Peptide drug modifications to enhance bioavailability and blood-brain barrier permeability

KA Witt, TJ Gillespie, JD Huber, RD Egleton, TP Davis - Peptides, 2001 - Elsevier
Peptides have the potential to be potent pharmaceutical agents for the treatment of many
central nervous system derived maladies. Unfortunately peptides are generally water …

Glycopeptide synthesis and the effects of glycosylation on protein structure and activity

O Seitz - ChemBioChem, 2000 - Wiley Online Library
Despite the omnipresence of protein glycosylation in nature, little is known about how the
attachment of carbohydrates affects peptide and protein activity. One reason is the lack of a …

[图书][B] Brain drug targeting: the future of brain drug development

WM Pardridge - 2001 - books.google.com
The thesis of this innovative and challenging book, first published in 2001, is that brain drug
development has been restricted by the failure of adequate brain drug targeting, and that …

Drug delivery across the blood-brain barrier

Y Chen, G Dalwadi, HAE Benson - Current drug delivery, 2004 - ingentaconnect.com
The brain is protected and isolated from the general circulation by a highly efficient blood-
brain barrier. This is characterised by relatively impermeable endothelial cells with tight …

Solid-phase synthesis of O-linked glycopeptide analogues of enkephalin

SA Mitchell, MR Pratt, VJ Hruby… - The Journal of Organic …, 2001 - ACS Publications
The synthesis of 18 N-α-FMOC-amino acid glycosides for solid-phase glycopeptide
assembly is reported. The glycosides were synthesized either from the corresponding …

Glycopeptide drugs: A pharmacological dimension between “Small Molecules” and “Biologics”

CR Apostol, M Hay, R Polt - Peptides, 2020 - Elsevier
Peptides are an important class of molecules with diverse biological activities. Many
endogenous peptides, especially neuropeptides and peptide hormones, play critical roles in …

Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability

EJ Bilsky, RD Egleton, SA Mitchell… - Journal of medicinal …, 2000 - ACS Publications
Endogenous peptides (eg enkephalins) control many aspects of brain function, cognition,
and perception. The use of these neuroactive peptides in diverse studies has led to an …

Peptidomimetics and their applications for opioid peptide drug discovery

YS Lee - Biomolecules, 2022 - mdpi.com
Despite various advantages, opioid peptides have been limited in their therapeutic uses due
to the main drawbacks in metabolic stability, blood-brain barrier permeability, and …

CNS drug delivery: opioid peptides and the blood-brain barrier

KA Witt, TP Davis - The AAPS journal, 2006 - Springer
Peptides are key regulators in cellular and intercellular physiological responses and
possess enormous promise for the treatment of pathological conditions. Opioid peptide …

Improved bioavailability to the brain of glycosylated Met-enkephalin analogs

RD Egleton, SA Mitchell, JD Huber, J Janders… - Brain research, 2000 - Elsevier
The blood–brain barrier prevents the entry of many potentially therapeutic peptide drugs to
the brain. Glycosylation has shown potential as a methodology for improving delivery to the …