Sixnewendomorphinanalogues,incorporatingconstrainedaminoacidsinplaceofnativeprolinehave beensynthesized.Residuesof(S)-azetidine-2-carboxylicacid(Aze),3,4-dehydro-(S)-proline(D3 Pro), azetidine-3-carboxylicacid(3Aze)anddehydro-alanine(DAla)havebeenusedtoprepare[D3 Pro2 ]EM- 2(1),[Aze2 ]EM-1(2),[Aze2 ]EM-2(3),[3Aze2 ]EM-1(4),[3Aze2 ]EM-2(5)and[DAla2 ]EM-2(6).Binding assaysandfunctionalbioactivitiesfor l-and d-receptorsarereported.Thehighestaffinity,bioactivity andselectivityareshownbypeptides 2 and 3 containingtheAzeresidue.
Synthesys and evaluation of new endomorphin analogues modified at the Pro2 residue
MOLLICA, ADRIANO;PINNEN, Francesco Enrico;FELICIANI, FEDERICA;
2009-01-01
Abstract
Sixnewendomorphinanalogues,incorporatingconstrainedaminoacidsinplaceofnativeprolinehave beensynthesized.Residuesof(S)-azetidine-2-carboxylicacid(Aze),3,4-dehydro-(S)-proline(D3 Pro), azetidine-3-carboxylicacid(3Aze)anddehydro-alanine(DAla)havebeenusedtoprepare[D3 Pro2 ]EM- 2(1),[Aze2 ]EM-1(2),[Aze2 ]EM-2(3),[3Aze2 ]EM-1(4),[3Aze2 ]EM-2(5)and[DAla2 ]EM-2(6).Binding assaysandfunctionalbioactivitiesfor l-and d-receptorsarereported.Thehighestaffinity,bioactivity andselectivityareshownbypeptides 2 and 3 containingtheAzeresidue.File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
