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Can I read Rational Design and Pharmacomodulation of Protein-Binding Theranostic Radioligands for Targeting the Fibroblast Activation Protein on EtoBox?
Rational Design and Pharmacomodulation of Protein-Binding Theranostic Radioligands for Targeting the Fibroblast Activation Protein by Lingxin Meng; Jianyang Fang; Liang Zhao; Tingting Wang; Pu Yuan; Zuoquan Zhao; Rongqiang Zhuang; Qin Lin; Haojun Chen; Xiaoyuan Chen; Xianzhong Zhang; Zhide Guo is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Rational Design and Pharmacomodulation of Protein-Binding Theranostic Radioligands for Targeting the Fibroblast Activation Protein about?
The fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts (CAFs), has become a valuable target for tumor diagnosis and therapy. However, most FAP-based radioligands show insufficient tumor uptake and retention. In this study, three novel albumin-binding FAP ligands (denoted as FSDDI, FSDDI, and FSDDI) were labeled with Ga and Lu to overcome these limitations. Cell-based studies and molecular docking assays were performed to identify the specificity and protein-binding properties for FAP. Positron emission tomography (PET) scans in human hepatocellular carcinoma patient-derived xenografts (HCC-PDXs) animal models revealed longer blood retention of Ga-FSDDI than Ga-FAPI-04, Ga-FSDDI, and Ga-FSDDI. Remarkably, Ga-FSDDI had prominent tumor-to-nontarget (T/NT) ratios. The prominent tumor retention properties of Lu-FSDDI in single photon emission computed tomography (SPECT) imaging and biodistribution studies were demonstrated. In summary, this study reports a proof-of-concept study of albumin-binding radioligands for FAP-targeted imaging and targeted radionuclide therapy (TRT).
Who reads Rational Design and Pharmacomodulation of Protein-Binding Theranostic Radioligands for Targeting the Fibroblast Activation Protein?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Lingxin Meng; Jianyang Fang; Liang Zhao; Tingting Wang; Pu Yuan; Zuoquan Zhao; Rongqiang Zhuang; Qin Lin; Haojun Chen; Xiaoyuan Chen; Xianzhong Zhang; Zhide Guo
- Publisher
- American Chemical Society (ACS)
- Published
- 2022
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)