Macrocyclic Peptides Uncover a Novel Binding Mode for Reversible Inhibitors of LSD1

[Image: see text] Lysine-specific demethylase 1 (LSD1) is an epigenetic enzyme which regulates the methylation of Lys4 of histone 3 (H3) and is overexpressed in certain cancers. We used structures of H3 substrate analogues bound to LSD1 to design macrocyclic peptide inhibitors of LSD1. A linear, Lys...

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Publicado en:ACS Omega
Main Authors: Yang, Jie, Talibov, Vladimir O., Peintner, Stefan, Rhee, Claire, Poongavanam, Vasanthanathan, Geitmann, Matthis, Sebastiano, Matteo Rossi, Simon, Bernd, Hennig, Janosch, Dobritzsch, Doreen, Danielson, U. Helena, Kihlberg, Jan
Formato: Artigo
Idioma:Inglês
Publicado: American Chemical Society 2020
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC7057333/
https://ncbi.nlm.nih.gov/pubmed/32149225
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsomega.9b03493
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