Posted by Adam Awdish on
Pooled Human Plasma (Blood Derived) from Innovative Research was used in the following study:
Satish Noonepalle, Sida Shen, Jakub Ptáček, Maurício T. Tavares, Guiping Zhang, Jan Stránský, Jiří Pavlíček, Glaucio M. Ferreira, Melissa Hadley, Guido Pelaez, Cyril Bařinka, Alan P. Kozikowski, and Alejandro Villagra
Journal of Medicinal Chemistry
August 20, 2020
Reversible acetylation of lysine side chains on protein and enzyme surfaces is modulated by histone acetyltransferases (HATs) and histone deacetylases (HDACs). Acetylation or deacetylation of protein lysine serves as a regulatory pathway for cellular transcription, cell cycles, and cellular metabolism.
HDAC6 is unique due to its ability to deacetylate a number of non-histone proteins and its preferred substrates. Selective inhibition of HDAC6 is recognized as a potential therapeutic approach for cancers, as it has been reported to interact with the transcription factor STAT3, a primary regulator of immune responses in the tumor microenvironment.
Researchers in this study designed a new HDAC6 inhibitor, named Suprastat, using in silico simulations. In vitro characterization of Suprastat demonstrated sub-nanomolar HDAC6 inhibitory potency and up to a thousand-fold HDAC6 selectivity over the other HDAC isoforms. In vivo studies showed that a combination of Suprastat and anti-PD1 immunotherapy enhances antitumor immune response, mediated by a decrease of protumoral M2 macrophages and increased infiltration of antitumor CD8+ effector and memory T-cells.
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