Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities

J T Lundquist 4th; E E Büllesbach; T A Dix

doi:10.1016/s0960-894x(00)00018-4

Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities

Bioorg Med Chem Lett. 2000 Mar 6;10(5):453-5. doi: 10.1016/s0960-894x(00)00018-4.

Authors

J T Lundquist 4th¹, E E Büllesbach, T A Dix

Affiliation

¹ Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston 29425-2303, USA.

PMID: 10743946
DOI: 10.1016/s0960-894x(00)00018-4

Abstract

Recent evidence is consistent with neurotensin (NT)(8-13) adopting a Type I beta-turn conformation while binding the NT receptor, which would place the cationic side-chains of Arg(8) and Arg(9) in close proximity. This was the basis for the design, synthesis and analysis of truncated NT(9-13) analogues 1-5 with dicationic position 9 side-chains to emulate the functions of the 8 and 9 side-chains of NT(8-13).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
CHO Cells
Chromatography, High Pressure Liquid
Cricetinae
Humans
Molecular Weight
Neurotensin / analogs & derivatives*
Neurotensin / chemical synthesis
Neurotensin / chemistry
Neurotensin / pharmacology*
Peptide Fragments / chemical synthesis
Peptide Fragments / chemistry
Peptide Fragments / pharmacology*
Receptors, Neurotensin / metabolism*
Structure-Activity Relationship

Substances

Peptide Fragments
Receptors, Neurotensin
neurotensin (9-13)
Neurotensin