TLDR The review suggests that while many AKR1C3 inhibitors show promise for treating certain cancers, more research is needed to confirm their effectiveness in humans.
The review discussed the potential of Aldo-Keto Reductase (AKR) 1C3 inhibitors in treating various malignancies, including castration-resistant prostate cancer (CRPC), breast cancer, and acute myeloid leukemia (AML). It highlighted different classes of inhibitors, such as N-phenylsulfonylindoles and repurposed NSAIDs, and their mechanisms of action. Despite promising preclinical results, clinical trials like ASP9521 faced challenges such as lack of efficacy and drug resistance. The review emphasized the need for further optimization and suggested that precision medicine and combination therapies might be necessary to enhance the effectiveness of AKR1C3 inhibitors.
45 citations,
May 2012 in “The Journal of Steroid Biochemistry and Molecular Biology” Too much AKR1C3 enzyme causes resistance to finasteride by increasing testosterone.
45 citations,
May 2012 in “The Journal of Steroid Biochemistry and Molecular Biology” Too much AKR1C3 enzyme causes resistance to finasteride by increasing testosterone.
6 citations,
October 2014 in “Experimental Dermatology” Prostaglandins and the enzyme AKR1C3 could play a role in skin cancer and hair loss, and further research is needed to understand these mechanisms.
402 citations,
August 2011 in “Cancer research” Prostate cancer cells can make their own androgens to activate the androgen receptor, and treatments like abiraterone may increase this ability, suggesting new therapies should target the entire steroid-making pathway.
December 2022 in “International Journal of Molecular Sciences” Afatinib, neratinib, and zanubrutinib could be effective against KRASG12C-mutant tumors.
131 citations,
September 2017 in “Molecular and Cellular Endocrinology” The document concludes that blocking the internal pathways that create androgens might help treat cancers that depend on sex hormones.
