Chen Po-Han, Chen Xiaoyan, He Xiaolin
Department of Molecular Pharmacology and Biological Chemistry, Northwestern University Feinberg School of Medicine, Searle 8-417, 303 East Chicago Avenue, Chicago, IL 60611, USA.
Biochim Biophys Acta. 2013 Oct;1834(10):2176-86. doi: 10.1016/j.bbapap.2012.10.015. Epub 2012 Nov 5.
The four types of platelet-derived growth factors (PDGFs) and the two types of PDGF receptors (PDGFRs, which belong to class III receptor tyrosine kinases) have important functions in the development of connective tissue cells. Recent structural studies have revealed novel mechanisms of PDGFs in propeptide loading and receptor recognition/activation. The detailed structural understanding of PDGF-PDGFR signaling has provided a template that can aid therapeutic intervention to counteract the aberrant signaling of this normally silent pathway, especially in proliferative diseases such as cancer. This review summarizes the advances in the PDGF system with a focus on relating the structural and functional understandings, and discusses the basic aspects of PDGFs and PDGFRs, the mechanisms of activation, and the insights into the therapeutic antagonism of PDGFRs. This article is part of a Special Issue entitled: Emerging recognition and activation mechanisms of receptor tyrosine kinases.
四种血小板衍生生长因子（PDGFs）和两种PDGF受体（PDGFRs，属于III类受体酪氨酸激酶）在结缔组织细胞的发育中具有重要功能。最近的结构研究揭示了PDGFs在前肽装载以及受体识别/激活方面的新机制。对PDGF-PDGFR信号传导的详细结构理解提供了一个模板，有助于进行治疗干预，以对抗这条通常沉默的通路的异常信号传导，尤其是在诸如癌症等增殖性疾病中。本综述总结了PDGF系统的进展，重点是将结构和功能的理解联系起来，并讨论了PDGFs和PDGFRs的基本方面、激活机制以及对PDGFRs治疗性拮抗作用的见解。本文是名为：受体酪氨酸激酶新的识别和激活机制的特刊的一部分。
