Natural products as LSD1 inhibitors for cancer therapy
| Autor: | Xiaochuan Li, Chao Yang, Yuan Fang, Guochao Liao, Bin Yu, Qingchun Mu, Zhiqiang Yu |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
CD11b
integrin alpha M Cancer therapy TCP tranylcypromine HDAC histone deacetylase MMA methylmalonic acid chemistry.chemical_compound 0302 clinical medicine NAD nicotinamide adenine dinucleotide General Pharmacology Toxicology and Pharmaceutics AML acute myeloid leukemia iPS induced pluripotent stem CCC cut countercurrent chromatography ΔΨm mitochondrial transmembrane potential Histone demethylase Natural products Tm melting temperature 0303 health sciences CD86 cluster of differentiation 86 Drug discovery H3K4 histone H3 lysine 4 HRP horseradish peroxidase α-MG α-mangostin FAD flavin adenine dinucleotide mRNA messenger RNA LSD1 lysine-specific histone demethylase 1A 030220 oncology & carcinogenesis Identification (biology) CoREST RE1-silencing transcription factor co-repressor Histone Demethylases CD14 cluster of differentiation 14 EMT epithelial-mesenchymal transition MHC myosin heavy chain animal structures SIRT1 sirtuin 1 THF tetrahydrofolate SPR surface plasmon resonance Computational biology Biology SARS-CoV-2 severe acute respiratory syndrome coronavirus 2 Article Natural (archaeology) Epigenetic regulation 03 medical and health sciences Lead (geology) Epigenetics COVID-19 coronavirus disease PDX patient-derived xenograft 030304 developmental biology EVOO extra virgin olive oil NTRK2 neurotrophic receptor tyrosine kinase 2 Natural product LSD1 inhibitors lcsh:RM1-950 H3K9 histone H3 lysine 9 MAO-A monoamine oxidase A Kt competitive inhibition constant SOX2 sex determining region Y-box 2 Chemical space FDA U.S. Food and Drug Administration lcsh:Therapeutics. Pharmacology chemistry SARs structure‒activity relationship studies siRNA small interfering RNA EdU 5-ethynyl-20-deoxyuridine GGA geranylgeranoic acid |
| Zdroj: | Acta Pharmaceutica Sinica. B Acta Pharmaceutica Sinica B, Vol 11, Iss 3, Pp 621-631 (2021) Acta Pharmaceutica Sinica B |
| ISSN: | 2211-3835 |
| Popis: | Natural products generally fall into the biologically relevant chemical space and always possess novel biological activities, thus making them a rich source of lead compounds for new drug discovery. With the recent technological advances, natural product-based drug discovery is now reaching a new era. Natural products have also shown promise in epigenetic drug discovery, some of them have advanced into clinical trials or are presently being used in clinic. The histone lysine specific demethylase 1 (LSD1), an important class of histone demethylases, has fundamental roles in the development of various pathological conditions. Targeting LSD1 has been recognized as a promising therapeutic option for cancer treatment. Notably, some natural products with different chemotypes including protoberberine alkaloids, flavones, polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel scaffolds for developing new LSD1 inhibitors. In this review, we mainly discuss the identification of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor activity and their modes of action. We also briefly discuss the challenges faced in this field. We believe this review will provide a landscape of natural LSD1 inhibitors. Graphical abstract In this review, the identification of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor activity, their modes of action, and the challenges faced in this field were mainly discussed. This review will provide a landscape of natural LSD1 inhibitors.Image 1 |
| Databáze: | OpenAIRE |
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