作者: T.K. Sawyer
DOI: 10.1016/B0-08-045044-X/00070-5
关键词:
摘要: Protein phosphorylation has become a central focus of drug discovery as the result identification and validation promising therapeutic targets such protein kinases, phosphatases, phosphoprotein binding domains.1–24 With respect to targets, significant progress been made in mapping signal transduction pathways involved disease, including particular molecular genesis and/or sustainment various cancers, several inflammatory, immune, metabolic, bone diseases. is an extraordinarily important component life processes, underlying cellular proliferation, differentiation, metabolism, survival, motility, gene transcription. complex phenomenon, with triggering, compensatory mechanisms, both spatial temporal factors contributing biological specificity functional endpoints within milieu. The global state proteins cells fundamentally impossible decipher at high resolution, even though sophisticated methods (e.g., mass spectrometry, interaction traps, affinity chromatography) are emerging that can be used analyze so-called phosphoproteome. In this chapter, described relative our current understanding biology kinase, phosphatase, phosphoprotein-interacting domain containing intracellular proteins. addition few noteworthy examples focused on developing small-molecule inhibitors described.