Abstract
Two peptide-linker-lipid constructs were designed and prepared which target the parathyroid hormone 1 receptor, a family B G protein-coupled receptor. Both show increased agonist activity in a cell-based assay. The lipid moiety enables the formation of micelle-like nanostructures, which is shown to hinder proteolytic digestion and is expected to reduce renal clearance.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Dose-Response Relationship, Drug
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HEK293 Cells
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Humans
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Ligands
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Lipids / chemistry
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Lipids / pharmacology*
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Molecular Structure
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Peptides / chemistry
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Peptides / pharmacology*
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Receptor, Parathyroid Hormone, Type 1 / biosynthesis*
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Receptor, Parathyroid Hormone, Type 1 / genetics
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Structure-Activity Relationship
Substances
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Ligands
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Lipids
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PTH1R protein, human
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Peptides
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Receptor, Parathyroid Hormone, Type 1