The influence of glycosylation on the structure-activity relationship of the tachykinin antagonist MEN10376 and of its minimal active fragment MEN10414 was investigated. The antagonist activity was preserved only when beta-D.glucosylated Tyr, Ser and Asn were added to the N-terminal position of MEN10376, while the modification of the side chain of the Tyr-2 induced a dramatic decrease in affinity.
Glycosyl derivatives of NK2 tachykinin receptor antagonists / D. PINZANI; A.M. PAPINI; M.E.VALLECCHI; M. CHELLI; M. GINANNESCHI; G. RAPI; L. QUARTARA; R. PATACCHINI; C.A. MAGGI.; F.M. ARCAMONE. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 6:(1996), pp. 367-372.
Glycosyl derivatives of NK2 tachykinin receptor antagonists.
PAPINI, ANNA MARIA;M. GINANNESCHI;
1996
Abstract
The influence of glycosylation on the structure-activity relationship of the tachykinin antagonist MEN10376 and of its minimal active fragment MEN10414 was investigated. The antagonist activity was preserved only when beta-D.glucosylated Tyr, Ser and Asn were added to the N-terminal position of MEN10376, while the modification of the side chain of the Tyr-2 induced a dramatic decrease in affinity.File | Dimensione | Formato | |
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