Synthesis and preliminary evaluation of a novel 125I-labeled T140 analog for quantitation of CXCR4 expression

被引：0

作者：

Yanjiang Han

Duanzhi Yin

Mingqiang Zheng

Wei Zhou

ZhenHong Lee

Lan Zhan

Yufei Ma

Mingxing Wu

Lingli Shi

Ni Wang

Jianbo Lee

Cheng Wang

Zheng Lee

Yongxian Wang

机构：

[1] Chinese Academy of Sciences,Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics

[2] Chinese Academy of Sciences,Graduate School

[3] Case Western Reserve University,Department of Nuclear Medicine/Radiology, University Hospitals Case Medical Center

来源：

Journal of Radioanalytical and Nuclear Chemistry | 2010年 / 284卷

关键词：

CXCR4; SDF-1; SIB; Radioiodination;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

The aim of this study was to develop a radiopharmaceutical for the imaging of CXCR4-expressing tumors in vivo. For 125I-labeling, 125I-SIB was synthesized and conjugated with the ε-NH2 group of Ac-TZ14011, a specific CXCR4 antagonist. The specific radioactivity of the product was 5 GBq/μmol and the radiochemical purity (RCP) was 96% (n = 3). After 6 h, the RCP of the product in PBS was 93%. The MCF-7 cell uptake of Ac-TZ14011 was rapid and high. Primary biodistribution studies indicated that 125I-IB-Ac-TZ14011 was mainly excreted via the kidney, and further evaluation in mice with induced tumors was necessary.

引用

页码：279 / 286

页数：7

共 50 条

[31] T140体内靶向阻断SDF-1/CXCR4信号通路对SDF-1及MMPs的影响
王坤
赵沣凯
李彦林
余洋
高寰宇
肖渝
李龙滕
闫祥甲
贾迪
实用医学杂志, 2015, 31 (19) : 3133 - 3136
[32] Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140
Tamamura, H
Omagari, A
Hiramatsu, K
Gotoh, K
Kanamoto, T
Xu, YN
Kodama, E
Matsuoka, M
Hattori, T
Yamamoto, N
Nakashima, H
Otaka, A
Fujii, N
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (14) : 1897 - 1902
[33] Synthesis and evaluation of 125I-labeled tetrazine prosthetic group for an efficient bioorthogonal radiolabeling of trans-cyclooctene containing biomolecules
Mushtaq, S.
Choi, M.
Shim, H.
Yun, S.
Lee, C.
Park, S.
Choi, D.
Jang, B.
Jeon, J.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 : S553 - S553
[34] T140体外阻断SDF-1/CXCR4信号通路阻止人关节软骨Ⅱ型胶原蛋白降解的研究
马珂
李晓林
李彦林
朱晓松
赵沣凯
实用医学杂志, 2014, 30 (12) : 1879 - 1882
[35] Targeting of chemokine receptor CXCR4: In vitro and in vivo evaluation of 125/123I-CPD-01011
Hu, Meiduo
Darwish, Alla
Wu, T.
Moran, Matthew
Simms, Ryan
Forbes, John
Stephenson, Karin
Valliant, John
JOURNAL OF NUCLEAR MEDICINE, 2014, 55
[36] Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity
Tamamura, H
Sugioka, M
Odagaki, Y
Omagari, A
Kan, Y
Oishi, S
Nakashima, H
Yamamoto, N
Peiper, SC
Hamanaka, N
Otaka, A
Fujii, N
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (03) : 359 - 362
[37] Synthesis and in vitro evaluation of 68Ga-DOTA-4-FBn-TN14003, a novel tracer for the imaging of CXCR4 expression
Hennrich, Ute
Seyler, Lisa
Schaefer, Martin
Bauder-Wuest, Ulrike
Eisenhut, Michael
Semmler, Wolfhard
Baeuerle, Tobias
BIOORGANIC & MEDICINAL CHEMISTRY, 2012, 20 (04) : 1502 - 1510
[38] Synthesis of a novel tripeptidomimetic scaffold and biological evaluation for CXC chemokine receptor 4 (CXCR4) antagonism
Baumann, Markus
Nome, Lina Marie
Zachariassen, Zack G.
Karlshoj, Stefanie
Fossen, Torgils
Rosenkilde, Mette M.
Vabeno, Jon
Haug, Bengt Erilc
TETRAHEDRON, 2017, 73 (27-28) : 3866 - 3877
[39] T140阻断SDF-1/CXCR4信号通路并在骨关节炎疾病模型中防止软骨退化
陈鹏
颜林淋
李杨
何润泽
刘峰
基因组学与应用生物学, 2020, 39 (04) : 1808 - 1813
[40] A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C axe weak partial agonists
Zhang, WB
Navenot, JM
Haribabu, B
Tamamura, H
Hiramatu, K
Omagari, A
Pei, G
Manfredi, JP
Fujii, N
Broach, JR
Peiper, SC
JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (27) : 24515 - 24521

← 1 2 3 4 5 →