Department of Chemistry, Louisiana State University, Baton Rouge, LA 70803, USA.
School of Basic Pharmaceutical and Toxicological Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71201, USA.
Molecules. 2021 Feb 18;26(4):1076. doi: 10.3390/molecules26041076.
Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) are two extensively studied membrane-bound receptor tyrosine kinase proteins that are frequently overexpressed in many cancers. As a result, these receptor families constitute attractive targets for imaging and therapeutic applications in the detection and treatment of cancer. This review explores the dynamic structure and structure-function relationships of these two growth factor receptors and their significance as it relates to theranostics of cancer, followed by some of the common inhibition modalities frequently employed to target EGFR and VEGFR, such as tyrosine kinase inhibitors (TKIs), antibodies, nanobodies, and peptides. A summary of the recent advances in molecular imaging techniques, including positron emission tomography (PET), single-photon emission computerized tomography (SPECT), computed tomography (CT), magnetic resonance imaging (MRI), and optical imaging (OI), and in particular, near-IR fluorescence imaging using tetrapyrrolic-based fluorophores, concludes this review.
表皮生长因子受体（EGFR）和血管内皮生长因子受体（VEGFR）是两种广泛研究的膜结合受体酪氨酸激酶蛋白，它们在许多癌症中经常过表达。因此，这些受体家族成为癌症检测和治疗中成像和治疗应用的有吸引力的靶标。本综述探讨了这两种生长因子受体的动态结构和结构-功能关系及其与癌症治疗学的关系，随后介绍了一些常用于靶向 EGFR 和 VEGFR 的常见抑制模式，如酪氨酸激酶抑制剂（TKIs）、抗体、纳米抗体和肽。本文还总结了分子成像技术的最新进展，包括正电子发射断层扫描（PET）、单光子发射计算机断层扫描（SPECT）、计算机断层扫描（CT）、磁共振成像（MRI）和光学成像（OI），特别是基于四吡咯的荧光团的近红外荧光成像。
