Pharmacological Potential of the Endogenous Dipeptide Kyotorphin and Selected Derivatives
| العنوان: | Pharmacological Potential of the Endogenous Dipeptide Kyotorphin and Selected Derivatives |
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| المؤلفون: | Miguel A. R. B. Castanho, Juliana Perazzo, Sónia Sá Santos |
| المساهمون: | Repositório da Universidade de Lisboa |
| المصدر: | Frontiers in Pharmacology Repositório Científico de Acesso Aberto de Portugal Repositório Científico de Acesso Aberto de Portugal (RCAAP) instacron:RCAAP |
| بيانات النشر: | Frontiers Media S.A., 2017. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | 0301 basic medicine, Biological effects, Drug candidates, Endogeny, Review, Pharmacology, Blood–brain barrier, blood–brain barrier, kyotorphin-derived peptides, Neuroprotection, Kyotorphin, Kyotorphin-derived peptides, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, medicine, Pharmacology (medical), drug candidates, Receptor, Dipeptide, biological effects, Biological activity, Clinical application, 3. Good health, clinical application, 030104 developmental biology, medicine.anatomical_structure, Biochemistry, Mechanism of action, chemistry, medicine.symptom, kyotorphin, 030217 neurology & neurosurgery |
| الوصف: | Copyright © 2017 Perazzo, Castanho and Sá Santos. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. The endogenous peptide kyotorphin (KTP) has been extensively studied since it was discovered in 1979. The dipeptide is distributed unevenly over the brain but the majority is concentrated in the cerebral cortex. The putative KTP receptor has not been identified yet. As many other neuropeptides, KTP clearance is mediated by extracellular peptidases and peptide transporters. From the wide spectrum of biological activity of KTP, analgesia was by far the most studied. The mechanism of action is still unclear, but researchers agree that KTP induces Met-enkephalins release. More recently, KTP was proposed as biomarker of Alzheimer disease. Despite all that, KTP limited pharmacological value prompted researchers to develop derivatives more lipophilic and therefore more prone to cross the blood-brain barrier (BBB), and also more resistant to enzymatic degradation. Conjugation of KTP with functional molecules, such as ibuprofen, generated a new class of compounds with additional biological properties. Moreover, the safety profile of these derivatives compared to opioids and their efficacy as neuroprotective agents greatly increases their pharmacological value. Funding was provided by the Portuguese Agency Fundação para a Ciência e a Tecnologia (SFRH/BPD/79542/2011 fellowship to SS and SFRH/BD/52225/2013 fellowship to JP), and by Marie Skłodowska-Curie Research and Innovation Staff Exchange (RISE): call H2020-MSCA-RISE-2014, Grant agreement 644167, 2015-2019. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1663-9812 2015-2019 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57955b649a11a4dd0b8807dfb5baccba http://europepmc.org/articles/PMC5226936 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....57955b649a11a4dd0b8807dfb5baccba |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 16639812 20152019 |
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