Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities.
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).
Lundquist
J T
JT
Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston 29425-2303, USA.
Büllesbach
E E
EE
Dix
T A
TA
D000818:Animals; D016466:CHO Cells; D002851:Chromatography, High Pressure Liquid; D006224:Cricetinae; D006801:Humans; D008970:Molecular Weight; D009496:Neurotensin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018028:Receptors, Neurotensin / Q000378:metabolism*; D013329:Structure-Activity Relationship
D010446:Peptide Fragments; D018028:Receptors, Neurotensin; C409806:neurotensin (9-13); D009496:Neurotensin