Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors

Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors

A series of analogues of Amb639752, a novel diacylglycerol kinase (DGK) inhibitor recently discovered by us via virtual screening, have been tested. The compounds were evaluated as DGK inhibitors on α, θ, and ζ isoforms, and as antagonists on serotonin receptors. From these assays emerged two novel...

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Bibliographic Details
Main Authors: Suresh Velnati, Alberto Massarotti, Annamaria Antona, Maria Talmon, Luigia Grazia Fresu, Alessandra Silvia Galetto, Daniela Capello, Alessandra Bertoni, Valentina Mercalli, Andrea Graziani, Gian Cesare Tron, Gianluca Baldanzi
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
diacylglycerol kinase
kinase inhibitors
structure–activity relationship
enzyme assays
molecular modelling
Online Access:http://dx.doi.org/10.1080/14756366.2019.1684911

Internet

http://dx.doi.org/10.1080/14756366.2019.1684911

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