The Synthesis and Initial Evaluation of MerTK Targeted PET Agents

Molecules

卷:27

Xinrui Ma¹  Zibo Li¹  Li Wang¹  Xuedan Wu¹  Zhanhong Wu¹  Ransheng Ding²  Bing Li²  Michael A. Stashko²  Yubai Zhou²  Xiaodong Wang² 

[1]Biomedical Research Imaging Center, Department of Radiology, and UNC Lineberger Comprehensive Cancer Center, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27514, USA

[2]|Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA

关键词: MerTK;    positron emission tomography;    fluorine-18;    radiolabeling;    cancer;   

DOI  :  10.3390/molecules27051460

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown