Synthesis and purification of two SP (6-11) analogues with enhanced selectivity for the NK-1 receptor.
Two hexapeptide analogues of Substance P (6-11) have been synthesized. Replacement of Gly9 by proline provides a peptide with tenfold enhanced selectivity for the NK-1 receptor. The corresponding proline-containing glycopeptide incorporating a beta-D-glucopyranosyl residue linked to the side-chain of Glu6 was 100 times more selective than Substance P for the same receptor.
Haro
I
I
Laboratory of Peptides, Biological Organic Chemistry Department, C.I.D., C.S.I.C., Barcelona, Spain.
Torres
J L
JL
Valencia
G
G
Garcia Anton
J M
JM
Reig
F
F
D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D010446:Peptide Fragments; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D013373:Substance P
D010446:Peptide Fragments; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D013373:Substance P; C032292:substance P (6-11); D011761:Pyrrolidonecarboxylic Acid