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乳腺癌诊断小分子放射性探针的研究进展

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乳腺癌严重威胁女性健康，临床上对其进行精准分型是有效治疗的前提，正电子发射断层扫描(positron emission computed tomography，PET)和单光子发射计算机断层扫描(single photon emission computed tomography，SPECT)技术正在乳腺癌诊断方面发挥重要作用，而放射性探针是PET和SPECT技术的核心，对乳腺癌诊断探针的研究进行总结和分析有望对开发新型探针和用好经典探针产生启迪。基于历年来国内外发表的关于乳腺癌诊断的小分子放射性探针的文献进行总结和分析，从乳腺癌的分型和活检技术遇到的挑战为切入点，介绍了PET和SPECT技术在乳腺癌诊断方面的独到优势，总结了靶向雌激素受体、孕激素受体、人表皮生长因子受体-2 的小分子探针的发现历程和研究进展，最后提出了目前主流探针[18F]16α-氟雌二醇和[18 F]21-氟代呋喃基去甲孕酮在实际临床应用中遇到的问题和可能的解决办法，也对这些经典探针未来临床应用方面的研究方向提出了一些建议。现有乳腺癌诊断小分子放射性探针均存在脂溶性强、代谢特征不够优良的缺陷，开发新型探针以拓展核医学影像技术在乳腺癌诊断方面的应用具备重要的现实意义。
The research progress of small molecule radioactive probes for diagnosis of breast cancer
Breast cancer poses a serious threat to women′s health.Clinically,accurate classification of breast cancer is the prerequisite for effective treatment.Positron emission tomography(PET)and single photon emission computed tomography(SPECT)provide powerful tools for the diagnosis and treatment of mammary cancer.Radioactive probes are the core elements of PET and SPECT technology.Summarizing and analyzing the research progress of breast cancer diagnostic probes are expected to inspire the development of novel probes and facilitate the use of classic probes.The literatures reported the small molecule radioactive probes for diagnosis of breast cancer at home and abroad were analyzed and summarized over these years.Starting from the classification of breast cancer and the challenges encountered by biopsy technology,we first presented the PET and SPECT technology and their unique advantages in the diagnosis of breast cancer,then summarized the discovery process and research progress of small molecule radioactive probes targeting estrogen receptor,progesterone receptor and human epidermal growth factor receptor 2 in detail,and finally pointed out the problems encountered in the applications of the widely recognized probes[18 F]fluoroestradiol(FES)and[18 F]fluorofuranylnorprogesterone(FFNP)and the possible solutions.Several suggestions on the future clinical application of these classical probes were also proposed eventually.There are several intrinsic drawbacks of the existing small molecule radioactive probes for the diagnosis of breast cancer such as strong liposolubility,unsatisfactory metabolic characteristics,and high hepatointestinal background in imaging.It is of great practical significance to develop new types of probes to expand the application of nuclear medical imaging technology in the diagnosis of breast cancer.

breast cancerestrogen receptorprogesterone receptorhuman epidermal growth factor 2small molecule radioactive probe

陈雨露、陆智彭、厉廷有、邱玲、陈盼盼、林建国

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南京医科大学 药学院,江苏 南京 211166

江苏省原子医学研究所,江苏 无锡 214063

乳腺癌 雌激素受体 孕激素受体 人表皮生长因子受体-2 小分子放射性探针

南京医科大学内涵建设重点项目中国博士后科学基金南京医科大学科技发展基金江苏省高等学校大学生创新创业训练计划项目

2022M711419NMUB20210013202210312095Y

2024

沈阳药科大学学报
沈阳药科大学

沈阳药科大学学报

CSTPCD
影响因子：0.604
ISSN：1006-2858
年,卷(期)：2024.41(9)