Docking Studies of Bcr-Abl And c-Abl by Structural Analogues of GNF-2: In silico analysis of myristate binding site - Softcover

Bhatt, Drushti; Kalapatapu, Sairam; Jasarai, Yogesh

 
9783659106972: Docking Studies of Bcr-Abl And c-Abl by Structural Analogues of GNF-2: In silico analysis of myristate binding site
Softcover
ISBN 10: 3659106976 ISBN 13: 9783659106972
Verlag: LAP LAMBERT Academic Publishing, 2012

Inhaltsangabe

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).

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Verlag
LAP LAMBERT Academic Publishing
Erscheinungsdatum
2012
Sprache
Englisch
ISBN 10 
3659106976
ISBN 13 
9783659106972
Einband
Taschenbuch
Anzahl der Seiten
96
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