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

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
Couverture souple
ISBN 10 : 3659106976 ISBN 13 : 9783659106972
Editeur : LAP LAMBERT Academic Publishing, 2012

Synopsis

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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Éditeur
LAP LAMBERT Academic Publishing
Date d'édition
2012
Langue
anglais
ISBN 10 
3659106976
ISBN 13 
9783659106972
Reliure
Broché
Nombre de pages
96
Coordonnées du fabricant
non disponible
Personne responsable
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