Bone Metastasis Imaging with Copper-64-labeled Peptides

描述（由申请人提供）：本提案的目的是解决关于癌症成像和治疗的假设，特别是用靶向avB 3整联蛋白的64 Cu标记肽靶向癌症转移过程。癌症转移到骨的过程已显示高度依赖于整联蛋白，特别是B3整联蛋白的存在。开发一种特异性靶向avB 3整联蛋白的骨显像剂将允许临床医生有区别地靶向骨转移部位，并允许他们更好地确定患者治疗的疗效，并根据需要计划额外的治疗。简言之，具体目的是（1）开发具有增强的体内稳定性的64 Cu-CB-配体缀合肽。(2)使用微PET成像结合体外分析来确定这些64 Cu-CB配体缀合的肽对avB 3整联蛋白的结合亲和力，并评价放射性药物作为PET骨转移成像剂的用途;和（3）评价这些64 Cu-CB-配体缀合的肽作为骨转移的治疗剂。

DESCRIPTION (provided by applicant): The goal of this proposal is to address hypotheses regarding the imaging and therapy of cancer, in particular the targeting of the process of cancer metastasis with 64Cu-labeled peptides that target the avB3 integrin. The process of cancer metastasizing to the bone has been shown to be highly dependent on the presence of integrins, in particular the B3 integrin. Developing a bone imaging agent which specifically targets the avB3 integrin will allow clinicians to discriminately target sites of bone metastasis and would permit them to better determine the efficacy of a patient's treatment and plan additional therapy as needed. The specific aims, in brief, are (1) to develop 64Cu-CB-ligand conjugated peptides which possess enhanced in vivo stability. (2) Use micro PET imaging in conjunction with in vitro analysis to determine the binding affinity of these 64Cu-Cbligand conjugated peptides for the avB3 integrin, and to evaluate the use of the radiopharmaceuticals as PET bone metastasis imaging agents; and (3) to evaluate these 64Cu-CB-ligand conjugated peptides as therapeutic agents for bone metastasis.