ISBN: 9783659106972 - docking studies of bcr-abl and c-abl by structural analogues of gnf-2: in silico analysis of myristate binding site (3 Ergebnisse)

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Taschenbuch. Zustand: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - In an attempt to search for new pharmacological approach to overcome resistance to ATP-binding-site inhibitors of Bcr-Abl, allosteric inhibitors had been discovered. The ATP-competitive inhibitors nilotinib and dasatinib, which bind to catalytically different conformation of the Abl kinase domain, had been approved for the targeting most of imatinib-resistant CML, fail to effectively suppress the Bcr-Abl activity of T351I (gatekeeper) mutation. The GNF-2, class of compound that inhibits Bcr-Abl kinase activity through an allosteric non-ATP competitive mechanism. The GNF-2 binds to myristate-binding site of Abl, leading to change in structure of ATP-binding-site. The GNF-5, an analogue of GNF-2 has appropriate pharmacokinetic properties, used in simultaneous binding of ATP-binding-inhibitors imatinib and nilotinib to obscure resistant mutation in Bcr-Abl. The aim of this work is to analyse the different structural analogues of GNF-2, which can be used as therapeutic agent to treat Chronic Myelogenous Leukemia (CML).…

Zustand: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Bhatt DrushtiPursuing M.Phil Bioinformatics from Gujarat University, Ahmedabad, India. Completed research work on cancer biology especially Chronic myelocytic leukaemia(CML) and Acute myelocytic leukaemia(AML). Presently working on t. …