Circumventing the side effects of L-asparaginase

Biomed Pharmacother. 2021 Jul:139:111616. doi: 10.1016/j.biopha.2021.111616. Epub 2021 Apr 28.

Abstract

L-asparaginase is an enzyme that catalyzes the degradation of asparagine and successfully used in the treatment of acute lymphoblastic leukemia. L-asparaginase toxicity is either related to hypersensitivity to the foreign protein or to a secondary L-glutaminase activity that causes inhibition of protein synthesis. PEGylated versions have been incorporated into the treatment protocols to reduce immunogenicity and an alternative L-asparaginase derived from Dickeya chrysanthemi is used in patients with anaphylactic reactions to the E. coli L-asparaginase. Alternative approaches commonly explore new sources of the enzyme as well as the use of protein engineering techniques to create less immunogenic, more stable variants with lower L-glutaminase activity. This article reviews the main strategies used to overcome L-asparaginase shortcomings and introduces recent tools that can be used to create therapeutic enzymes with improved features.

Keywords: Deimmunization; Epitope prediction; Half-life; Immunogenicity; L-glutaminase activity; Protein engineering.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use
  • Asparaginase / adverse effects*
  • Asparaginase / chemistry
  • Asparaginase / therapeutic use
  • Glutaminase / chemistry
  • Humans
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*
  • Protein Engineering

Substances

  • Antineoplastic Agents
  • Asparaginase
  • Glutaminase