Journal
FRONTIERS IN PHARMACOLOGY
Volume 13, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2022.1046818
Keywords
indoleamine 2; 3-dioxygenase 1; tryptophan; kynurenine; IDO1 inhibitors; natural compounds
Categories
Funding
- Key Technology Research and Development Program of Shandong, China [2021CXGC010511]
- Project for development of TCM Science and Technology in Shandong Province [2019-0231, M-2022145]
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L-tryptophan metabolism is involved in the regulation of various physiological processes. Inhibiting the enzyme IDO1, which catalyzes the conversion of tryptophan, has therapeutic benefits for several diseases. Natural compounds, such as quinones, polyphenols, alkaloids, and others, have been found to have inhibitory activity against IDO1 and can be further optimized for potential use as IDO1 inhibitors.
L-tryptophan metabolism is involved in the regulation of many important physiological processes, such as, immune response, inflammation, and neuronal function. Indoleamine 2, 3-dioxygenase 1 (IDO1) is a key enzyme that catalyzes the first rate-limiting step of tryptophan conversion to kynurenine. Thus, inhibiting IDO1 may have therapeutic benefits for various diseases, such as, cancer, autoimmune disease, and depression. In the search for potent IDO1 inhibitors, natural quinones were the first reported IDO1 inhibitors with potent inhibitory activity. Subsequently, natural compounds with diverse structures have been found to have anti-IDO1 inhibitory activity. In this review, we provide a summary of these natural IDO1 inhibitors, which are classified as quinones, polyphenols, alkaloids and others. The overview of in vitro IDO1 inhibitory activity of natural compounds will help medicinal chemists to understand the mode of action and medical benefits of them. The scaffolds of these natural compounds can also be used for further optimization of potent IDO1 inhibitors.
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