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Analog mini-gastryny, w szczególności do zastosowania w diagnozowaniu i/lub leczeniu guza nowotworowego dodatniego pod względem receptora CCK2
专利权人:
Paul Scherrer Institut
发明人:
BEHE, MARTIN,SCHIBLI, ROGER
申请号:
PL14795569
公开号:
PL3065764T3
申请日:
2014.10.23
申请国别(地区):
PL
年份:
2018
代理人:
摘要:
It is the objective of the present invention to provide a gastrin analogue which show high uptake in CCK-2 receptor positive tumours by simultaneously very low accumulation in the kidneys. This objective is achieved according to the present invention by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH 2 , wherein Y stands for an amino acid replacing methionine and X stands for a chemical group attached to the peptide for the purpose of diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. In particular, very suitable compounds with respect to a high tumour to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidised easily which is a disadvantage for clinical application under GMP due to the forms which may occur. Therefore, the elimination of the methionine leads to a lower affinity to oxidation which in general favours the tumour-kidney-ratio. In a preferred embodiment of the present invention, the methionine is replaced by norleucine. This so-called PP-F11N mini gastrin exhibits currently the best tumour-kidney-ratio and is therefore the most promising candidate for clinical applications.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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