Abstract
An increasing number of studies demonstrate the ability of peptides to cross the blood-brain barrier (BBB), opening perspectives for a new class of therapeutics for central nervous system diseases. However, information on the BBB transport of peptides suffer from a wide variety in used methods and experimental set-up. Therefore, it is currently difficult, if not impossible, to classify peptides according to their BBB influx characteristics. To allow direct comparison of BBB influx results of peptides, we introduce a classification method and unified response for BBB influx transport of peptides. First, the results of BBB influx response types (i.e. Kin (MTR), Kin (Perfusion), Pin vitro and Pin vivo), which quantitatively express brain influx, were classified into five classes of BBB influx magnitude based on the distribution of these results for the individual response types. Then, these classes were converted to a BBBin-response, representing a scaled value ranging from zero (no influx) to ten (high influx), independent from the BBB influx response type from which it was derived. This unified response can immediately be applied for new BBB influx results of peptides and represents a ballpark figure for BBB influx and allows direct comparison and ranking of peptides independent of the response type.
Keywords: Blood-brain barrier, classification, influx, peptides, permeability, unified response.
Graphical Abstract
Protein & Peptide Letters
Title:Classification of Peptides According to their Blood-Brain Barrier Influx
Volume: 22 Issue: 9
Author(s): Sofie Stalmans, Bert Gevaert, Evelien Wynendaele, Joachim Nielandt, Guy De Tre, Kathelijne Peremans, Christian Burvenich and Bart De Spiegeleer
Affiliation:
Keywords: Blood-brain barrier, classification, influx, peptides, permeability, unified response.
Abstract: An increasing number of studies demonstrate the ability of peptides to cross the blood-brain barrier (BBB), opening perspectives for a new class of therapeutics for central nervous system diseases. However, information on the BBB transport of peptides suffer from a wide variety in used methods and experimental set-up. Therefore, it is currently difficult, if not impossible, to classify peptides according to their BBB influx characteristics. To allow direct comparison of BBB influx results of peptides, we introduce a classification method and unified response for BBB influx transport of peptides. First, the results of BBB influx response types (i.e. Kin (MTR), Kin (Perfusion), Pin vitro and Pin vivo), which quantitatively express brain influx, were classified into five classes of BBB influx magnitude based on the distribution of these results for the individual response types. Then, these classes were converted to a BBBin-response, representing a scaled value ranging from zero (no influx) to ten (high influx), independent from the BBB influx response type from which it was derived. This unified response can immediately be applied for new BBB influx results of peptides and represents a ballpark figure for BBB influx and allows direct comparison and ranking of peptides independent of the response type.
Export Options
About this article
Cite this article as:
Stalmans Sofie, Gevaert Bert, Wynendaele Evelien, Nielandt Joachim, De Tre Guy, Peremans Kathelijne, Burvenich Christian and De Spiegeleer Bart, Classification of Peptides According to their Blood-Brain Barrier Influx, Protein & Peptide Letters 2015; 22 (9) . https://dx.doi.org/10.2174/0929866522666150622101223
DOI https://dx.doi.org/10.2174/0929866522666150622101223 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Spatiotemporal Gait Characteristics Associated with Cognitive Impairment: A Multicenter Cross-Sectional Study, the Intercontinental “Gait, cOgnitiOn & Decline” Initiative
Current Alzheimer Research Metformin: A Growing Journey from Glycemic Control to the Treatment of Alzheimer’s Disease and Depression
Current Medicinal Chemistry Insulin-Degrading Enzyme: A Link Between Alzheimer’s and Type 2 Diabetes Mellitus
CNS & Neurological Disorders - Drug Targets Macaque CYP2C76 Encodes Cytochrome P450 Enzyme Not Orthologous to Any Human Isozymes
Current Drug Metabolism Orthostatic Hypotension: Evaluation and Treatment
Cardiovascular & Hematological Disorders-Drug Targets The Integration of the Glutamatergic and the White Matter Hypotheses of Schizophrenias Etiology
Current Neuropharmacology Arundic Acid a Potential Neuroprotective Agent: Biological Development and Syntheses
Current Medicinal Chemistry Editorial [Hot Topic: Cannabinoid Receptors Ligands (Guest Editor: Gabriele Murineddu)]
Recent Patents on CNS Drug Discovery (Discontinued) Age-Related Neurodegeneration Prevention Through mTOR Inhibition: Potential Mechanisms and Remaining Questions
Current Topics in Medicinal Chemistry Advanced Glycation End Products: Association with the Pathogenesis of Diseases and the Current Therapeutic Advances
Current Clinical Pharmacology Cytotoxic and Radio-sensitizing Effects of Polyphenolic Acetates in a Human Glioma Cell Line (BMG-1)
Current Pharmaceutical Design Statins and Alkylphospholipids as New Anticancer Agents Targeting Lipid Metabolism
Anti-Cancer Agents in Medicinal Chemistry Pathophysiological Role of Mitochondrial Potassium Channels and their Modulation by Drugs
Current Medicinal Chemistry Associations between Depressive Disorders and Inflammatory Rheumatic Diseases
Current Topics in Medicinal Chemistry Human Mesotrypsin Defies Natural Trypsin Inhibitors: From Passive Resistance to Active Destruction.
Protein & Peptide Letters New Strategies for Clinical Trials in Autism Spectrum Disorder
Reviews on Recent Clinical Trials Pharmacological Targeting of IDO-Mediated Tolerance for Treating Autoimmune Disease
Current Drug Metabolism Rikkunshito and Ghrelin Secretion
Current Pharmaceutical Design Nucleic Acid Aptamers Against Proteases
Current Medicinal Chemistry Rehab of NAD(P)-Dependent Enzymes with NAD(P)-Based Inhibitors
Current Medicinal Chemistry