Docking Studies of Bcr-Abl And c-Abl by Structural Analogues of GNF-2 (häftad)
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Format
Häftad (Paperback / softback)
Språk
Engelska
Antal sidor
96
Utgivningsdatum
2012-04-27
Förlag
LAP Lambert Academic Publishing
Medarbetare
Kalapatapu, Sairam / Jasarai, Yogesh
Illustrationer
black & white illustrations
Dimensioner
229 x 152 x 6 mm
Vikt
150 g
Antal komponenter
1
Komponenter
Paperback
ISBN
9783659106972

Docking Studies of Bcr-Abl And c-Abl by Structural Analogues of GNF-2

In silico analysis of myristate binding site

av Drushti Bhatt, Sairam Kalapatapu, Yogesh Jasarai
Häftad,  Engelska, 2012-04-27
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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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