Development of LHRH antagonists suitable for oral administration via the VB12 uptake system

G. J. Russell-Jones; S. W. Westwood; B. McInerney; P. G. Farnworth; J. K. Findlay; H. G. Burger

Development of LHRH antagonists suitable for oral administration via the VB₁₂ uptake system

G. J. Russell-Jones^*, S. W. Westwood, B. McInerney, P. G. Farnworth, J. K. Findlay, H. G. Burger

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

Abstract

Preliminary research has shown that it is possible to make two analogues of ANTIDE, ANTIDE-1 and ANTIDE-3 that have activities similar to ANTIDE in the rat pituitary cell assay. Direct conjugation of these analogues to VB₁₂ dramatically reduced the bio-activity of either analogue. Conjugation of either ANTIDE-1 or ANTIDE-3 to VB₁₂ via extended spacers regenerated their in vitro activity, however their in vivo activity was still greatly diminished. Conjugation of either analogue to VB₁₂ via thiol cleavable spacers gave rise to analogues with similar in vitro and in vivo bio-activity to ANTIDE.

Original language	English
Pages (from-to)	35-36
Number of pages	2
Journal	Proceedings of the Controlled Release Society
Issue number	21
Publication status	Published - 12 Dec 1994
Externally published	Yes

Cite this

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title = "Development of LHRH antagonists suitable for oral administration via the VB12 uptake system",

abstract = "Preliminary research has shown that it is possible to make two analogues of ANTIDE, ANTIDE-1 and ANTIDE-3 that have activities similar to ANTIDE in the rat pituitary cell assay. Direct conjugation of these analogues to VB12 dramatically reduced the bio-activity of either analogue. Conjugation of either ANTIDE-1 or ANTIDE-3 to VB12 via extended spacers regenerated their in vitro activity, however their in vivo activity was still greatly diminished. Conjugation of either analogue to VB12 via thiol cleavable spacers gave rise to analogues with similar in vitro and in vivo bio-activity to ANTIDE.",

author = "Russell-Jones, {G. J.} and Westwood, {S. W.} and B. McInerney and Farnworth, {P. G.} and Findlay, {J. K.} and Burger, {H. G.}",

year = "1994",

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language = "English",

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journal = "Proceedings of the Controlled Release Society",

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AU - Russell-Jones, G. J.

AU - Westwood, S. W.

AU - McInerney, B.

AU - Farnworth, P. G.

AU - Findlay, J. K.

AU - Burger, H. G.

PY - 1994/12/12

Y1 - 1994/12/12

N2 - Preliminary research has shown that it is possible to make two analogues of ANTIDE, ANTIDE-1 and ANTIDE-3 that have activities similar to ANTIDE in the rat pituitary cell assay. Direct conjugation of these analogues to VB12 dramatically reduced the bio-activity of either analogue. Conjugation of either ANTIDE-1 or ANTIDE-3 to VB12 via extended spacers regenerated their in vitro activity, however their in vivo activity was still greatly diminished. Conjugation of either analogue to VB12 via thiol cleavable spacers gave rise to analogues with similar in vitro and in vivo bio-activity to ANTIDE.

AB - Preliminary research has shown that it is possible to make two analogues of ANTIDE, ANTIDE-1 and ANTIDE-3 that have activities similar to ANTIDE in the rat pituitary cell assay. Direct conjugation of these analogues to VB12 dramatically reduced the bio-activity of either analogue. Conjugation of either ANTIDE-1 or ANTIDE-3 to VB12 via extended spacers regenerated their in vitro activity, however their in vivo activity was still greatly diminished. Conjugation of either analogue to VB12 via thiol cleavable spacers gave rise to analogues with similar in vitro and in vivo bio-activity to ANTIDE.

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M3 - Article

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JO - Proceedings of the Controlled Release Society

JF - Proceedings of the Controlled Release Society

SN - 1076-0458

IS - 21

ER -

Development of LHRH antagonists suitable for oral administration via the VB₁₂ uptake system

Abstract

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