2fum
From Proteopedia
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Catalytic domain of protein kinase PknB from Mycobacterium tuberculosis in complex with mitoxantrone
Overview
Mycobacterium tuberculosis PknB is an essential receptor-like protein, kinase involved in cell growth control. Here, we demonstrate that, mitoxantrone, an anthraquinone derivative used in cancer therapy, is a, PknB inhibitor capable of preventing mycobacterial growth. The structure, of the complex reveals that mitoxantrone partially occupies the, adenine-binding pocket in PknB, providing a framework for the design of, compounds with potential therapeutic applications. PknB crystallizes as a, 'back-to-back' homodimer identical to those observed in other structures, of PknB in complex with ATP analogs. This organization resembles that of, the RNA-dependent protein kinase PKR, suggesting a mechanism for kinase, activation in mycobacteria.
About this Structure
2FUM is a Single protein structure of sequence from Mycobacterium tuberculosis with MIX as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
The structure of PknB in complex with mitoxantrone, an ATP-competitive inhibitor, suggests a mode of protein kinase regulation in mycobacteria., Wehenkel A, Fernandez P, Bellinzoni M, Catherinot V, Barilone N, Labesse G, Jackson M, Alzari PM, FEBS Lett. 2006 May 29;580(13):3018-22. Epub 2006 Apr 27. PMID:16674948
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