8-Azaadenosine is a potent adenosine deaminase acting on RNA1 (ADAR1) inhibitor that reduces ADAR1-mediated A-to-I editing activity and prevents self-renewal of the K562 leukemic cell line[1]. ADAR1-mediated A-to-I editing is an important pathway involved in the progression of various cancers, including thyroid cancer. 8-Azaadenosine inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells[2]. 8-Azaadenosine targets ADAR activity only and does not affect ADAR1 mRNA levels[2].
In vitro, 8-Azaadenosine (0.1-2µM; 1-6d) decreased cell viability/proliferation in a dose-dependent manner in TPC1 and Cal62 cells. 8-Azaadenosine (1, 2µM; 72h) inhibited A-to-I editing activity of both TPC1 and Cal62 cells. 8-Azaadenosine (1, 2µM; 16h) reduced 3D growth and 2D invasion and migration in TPC1 and Cal62 cells[2].
References:
[1] Zipeto MA, Court AC, Sadarangani A, et al. ADAR1 Activation Drives Leukemia Stem Cell Self-Renewal by Impairing Let-7 Biogenesis. Cell Stem Cell. 2016;19(2):177-191.
[2] Ramírez-Moya, Julia et al. “ADAR1-mediated RNA editing is a novel oncogenic process in thyroid cancer and regulates miR-200 activity.” Oncogene vol. 39,18 (2020): 3738-3753.