Bone Metastasis Imaging with Copper-64-labeled Peptides

描述（由申请人提供）：本提案的目标是解决有关癌症成像和治疗的假设，特别是针对avB3整合素的64cu标记肽靶向癌症转移过程。癌症骨转移的过程已被证明高度依赖于整合素的存在，特别是B3整合素。开发一种专门针对avB3整合素的骨显像剂，将使临床医生能够区分骨转移部位，并使他们能够更好地确定患者的治疗效果，并根据需要计划额外的治疗。简而言之，具体目标是：(1)开发具有增强体内稳定性的64cu - cb配体共轭肽。(2)利用微PET成像结合体外分析，确定64Cu-Cbligand偶联肽对avB3整合素的结合亲和力，并评价放射性药物作为PET骨转移显像剂的应用；(3)评价这些64cu - cb配体结合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.