The use of tripeptides for lead discovery of 5-HT4 receptor ligands.
A series of 30 tripeptides were synthesized and tested as novel 5-HT4 receptor ligands. Receptor binding assays showed that a subset of compounds had reasonable potency relative to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses and molecular docking have highlighted avenues for further synthetic work.
Hanna-Elias
A
A
Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Vic. 3052, Australia.
Thompson
P E
PE
Manallack
D T
DT
Irving
H R
HR
Coupar
I M
IM
Berque-Bestel
I
I
Iskander
M N
MN
D000595:Amino Acid Sequence; D001679:Biogenic Amines / Q000378:metabolism; D055808:Drug Discovery; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism*; D044422:Receptors, Serotonin, 5-HT4 / Q000737:chemistry / Q000378:metabolism*
D001679:Biogenic Amines; D008024:Ligands; D009842:Oligopeptides; D044422:Receptors, Serotonin, 5-HT4