Boronic acid-based arginase inhibitors in cancer immunotherapy |
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Institution: | 1. Division of Cardiology, Department of Medicine, Division of Cardiology, Karolinska Institutet, Stockholm, Sweden;2. Heart and Vascular Division, Karolinska University Hospital, Stockholm, Sweden |
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Abstract: | Arginase is an enzyme that converts l-arginine to l-ornithine and urea in the urea cycle. There are two isoforms of arginase in mammals: ARG-1 and ARG-2. l-Arginine level changes occur in patients with various types of affliction. An overexpression of arginase leads to the depletion of arginine and then to inhibition of the growth of T and NK cells, and in effect to the tumor escape of the immune response. Based on those observations, an inhibition of arginase is proposed as a method to improve anti-tumor immune responses (via an activation and proliferation of T and NK cells). Boronic acid derivatives as arginase inhibitors are leading, potential therapeutic agents for the treatment of several diseases. All these compounds are derived from the original 2-(S)-amino-6-boronohexanoic acid (ABH), the first boronic acid arginase inhibitor proposed by Christianson et al. This article focuses on the review of such sub-class of arginase inhibitors and highlights their SAR and PK properties. It covers molecules published until early 2020, including patent applications. |
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Keywords: | Arginase Cancer immunotherapy Boronic acids Arginase inhibitors |
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