1. Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021
Yihui Song, Huiqing Zhang, Xiaoke Yang, Yuting Shi, Bin Yu Eur J Med Chem. 2022 Jan 15;228:114042. doi: 10.1016/j.ejmech.2021.114042. Epub 2021 Dec 6.
Lysine-specific demethylase 1 (LSD1/KDM1A) has emerged as a promising epigenetic target for disease treatment. Several LSD1 inhibitors have advanced into clinical trials. Following our last annual review on LSD1 inhibitors in 2020 (Eur. J. Med. Chem. 2021, 214, 113254), in this review we aim to update LSD1 inhibitors including natural products, synthetic compounds and cyclic peptides reported during 2021. Design strategies, structure-activity relationships, binding model analysis and modes of action are highlighted. In particular, two FDA-approved antihypertensive drugs raloxifene and fenoldopam were repurposed as reversible LSD1 inhibitors. The clinical candidate TAK-418 for treating neurodevelopmental disorders and PET imaging agent [18F]30 for LSD1 were identified. Moreover, dual inhibitors targeting both LSD1 and HDAC6 or tubulin displayed enhanced anti-cancer effects than single agents. These compounds further enrich the structural types of LSD1 inhibitors.
3. Cyclopeptide scaffolds in carbohydrate-based synthetic vaccines
Carlo Pifferi, Nathalie Berthet, Olivier Renaudet Biomater Sci. 2017 May 2;5(5):953-965. doi: 10.1039/c7bm00072c.
Cyclopeptides have been recently used successfully as carriers for the multivalent presentation of carbohydrate and peptide antigens in immunotherapy. Beside their synthetic versatility, these scaffolds are indeed interesting due to their stability against enzyme degradation and low immunogenicity. This mini-review highlights the recent advances in the utilization of cyclopeptides to prepare fully synthetic vaccines prototypes against cancers and pathogens.
