Abstract
To compare backbone-induced susceptibilities with affinity changes that are caused by side-chain modifications in the respective positions, structure activity relationship studies on a series of NT(8-13) analogues were performed providing valuable insights into the major requirement for neurotensin receptor recognition and activation. The data led us to highly potent NTR1 ligands and the generation of a pharmacophore model that will be helpful for the discovery of therapeutically relevant non-peptidic NTR1 agonists.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Calcium / metabolism
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Molecular Structure
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Mutagenesis, Site-Directed
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Mutation / genetics
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Neurotensin / chemistry*
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Neurotensin / metabolism
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Palladium / pharmacology
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Peptide Fragments / chemistry*
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Protein Binding
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RNA, Messenger / genetics
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RNA, Messenger / metabolism
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Receptors, Neurotensin / genetics
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Receptors, Neurotensin / metabolism*
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Reverse Transcriptase Polymerase Chain Reaction
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Structure-Activity Relationship
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Swine
Substances
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Peptide Fragments
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RNA, Messenger
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Receptors, Neurotensin
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neurotensin type 1 receptor
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Neurotensin
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Palladium
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Calcium