Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.
Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is preferentially adopted to rationalize the obtained results.
Altamura
Maria
M
Menarini Ricerche S.p.A., Via dei Sette Santi 3, Florence, Italy.
Canfarini
Franca
F
Catalioto
Rose-Marie
RM
Guidi
Antonio
A
Pasqui
Franco
F
Renzetti
Anna R
AR
Triolo
Antonio
A
Maggi
Carlo A
CA
D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008024:Ligands; D013058:Mass Spectrometry; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000494:pharmacology; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism
D008024:Ligands; C463499:MEN 11558; D010455:Peptides; D010456:Peptides, Cyclic; D018041:Receptors, Neurokinin-2