Electrophilic fragment–based drug design leads to new monocyclic, bicyclic, and tricyclic reversible covalent compounds with strong anti-inflammatory and cytoprotective properties
Recently, reversible covalent drugs have been gaining attention because of their unique features. Reversible covalent drugs have high potency, high ligand efficiency and long duration of action thereby exhibiting the advantages yet circumvent the disadvantages of irreversible covalent drugs. Nevertheless, reversible covalent drugs have been largely ignored because of a lack of reactive compounds to produce reversible covalent adducts with protein targets.
Dr. Tadashi Honda, Research Professor in the Department of Chemistry and Director of the Anti-Inflammatory Research Laboratory in the Institute of Chemical Biology and Drug Discover at Stony Brook University, and collaborators at the University of Dundee have developed novel monocyclic, bicyclic, and tricyclic compounds containing an electrophilic moiety, which exhibit strong anti-inflammatory and cytoprotective properties. These novel compounds are potent activators of the Keap1/Nrf2/AREpathway and act to inhibit iNOS in vivo and in vitro. These novel compounds can be further developed as cancer therapeutics and for the treatment of inflammation based diseases.
Covalent yet reversible binding to protein target.
Easy synthesis with few steps.
Cancer. Inflammatory Disease.
In vitro data
We seek to develop and commercialize, by an exclusive license agreement and/or sponsored research, with a company active in the area
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Fragment-based drug discovery, Acetylenic cyanoenones, Reversible covalent drugs, Therapeutics, Inflammation, Carcinogenesis