发明名称 Thiolation of peptides for radionuclide-based radiodetection and radiotherapy
摘要 A method of radiolabeling a peptide, e.g., somatostatin or an analogue thereof or vasoactive intestinal peptide, with a radioisotope of technetium or rhenium, comprises the steps of: (a) reacting the peptide with an acetyl-protected t-thiol-containing, amine-reactive bifunctional chelating agent; (b) deprotecting the acetyl-t-thiol group to generate a free t-thiol group; and either (c) admixing the peptide-t-thiol-containing conjugate with a stannous salt; and (d) reacting the mixture of step (c) with pertechnetate or perrhenate, or (c') adding reduced pertechnetate or perrhenate to said peptide-t-thiol-containing conjugate, thereby forming a radiolabeled peptide. Kits for effecting the radiolabeling method, and methods of tumor detection/imaging or therapy are provided.
申请公布号 US5746996(A) 申请公布日期 1998.05.05
申请号 US19950483095 申请日期 1995.06.07
申请人 IMMUNOMEDICS, INC. 发明人 GOVINDAN, SERENGULAM V.;GRIFFITHS, GARY L.;HANSEN, HANS L.
分类号 A61K38/00;A61K39/395;A61K51/00;A61K51/08;A61K51/10;A61P9/08;A61P9/10;A61P31/00;A61P35/00;A61P37/00;C07B59/00;C07K1/13;C07K14/00;C07K16/00;C09K3/00;(IPC1-7):A61K51/00;A61M36/14 主分类号 A61K38/00
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