Novel Peptide-Based Inhibitors of Protein Kinases

摘要: Protein kinases are a class of enzymes that modulate the function and activity other proteins through phosphorylation. regulate many aspects cellular metabolism including signal transduction, transcription, translation, cell-cycle progression, biosynthesis. Owing to their profound influence over such critical processes, mutations or aberrant expression protein can have major implications on cell health viability. Indeed, dysfunctional kinase has been linked pathological conditions as neurodegeneration, inflammation, autoimmunity, cancer. Despite therapeutic importance, our ability target discrete using small-molecule-based inhibitors hindered due high degrees structural similarity among active sites. Recently, peptides emerged powerful, yet selective, modulators by virtue mimic highly specific substrate-interaction domains kinases. This chapter provides an overview development application novel peptide-based inhibitors. The goal here is highlight how various binding modes efforts enhance affinities contributed understanding complex nature kinase–substrate interactions. Furthermore, relevance explored, focusing advantages limitations molecules they applied in treatment kinase-mediated disease.