HAI Peptide and Backbone Analogs—Validation and Enhancement of Biostability and Bioactivity of BBB Shuttles

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dc.contributor.authorPrades, Roger
dc.contributor.authorGuixer, Bernat
dc.contributor.authorGuerrero, Simón
dc.contributor.authorAraya, Eyleen
dc.contributor.authorCiudad, Sonia
dc.contributor.authorKogan, Marcelo J.
dc.contributor.authorGiralt, Ernesta
dc.contributor.authorTeixidó, Meritxell
dc.contributor.authorArranz-Gibert, Pol
dc.date.accessioned2022-06-22T13:37:43Z
dc.date.available2022-06-22T13:37:43Z
dc.date.issued2018-12
dc.descriptionIndexación Scopuses
dc.description.abstractLow effectiveness and resistance to treatments are commonplace in disorders of the central nervous system (CNS). These issues concern mainly the blood-brain barrier (BBB), which preserves homeostasis in the brain and protects this organ from toxic molecules and biohazards by regulating transport through it. BBB shuttles—short peptides able to cross the BBB—are being developed to help therapeutics to cross this barrier. BBB shuttles can be discovered by massive exploration of chemical diversity (e.g. computational means, phage display) or rational design (e.g. derivatives from a known peptide/protein able to cross). Here we present the selection of a peptide shuttle (HAI) from several candidates and the subsequent in-depth in vitro and in vivo study of this molecule. In order to explore the chemical diversity of HAI and enhance its biostability, and thereby its bioactivity, we explored two new protease-resistant versions of HAI (i.e. the retro-D-version, and a version that was N-methylated at the most sensitive sites to enzymatic cleavage). Our results show that, while both versions of HAI are resistant to proteases, the retro-D-approach preserved better transport properties. © 2018, The Author(s).es
dc.description.urihttps://www-nature-com.recursosbiblioteca.unab.cl/articles/s41598-018-35938-8
dc.identifier.citationScientific Reports Volume 8, Issue 11 December 2018 Article number 17932es
dc.identifier.doi10.1038/s41598-018-35938-8
dc.identifier.issn20452322
dc.identifier.urihttps://repositorio.unab.cl/xmlui/handle/ria/22929
dc.language.isoenes
dc.publisherNature Publishing Groupes
dc.subjectDrug Delivery Systemses
dc.subjectBlood-Brain Barrieres
dc.subjectTransferrin Receptorses
dc.titleHAI Peptide and Backbone Analogs—Validation and Enhancement of Biostability and Bioactivity of BBB Shuttleses
dc.typeArtículoes
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