Work

The current toolbox for APOBEC drug discovery

Year: 2022

Type: review

Abstract: Mutational processes driving genome evolution and heterogeneity contribute to immune evasion and therapy resistance in viral infections and cancer. APOBEC3 (A3) enzymes promote such mutations by catalyzing the deamination of cytosines to uracils in single-stranded DNA. Chemical inhibition of A3 enzymes may yield an antimutation therapeutic strategy to improve the durability of current drug therapies that are prone to resistance mutations. A3 small-molecule drug discovery efforts to date have been restricted to a single high-throughput biochemical activity assay; however, the arsenal of discovery assays has significantly expanded in recent years. The assays used to study A3 enzymes are reviewed here with an eye towards their potential for small-molecule discovery efforts.

Source: Trends in Pharmacological Sciences

DOI: 10.1016/j.tips.2022.02.007

Authors: Michael J. Grillo, Katherine F.M. Jones, Michael A. Carpenter, Reuben S. Harris, Daniel A. Harki

Institutions: University of Minnesota, Howard Hughes Medical Institute

Language: English

Topic: HIV/AIDS drug development and treatment

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $6,700