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Preparation and evaluation of 99m Tc-HYNIC-D (TPPE) as a new targeted imaging probe for detection of colon cancer: Preclinical comparison with 99m Tc-HYNIC-EPPT.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-05-19 , DOI: 10.1111/cbdd.13707 Fariba Maleki 1, 2 , Arezou Masteri Farahani 1, 2 , Nourollah Sadeghzadeh 1 , Alireza Mardanshahi 3 , Saeid Abediankenari 4
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-05-19 , DOI: 10.1111/cbdd.13707 Fariba Maleki 1, 2 , Arezou Masteri Farahani 1, 2 , Nourollah Sadeghzadeh 1 , Alireza Mardanshahi 3 , Saeid Abediankenari 4
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The aim of this study was to prepare radiolabeled peptide‐based agents for imaging of colon cancer. According to the incorporation of HYNIC for radiolabeling with technetium‐99m, two analogs were designed and compared: an antitumor‐antibody‐derived peptide based on the EPPT sequence and a novel retro‐inverso peptidomimetic derivative D(TPPE) structurally modified by replacing the L‐amino acids with D‐amino acids and reversing the primary amino acid sequence of EPPT. The HYNIC‐conjugated peptides were labeled with 99mTc using tricine/EDDA coligand with more than 98% radiochemical yield and showed high metabolic stability. Kd values of 41.77 ± 7.34 nM and 37.33 ± 8.37 nM for 99mTc‐HYNIC‐EPPT and 99mTc‐HYNIC‐D(TPPE) confirmed high affinity of both peptides for cell surface antigen MUC1. These radiotracers demonstrated no significant differences in the cellular uptake and internalization value, but the biodistribution profile of 99mTc‐HYNIC‐D(TPPE) was more favorable than that of 99mTc‐HYNIC‐EPPT as a result of better tumor‐to‐non‐target ratios for the examined tissues and organs. HT29 tumors were visualized more clearly in scintigraphic images with 99mTc‐HYNIC‐D(TPPE) in comparison with 99mTc‐HYNIC‐EPPT. The results showed the retro‐inverso analog to be a more promising radiotracer as a probe for in vivo targeting of HT‐29 tumors than the parent peptide.
中文翻译：
99m Tc-HYNIC-D（TPPE）作为结肠癌检测新靶向成像探针的制备与评价：与99m Tc-HYNIC-EPT的临床前比较。
本研究的目的是制备用于结肠癌成像的放射性标记肽基试剂。根据 HYNIC 与锝-99m 放射性标记的结合，设计并比较了两种类似物：一种基于 EPPT 序列的抗肿瘤抗体衍生肽和一种通过取代 L 进行结构修饰的新型逆反肽模拟衍生物D (TPPE) -氨基酸与 D-氨基酸并反转 EPPT 的一级氨基酸序列。使用 tricine/EDDA 共配体以99m Tc标记 HYNIC 缀合的肽，放射化学产率超过 98%，并显示出高代谢稳定性。的41.77±7.34ÑKd值中号和37.33±8.37Ñ中号为99米的Tc-HYNIC-EPPT和99m Tc-HYNIC- D (TPPE) 证实了两种肽对细胞表面抗原 MUC1 的高亲和力。这些放射性示踪剂证明在细胞摄取和内化值没有显著差异，但的生物分布轮廓99米的Tc-HYNIC- d（TPPE）比的更有利的99米的Tc-HYNIC-EPPT更好肿瘤-非的结果-检查的组织和器官的目标比率。HT29肿瘤与闪烁照相图像更加清楚地显现99米的Tc-HYNIC- d与比较（TPPE）99米Tc-HYNIC-EPT。结果表明，与母体肽相比，逆反类似物作为体内靶向 HT-29 肿瘤的探针是更有前景的放射性示踪剂。
更新日期：2020-05-19
中文翻译：
99m Tc-HYNIC-D（TPPE）作为结肠癌检测新靶向成像探针的制备与评价：与99m Tc-HYNIC-EPT的临床前比较。
本研究的目的是制备用于结肠癌成像的放射性标记肽基试剂。根据 HYNIC 与锝-99m 放射性标记的结合，设计并比较了两种类似物：一种基于 EPPT 序列的抗肿瘤抗体衍生肽和一种通过取代 L 进行结构修饰的新型逆反肽模拟衍生物D (TPPE) -氨基酸与 D-氨基酸并反转 EPPT 的一级氨基酸序列。使用 tricine/EDDA 共配体以99m Tc标记 HYNIC 缀合的肽，放射化学产率超过 98%，并显示出高代谢稳定性。的41.77±7.34ÑKd值中号和37.33±8.37Ñ中号为99米的Tc-HYNIC-EPPT和99m Tc-HYNIC- D (TPPE) 证实了两种肽对细胞表面抗原 MUC1 的高亲和力。这些放射性示踪剂证明在细胞摄取和内化值没有显著差异，但的生物分布轮廓99米的Tc-HYNIC- d（TPPE）比的更有利的99米的Tc-HYNIC-EPPT更好肿瘤-非的结果-检查的组织和器官的目标比率。HT29肿瘤与闪烁照相图像更加清楚地显现99米的Tc-HYNIC- d与比较（TPPE）99米Tc-HYNIC-EPT。结果表明，与母体肽相比，逆反类似物作为体内靶向 HT-29 肿瘤的探针是更有前景的放射性示踪剂。
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