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Design, Synthesis, and Biological Evaluation of 68Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Most of the radiolabeled somatostatin analogues (SSAs) are specific for subtype somatostatin receptor 2 (SSTR2). Lack of ligands targeting other subtypes of SSTRs, especially SSTR1, SSTR3, and SSTR5, limited their applications in tumors of low SSTR2 expression, including lung tumor. In this study, we aimed to design and synthesize a positron emission tomography (PET) radiotracer targeting multi-subtypes of SSTRs for PET imaging. PA1 peptide and its conjugate with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator or fluorescein isothiocyanate (FITC) at the N-terminal of the lysine position were synthesized. 68Ga was chelated to DOTA–PA1 to obtain 68Ga-DOTA–PA1 radiotracer. The stability, lipophilicity, binding affinity, and binding specificity of 68Ga-DOTA–PA1 and FITC–PA1 were evaluated by various in vitro experiments. Micro-PET imaging of 68Ga-DOTA–PA1 was performed in nude mice bearing A549 lung adenocarcinoma, as compared with 68Ga-DOTA-(Tyr3)-octreotate (68Ga-DOTA-TATE). Histolo...

Autoren:   Fei Liu; Teli Liu; Xiaoxia Xu; Xiaoyi Guo; Nan Li; Chiyi Xiong; Chun Li; Hua Zhu; Zhi Yang
Journal:   Molecular Pharmaceutics
Jahrgang:   2018
DOI:   10.1021/acs.molpharmaceut.7b00963
Erscheinungsdatum:   19.01.2018
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