癌症分子影像技术利用特定的探针设计来识别癌症目标蛋白是一种强大的工具，可以指导治疗选择、患者管理和随访。我们证明icatibant可以用作肠癌（CRC）中显著上调的缓激肽B2R的靶向探针。鉴定出具有高亲和力的以缓激肽B2R为靶点的icatibant基于探针。近红外荧光染料偶联物MPA-PEG3-k-Icatibant和放射性偶联物[99mTc]Tc-HYNIC-PEG4-Icatibant在皮下移植和正常肠肿瘤小鼠模型中，分别使用近红外荧光成像和单光子发射计算机体层摄影（SPECT-CT）时，表现出有利的选择性和特异性摄取肿瘤的属性。[99mTc]Tc-HYNIC-PEG4-Icatibant的示踪剂在生物分布研究中在肿瘤中积累，注射静脉（i.v.）后在HT29肿瘤小鼠中在4小时时达到3.41±0.27% ID / g的摄取值。尾静脉注射后1、2、4和6小时的肿瘤与结肠信号比分别为5.03±0.37、15.45±0.32、13.58±1.19和11.33±1.73。总体而言，在快速和精确的肿瘤描绘和穿透特性之后，基于icatibant的探针代表了检测缓激肽B2R的有前途的高对比度分子影像探针。 版权所有©2023 Elsevier B.V.。

Cancer molecular imaging using specific probes designed to identify target proteins in cancer is a powerful tool to guide therapeutic selection, patient management, and follow-up. We demonstrated that icatibant may be used as a targeting probe for the significantly upregulated bradykinin B2R in colorectal cancer (CRC). Icatibant-based probes with high affinity towards bradykinin B2R were identified. The near-infrared (NIR) fluorescent dye conjugate MPA-PEG3-k-Icatibant and radioconjugate [99mTc]Tc-HYNIC-PEG4-Icatibant exhibited favourable selective and specific uptake in tumours when the subcutaneous and orthotopic colorectal tumour-bearing mouse models were imaged using NIR fluorescence imaging and Single-Photon Emission Computed Tomography-Computed Tomography (SPECT-CT), respectively. The tracer of [99mTc]Tc-HYNIC-PEG4-Icatibant accumulated in tumours according to biodistribution studies and peaked at 4 h with an uptake value of 3.41 ± 0.27%ID/g in HT29 tumour-bearing nude mice following intravenous injection (i.v.). The tumour-to-colorectal signal ratios were 5.03 ± 0.37, 15.45 ± 0.32, 13.58 ± 1.19 and 11.33 ± 1.73 1, 2, 4 and 6 h after tail-veil injection, respectively. Overall, in the wake of rapid and precise tumour delineation and penetration characteristics, icatibant-based probes represent promising high-contrast molecular imaging probes for the detection of bradykinin B2R.Copyright © 2023 Elsevier B.V. All rights reserved.