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Improving oral bioavailability of peptides by multiple N-methylation: somatostatin analogues.
Low bioavailability of peptides following oral administration is attributed to their inactivation in the gastro–intestinal tract through enhanced enzymatic degradation in the gut wall by a variety ofExpand
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Carrier‐mediated transport of metformin across the human placenta determined by using the ex vivo perfusion of the placental cotyledon model
Metformin is a polar positively charged compound. The aim of the study was to characterize its permeability across the human placenta using the ex vivo placental perfusion model.
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Multiple N-methylation by a designed approach enhances receptor selectivity.
An unselective cyclic peptide integrin ligand was sequentially N-methylated by a designed approach, where only the externally oriented (solvent exposed) amide bonds were N-methylated. TheExpand
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The effect of multiple N-methylation on intestinal permeability of cyclic hexapeptides.
Recent progress in peptide synthesis simplified the synthesis of multiple N-methylation of peptides. To evaluate how multiple N-methylation affects the bioavailability of peptides, a poly alanineExpand
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Prokineticins (endocrine gland-derived vascular endothelial growth factor and BV8) in the bovine ovary: expression and role as mitogens and survival factors for corpus luteum-derived endothelial
A highly vascular endocrine gland, the corpus luteum (CL) is an excellent model for the study of angiogenic factors. Prokineticins (PK-1 and -2), also termed endocrine-gland-derived vascularExpand
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Structure-activity relationship and metabolic stability studies of backbone cyclization and N-methylation of melanocortin peptides.
Backbone cyclization (BC) and N-methylation have been shown to enhance the activity and/or selectivity of biologically active peptides and improve metabolic stability and intestinal permeability. InExpand
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Differential Expression of Prokineticin Receptors by Endothelial Cells Derived from Different Vascular Beds: a Physiological Basis for Distinct Endothelial Function
Prokineticins (PKs), multifunctional secreted proteins, activate two endogenous G protein-coupled receptors (R) termed PK-R1 and PK-R2. It was suggested that PK1 acts selectively on the endotheliumExpand
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cis-Peptide Bonds: A Key for Intestinal Permeability of Peptides? .
Recent structural studies on libraries of cyclic hexapeptides led to the identification of common backbone conformations that may be instrumental to the oral availability of peptides. Furthermore,Expand
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Intestinal permeability of cyclic peptides: common key backbone motifs identified.
Insufficient oral bioavailability is considered as a key limitation for the widespread development of peptides as therapeutics. While the oral bioavailability of small organic compounds is oftenExpand
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Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
The tetrapeptide sequence His-Phe-Arg-Trp, derived from melanocyte-stimulating hormone (alphaMSH) and its analogs, causes a decrease in food intake and elevates energy utilization upon binding to theExpand
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