The protein encoded by this gene is a microsomal enzyme that catalyzes the conversion of the stress hormone cortisol to the inactive metabolite cortisone.

In addition, the encoded protein can catalyze the reverse reaction, the conversion of cortisone to cortisol.

[6] Salicylate downregulates 11β-HSD1 expression in adipose tissue in obese mice and hence may explain why aspirin improves glycemic control in type 2 diabetes.

[7] Epigallocatechin gallate from green tea can also potently inhibit this enzyme;[8] green tea is a complex mixture of various phenolics with contents varying with production and processing, and some of the phenolics are known HDAC inhibitors that alter genetic expression.

[citation needed] Emestedastat is a compound being developed as a potential treatment of Alzheimer's disease and depression that acts by inhibiting 11β-HSD1.