)M(-1), respectively. The high sensitivity of this analytical technique makes it suitable for binding analysis of FK506 to proteins
dc.description.departmentDepto. de Bioquímica y Biología Molecular
dc.description.departmentDepto. de Química Orgánica
dc.description.facultyFac. de Ciencias Biológicas
dc.description.facultyFac. de Ciencias Químicas
dc.description.refereedTRUE
dc.description.sponsorshipFondo de Investigacion Sanitaria
dc.description.sponsorshipMCyT
dc.description.sponsorshipFujisawa GmbH
dc.description.statuspub
dc.identifier.citationCañadas O, Sáenz A, Orellana G, Casals C. Equilibrium studies of a fluorescent tacrolimus binding to surfactant protein A. Anal. Biochem. 2005 May 1; 340(1): 57-65. 2005
dc.identifier.doi10.1016/j.ab.2005.01.056
dc.identifier.issn0003-2697
dc.identifier.urihttps://hdl.handle.net/20.500.14352/93041
dc.issue.number1
dc.journal.titleAnalytical Biochemistry
dc.language.isoeng
dc.page.final65
dc.page.initial57
dc.rightsAttribution-NoDerivatives 4.0 Internationalen
dc.rights.accessRightsopen access
dc.rights.urihttp://creativecommons.org/licenses/by-nd/4.0/
dc.subject.cdu547
dc.subject.cdu577.1
dc.subject.keywordFluorescent tacrolimus
dc.subject.keywordDansylcadaverine-FK506
dc.subject.keywordSP-A
dc.subject.keywordFK506 binding protein
dc.subject.keywordHuman serum albumin
dc.subject.keywordFluorescence anisotropy assay
dc.subject.ucmCiencias
dc.subject.unesco23 Química
dc.subject.unesco24 Ciencias de la Vida
dc.titleEquilibrium studies of a fluorescent tacrolimus binding to surfactant protein A
dc.typejournal article
dc.type.hasVersionVoR
dc.volume.number340
dspace.entity.typePublication
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relation.isAuthorOfPublicationd4e23d80-fa5c-4614-bd2d-2c391b596713
relation.isAuthorOfPublication.latestForDiscoverydefd6c32-fdda-4eae-8e60-5942fcbed64b
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