Enzymes

Enzymes catalyze nearly all of the chemical reactions that occur in biological systems. Enzymes are generally proteins but also include catalytic DNA and catalytic RNA. As effective biological catalysts, enzymes work by lowering a reaction’s activation energy barrier, thereby increasing the rate of the reaction. They also improve the specificity of the reactions.

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  • News and Views |

    The limited availability of small-molecule ligands for E3 ubiquitin ligases stymies the development of next-generation degraders. Two recent papers report the identification of novel, covalent and PROTAC-compatible ligands that hijack the previously untargeted ligases RNF114 and DCAF16.

    • Matthias Brand
    •  & Georg E. Winter
  • Research Highlights |

    Smith et al. report the design of ripretinib, an investigational tyrosine kinase inhibitor that forces the activation loop of KIT and PDGFRα into an inactive conformation and targets a broad spectrum of KIT and PDGFRα mutants in GIST.

    • M. Teresa Villanueva
  • News and Views |

    A synthetic DNA enzyme catalyses the formation of a native phosphodiester bond between two RNA fragments, but the molecular details of the mechanism remained elusive. Research using computational and biochemical approaches now suggests that the DNA enzyme recruits two magnesium ions to assist in the catalysis of RNA ligation.

    • Claudia Höbartner
    Nature Catalysis 2, 483-484