The Synthesis and Initial Evaluation of MerTK Targeted PET Agents.
The Synthesis and Initial Evaluation of MerTK Targeted PET Agents.
复制标题
MerTK靶向PET药物的合成及初步评价
DOI：
10.3390/molecules27051460
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发表时间：
2022-02-22
期刊：
影响因子：
--
通讯作者：
Li Z
中科院分区：
文献类型：
--
作者：
Wang L;Zhou Y;Wu X;Ma X;Li B;Ding R;Stashko MA;Wu Z;Wang X;Li Z
MerTK (Mer tyrosine kinase), a receptor tyrosine kinase, is ectopically or aberrantly expressed in numerous human hematologic and solid malignancies. Although a variety of MerTK targeting therapies are being developed to enhance outcomes for patients with various cancers, the sensitivity of tumors to MerTK suppression may not be uniform due to the heterogeneity of solid tumors and different tumor stages. In this report, we develop a series of radiolabeled agents as potential MerTK PET (positron emission tomography) agents. In our initial in vivo evaluation, [18F]-MerTK-6 showed prominent uptake rate (4.79 ± 0.24%ID/g) in B16F10 tumor-bearing mice. The tumor to muscle ratio reached 1.86 and 3.09 at 0.5 and 2 h post-injection, respectively. In summary, [18F]-MerTK-6 is a promising PET agent for MerTK imaging and is worth further evaluation in future studies.
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DOI：
10.1158/1078-0432.ccr-16-1330
发表时间：
2017-03-15
期刊：
Clinical cancer research : an official journal of the American Association for Cancer Research
影响因子：
--
作者：
DeRyckere D;Lee-Sherick AB;Huey MG;Hill AA;Tyner JW;Jacobsen KM;Page LS;Kirkpatrick GG;Eryildiz F;Montgomery SA;Zhang W;Wang X;Frye SV;Earp HS;Graham DK
通讯作者：
Graham DK
影响因子：
8
作者：
Lee-Sherick, Alisa B.;Jacobsen, Kristen M.;Graham, Douglas K.
通讯作者：
Graham, Douglas K.
影响因子：
8
作者：
Linger, R. M. A.;Cohen, R. A.;Cummings, C. T.;Sather, S.;Migdall-Wilson, J.;Middleton, D. H. G.;Lu, X.;Baron, A. E.;Franklin, W. A.;Merrick, D. T.;Jedlicka, P.;DeRyckere, D.;Heasley, L. E.;Graham, D. K.
通讯作者：
Graham, D. K.
影响因子：
7.2
作者：
Lemke, Greg
通讯作者：
Lemke, Greg
影响因子：
7.3
作者：
Zhao, Jichen;Zhang, Dehui;Wang, Xiaodong
通讯作者：
Wang, Xiaodong