孕激素受体(PR)靶向的18F标记探针的设计、合成及初步生物评价研究
Design, synthesis and preliminary bio-evaluation of progestrone receptor targeting probes for breast cancer imaging with PET
Abstract
乳腺癌是严重威胁女性健康的疾病,它的早期诊断能够有效的降低病人的死亡率。孕激素受体属于核受体超家族,有PRA和PRB两种亚型,在调节和控制卵巢,子宫和乳腺的功能方面有重要作用。研究表明,在雌激素受体阳性(ER+)的乳腺癌病人中,PR的表达与否不会对病人接受他莫西芬治疗的疗效产生影响。但是在雌激素受体表达阴性(ER-)的乳腺癌病人中,病人接受他莫西芬治疗的疗效依赖于PR的表达。因此,监测PR的表达对乳腺癌的早期诊断和ER-/PR+病人的治疗都是很重要的。PET的灵敏度高,空间分辨率好,安全性也较好,PET探针的核素用量很少,且半衰期短,在体内存在时间短,短时间内能重复使用。因此,在乳腺癌尚未出现... Early diagnosis of breast cancer, which seriously endangers the women all over the world, could effectively promote the curative effect and reduce the mortality rate. Progesterone receptor (PR) is a member of the nuclear receptor superfamily with two subtypes named PRA and PRB, and plays key roles in mediating and regulating the function of ovary, uterus and mammary gland. Many studies also showed...