Tian X, Aruva M R, Wolfe H R, Qin W, Sauter E R, Thakur M L, Waldman S A, Wickstrom E
Biochemistry and Molecular Pharmacology, Thomas Jefferson University, Philadelphia, Pennsylvania, USA.
Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):1085-91. doi: 10.1081/ncn-200059177.
We have optimized a method involving continuous solid phase synthesis of chelator-peptide-PNA-peptide probes in order to noninvasively image oncogene mRNAs overexpressed in tumors. The PNA (peptide nucleic acid) probes carry cyclized peptide ligand analogs specific for receptors overexpressed on malignant breast or colorectal cancer cells, and chelators to bind radioactive metal ions, or a fluorophore. In vivo scintigraphic imaging of MCF7 xenografts in immunocompromised mice indicated that CCND1 and MYC [99sTc] chelator-PNA-D (CSKC) probes concentrated in MCF7 cells up to 7 times more than the corresponding mismatch controls.
我们优化了一种方法，该方法涉及螯合剂 - 肽 - PNA - 肽探针的连续固相合成，以便对肿瘤中过表达的癌基因mRNA进行无创成像。PNA（肽核酸）探针携带对恶性乳腺癌或结肠直肠癌细胞上过表达的受体具有特异性的环化肽配体类似物，以及用于结合放射性金属离子或荧光团的螯合剂。免疫缺陷小鼠体内MCF7异种移植物的闪烁成像表明，CCND1和MYC [99sTc]螯合剂 - PNA - D（CSKC）探针在MCF7细胞中的富集程度比相应的错配对照高7倍。
