Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China.
Fujian Provincial Key Laboratory of Brain Aging and Neurodegenerative Diseases, School of Basic Medical Sciences, Fujian Medical University, Fuzhou, Fujian 350122, China.
J Med Chem. 2024 Sep 12;67(17):15118-15130. doi: 10.1021/acs.jmedchem.4c00759. Epub 2024 Aug 21.
B-cell maturation antigen (BCMA) has emerged as a promising tumor marker for the diagnosis and treatment of multiple myeloma. The noninvasive and rapid detection of BCMA expression in vivo provides significant value in screening and evaluating multiple myeloma patients receiving BCMA-targeted therapy. We identified the BCMA-targeting peptide BP1 from a one-bead-one-compound (OBOC) peptide library using a high-throughput microarray strategy. The BCMA-targeting specificity and affinity of BP1 were assessed by surface plasmon resonance imaging (SPRi), flow cytometry, and confocal imaging. BCMA-positive (H929) and BCMA-negative (K562) subcutaneous tumor models were established and labeled with Ga for BP1, followed by PET imaging and biodistribution studies. PET imaging demonstrated that Ga-labeled BP1 has significant specific uptake in multiple myeloma, enabling rapid identification of BCMA expression and precise delineation of the disease. Thus, BP1 represents an ideal candidate for multiple myeloma imaging.
B 细胞成熟抗原（BCMA）已成为多发性骨髓瘤诊断和治疗的有前途的肿瘤标志物。BCMA 表达的非侵入性和快速体内检测在接受 BCMA 靶向治疗的多发性骨髓瘤患者的筛选和评估中具有重要价值。我们使用高通量微阵列策略从一个珠一个化合物（OBOC）肽文库中鉴定出 BCMA 靶向肽 BP1。通过表面等离子体共振成像（SPRi）、流式细胞术和共聚焦成像评估了 BP1 的 BCMA 靶向特异性和亲和力。建立了 BCMA 阳性（H929）和 BCMA 阴性（K562）皮下肿瘤模型，并将 Ga 标记到 BP1 上，然后进行 PET 成像和生物分布研究。PET 成像表明，Ga 标记的 BP1 在多发性骨髓瘤中有明显的特异性摄取，能够快速识别 BCMA 表达并精确描绘疾病。因此，BP1 是多发性骨髓瘤成像的理想候选物。
