Ja William W, Roberts Richard W
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Trends Biochem Sci. 2005 Jun;30(6):318-24. doi: 10.1016/j.tibs.2005.04.001.
Modulators of G-protein signaling have a central role in controlling cell physiology and represent over half of all marketed prescription drugs. G-protein pathways have traditionally been targeted by developing ligands to the extracellular surface of a small subset of the estimated approximately 1000 G-protein-coupled receptors in humans. The intracellular machinery, consisting of the cytosolic receptor surfaces and heterotrimeric G proteins, provides an equivalent diversity of targets that has remained relatively unexplored until now. This review summarizes recent efforts using combinatorial peptide libraries to develop new G-protein signaling modulators targeting intracellular components.
G蛋白信号调节剂在控制细胞生理过程中起着核心作用，并且占所有已上市处方药的一半以上。传统上，G蛋白途径的靶向是通过开发配体作用于人类大约1000种G蛋白偶联受体中的一小部分的细胞外表面来实现的。由胞质受体表面和异源三聚体G蛋白组成的细胞内机制提供了同等多样的靶点，直到现在这些靶点仍相对未被探索。这篇综述总结了最近利用组合肽库开发针对细胞内成分的新型G蛋白信号调节剂的研究成果。
