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Mini-gastrin analogue, in particular for use in CCK2 receptor positive tumour diagnosis and/or treatment
专利权人:
PAUL SCHERRER INSTITUT
发明人:
MARTIN, BEHE,ROGER, SCHIBLI
申请号:
TR201802723
公开号:
TR201802723T4
申请日:
2014.10.23
申请国别(地区):
TR
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-NH2, 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.CCK-2 reseptör pozitif tümörlerde eşzamanlı olarak böbreklerde çok düşük birikim ile yüksek tutulum gösteren bir gastrin analogunun sağlanması mevcut buluşun bir amacıdır. Bu amaca PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH2 formülüne sahip bir mini-gastrin analogu yoluyla ulaşılmakta olup, burada Y metiyoninin yerine geçen bir amino asidi, X ise CCK-2 reseptörü ile ilgili hastalıklarda tanısal ve/veya terapötik müdahale amacıyla peptide bağlanmış bir kimyasal grubu temsil etmektedir.
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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