Preston S R, Woodhouse L F, Jones-Blackett S, Miller G V, Primrose J N
Academic Unit of Surgery, St. James's University Hospital, Leeds, UK.
Br J Cancer. 1995 May;71(5):1087-9. doi: 10.1038/bjc.1995.210.
Human colorectal cancer tissue and matched uninvolved mucosa from 21 patients were examined by radioligand displacement for the presence of binding sites for bombesin-like peptides. Five cancers, but no uninvolved mucosa, expressed high-affinity, low-capacity bombesin binding sites (Kd = 6.53 nM, Bmax = 58.6 fmol mg-1 protein) of the gastrin-releasing peptide (GRP)-preferring subtype (IC50 4.8 nM). Bombesin-like peptides may have a role in the pathogenesis of colorectal cancer, and bombesin receptor antagonists may be of value in the treatment of receptor-positive tumours.
对21例患者的人大肠癌组织及配对的未受累黏膜进行放射性配体置换检测，以确定是否存在蛙皮素样肽的结合位点。5例癌症组织表达了胃泌素释放肽（GRP）偏好亚型的高亲和力、低容量蛙皮素结合位点（解离常数Kd = 6.53 nM，最大结合容量Bmax = 58.6 fmol mg-1蛋白）（半数抑制浓度IC50为4.8 nM），而未受累黏膜则未表达。蛙皮素样肽可能在结直肠癌的发病机制中起作用，蛙皮素受体拮抗剂可能对治疗受体阳性肿瘤有价值。
