Imatinib can act as an allosteric activator of Abl kinase.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2021.167349
Abstract: Imatinib is an ATP-competitive inhibitor of Bcr-Abl kinase and the first drug approved for chronic myelogenous leukemia (CML) treatment. Here we show that imatinib binds to a secondary, allosteric site located in the myristoyl pocket… read more here.
Keywords: allosteric pocket; kinase; imatinib; abl kinase ... See more keywords
Characterization of an Allosteric Pocket in Zika Virus NS2B-NS3 Protease
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DOI: 10.1021/acs.jcim.1c01326
Abstract: The NS2B-NS3 protease from Zika virus (ZIKV NS2B-NS3pro) cleaves the viral polyprotein, being essential for its replication and a therapeutic target. Inhibitors that target the active site of ZIKV NS2B-NS3pro have been developed, but they… read more here.
Keywords: protease; ns2b ns3pro; allosteric pocket; zikv ns2b ... See more keywords
Identification of the molecular determinants of antagonist potency in the allosteric binding pocket of human P2X4
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1101023
Abstract: P2X receptors are a family of ATP-gated cation channels comprising seven subtypes in mammals, which play key roles in nerve transmission, pain sensation and inflammation. The P2X4 receptor in particular has attracted significant interest from… read more here.
Keywords: bx430; allosteric pocket; pocket; human p2x4 ... See more keywords