Chakrabarti A, Aruva M R, Sajankila S P, Thakur M L, Wickstrom Eric
Department of Biochemistry and Molecular Pharmacology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA.
Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):409-14. doi: 10.1081/ncn-200061865.
A chelator-peptide-PNA-peptide chimera specific for KRAS has been prepared by continuous solid phase coupling with a C-terminal insulin-like growth factor 1 (IGF1) ligand, D(cys-ser-lys-cys), and N-terminal bis(S-benzoyl thioglycoloyl) diaminopropanoate chelator for radionuclide labeling. The probe was purified by RP-HPLC and characterized by MALDI-TOF mass spectroscopy. The probe was labeled with 99mTc and 64Cu. Both labeled probes accumulated in human pancreatic cancer xenografts in immunocompromised mice. Control experiments with mismatch chimeras and control xenografts will be necessary to determine the specificity of this molecular diagnostic strategy.
一种针对KRAS的螯合剂-肽-PNA-肽嵌合体已通过与C端胰岛素样生长因子1（IGF1）配体D（cys-ser-lys-cys）以及用于放射性核素标记的N端双（S-苯甲酰硫代乙醇酰）二氨基丙酸酯螯合剂进行连续固相偶联而制备。该探针通过反相高效液相色谱（RP-HPLC）纯化，并通过基质辅助激光解吸电离飞行时间质谱（MALDI-TOF）进行表征。该探针用99mTc和64Cu进行标记。两种标记探针均在免疫缺陷小鼠的人胰腺癌异种移植瘤中聚集。需要用错配嵌合体和对照异种移植瘤进行对照实验，以确定这种分子诊断策略的特异性。
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