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配体对受体占有率的定量分析——一类研究不足的潜在生物标志物

Quantification of Receptor Occupancy by Ligand-An Understudied Class of Potential Biomarkers.

作者信息

Veeramani Suresh, Weiner George J

机构信息

Holden Comprehensive Cancer Center, University of Iowa, Iowa City, IA 52241, USA.

Department of Internal Medicine, University of Iowa, Iowa City, IA 52241, USA.

出版信息

Cancers (Basel). 2020 Oct 13;12(10):2956. doi: 10.3390/cancers12102956.

DOI:10.3390/cancers12102956
PMID:33066142
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7601969/
Abstract

Molecular complexes, such as ligand-receptor complexes, are vital for both health and disease and can be shed into the circulation in soluble form. Relatively little is known about the biology of soluble ligand-receptor complexes. The functional importance of such complexes and their potential use as clinical biomarkers in diagnosis and therapy remains underappreciated. Most traditional technologies used to study ligand-receptor complexes measure the individual levels of soluble ligands or receptors rather than the complexes themselves. The fraction of receptors occupied by ligand, and the potential clinical relevance of such information, has been largely overlooked. Here, we review the biological significance of soluble ligand-receptor complexes with a specific focus on their potential as biomarkers of cancer and other inflammatory diseases. In addition, we discuss a novel RNA aptamer-based technology, designated ligand-receptor complex-binding aptamers (LIRECAP), that can provide precise measurement of the fraction of a soluble receptor occupied by its ligand. The potential applicability of the LIRECAP technology as a biomarker discovery platform is also described.

摘要

分子复合物,如配体-受体复合物,对健康和疾病都至关重要,并且可以以可溶性形式释放到循环系统中。人们对可溶性配体-受体复合物的生物学特性了解相对较少。这类复合物的功能重要性及其作为临床生物标志物在诊断和治疗中的潜在用途仍未得到充分认识。大多数用于研究配体-受体复合物的传统技术测量的是可溶性配体或受体的个体水平,而非复合物本身。配体占据受体的比例以及此类信息的潜在临床相关性在很大程度上被忽视了。在此,我们综述可溶性配体-受体复合物的生物学意义,特别关注其作为癌症和其他炎症性疾病生物标志物的潜力。此外,我们还讨论了一种基于新型RNA适配体的技术,称为配体-受体复合物结合适配体(LIRECAP),它可以精确测量可溶性受体被其配体占据的比例。还描述了LIRECAP技术作为生物标志物发现平台的潜在适用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/af5216e96df4/cancers-12-02956-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/9edfe32141fe/cancers-12-02956-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/95911777d195/cancers-12-02956-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/af5216e96df4/cancers-12-02956-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/9edfe32141fe/cancers-12-02956-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/95911777d195/cancers-12-02956-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d761/7601969/af5216e96df4/cancers-12-02956-g003.jpg

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本文引用的文献

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