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...
Fei Liu; Teli Liu; Xiaoxia Xu; Xiaoyi Guo; Nan Li; Chiyi Xiong; Chun Li; Hua Zhu; Zhi Yang
Chemokine receptor CXCR4 plays an important role in cancer cell invasion and metastasis. Recent findings suggest that anti-VEGF therapies upregulate CXCR4 expression, which contributes to resistance to antiangiogenic therapies. Here, we report the development of novel derivatives of polyeth ... mehr
The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensol ... mehr
The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ... mehr