Design, synthesis, and biological evaluation of 4-(5-dimethylamino-naphthalene-1-sulfon-amido)-3-(4-iodophenyl)butanoic acid as a novel molecular probe for apoptosis imaging.
Design, synthesis, and biological evaluation of 4-(5-dimethylamino-naphthalene-1-sulfon-amido)-3-(4-iodophenyl)butanoic acid as a novel molecular probe for apoptosis imaging.
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DOI：
10.1016/j.bbrc.2010.06.120
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发表时间：
2010-07
影响因子：
3.1
通讯作者：
Wenbin Zeng;W. Miao;M. Le Puil;Guang-Qing Shi;J. Biggerstaff;G. Kabalka;D. Townsend
中科院分区：
文献类型：
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作者：
Wenbin Zeng;W. Miao;M. Le Puil;Guang-Qing Shi;J. Biggerstaff;G. Kabalka;D. Townsend
细胞凋亡（程序性细胞死亡）在许多疾病的发病机制中起着至关重要的作用，因此凋亡细胞的检测可以为医生提供进一步治疗策略的重要信息，并将大大促进患者的护理。设计并合成了一种新的凋亡探针分子4-（5-二甲氨基萘-1-磺酰胺基）-3-（4-碘苯基）丁酸（DNSBA）。生物学特性表明，DNSBA可用于特异性和选择性地检测所有阶段的凋亡癌细胞。当用放射性碘（I-123、-124和-131）标记时，DNSBA也被设计为潜在的SPECT和PET探针。
Apoptosis (programmed cell death) plays a crucial role in the pathogenesis of many disorders, thus the detection of apoptotic cells can provide the physician with important information to further therapeutic strategies and would substantially advance patient care. A small molecule, 4-(5-dimethylamino-naphthalene-1-sulfonamido)-3-(4-iodo-phenyl)butanoic acid (DNSBA), was designed as a novel probe for imaging apoptosis and synthesized with good yield. The biological characterization demonstrated that DNSBA can be used to specifically and selectively detect apoptotic cancer cells at all stages. DNSBA is also designed as a potential SPECT and PET probe when labeled with radioiodine (I-123, -124, and -131).