Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

Posted by Adam Awdish on

Pooled Human Plasma (Blood Derived) from Innovative Research was used in the following study:

 

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

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.

 

Related products available from Innovative Research also include:

Single Donor Human Whole Blood

Single Donor Human Plasma (Blood Derived)

Pooled Human Complement Serum

 

  • Tags: Human Plasma, Pooled Human Plasma (Blood Derived)

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