Ceresa Brian P
Department of Pharmacology and Toxicology, University of Louisville, Louisville, KY 40202, USA.
Int J Mol Sci. 2012 Dec 20;14(1):72-87. doi: 10.3390/ijms14010072.
Signaling by cell surface receptors appears to be relatively straight-forward: ligand binds to the extracellular domain of the receptor and biochemical changes are communicated into the cell. However, this process is more complex than it first seems due to the various mechanisms that regulate signaling. In order to effectively target these receptors for pharmacological purposes, a more complete understanding of how their signaling is regulated is needed. Here, how the endocytic pathway regulates receptor signaling is discussed, using the epidermal growth factor receptor (EGFR) as a model. In particular, the spatial regulation of signaling is examined. Areas of discussion include: how endocytic trafficking affects biology/pathology, varying approaches for studying the relationship between receptor endocytosis and signaling, and developments in how the endocytic pathway controls EGFR:effector communication and EGFR-mediated cell biology.
配体与受体的细胞外结构域结合，生化变化传递到细胞内。然而，由于调节信号传导的各种机制，这个过程比最初看起来要复杂得多。为了从药理学角度有效靶向这些受体，需要更全面地了解其信号传导是如何被调节的。在此，以表皮生长因子受体（EGFR）为模型，讨论内吞途径如何调节受体信号传导。特别地，研究了信号传导的空间调节。讨论的内容包括：内吞运输如何影响生物学/病理学、研究受体内吞作用与信号传导之间关系的不同方法，以及内吞途径控制EGFR：效应器通讯和EGFR介导的细胞生物学方面的进展。
