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PDBsum entry 4az1
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References listed in PDB file
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Key reference
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Title
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Structure of the trypanosoma cruzi protein tyrosine phosphatase tcptp1, A potential therapeutic target for chagas' Disease.
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Authors
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G.T.Lountos,
J.E.Tropea,
D.S.Waugh.
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Ref.
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Mol Biochem Parasitol, 2013,
187,
1-8.
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PubMed id
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Abstract
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Chagas' disease, a neglected tropical affliction transmitted by the flagellated
protozoan Trypanosoma cruzi, is prevalent in Latin America and affects nearly 18
million people worldwide, yet few approved drugs are available to treat the
disease. Moreover, the currently available drugs exhibit severe toxicity or are
poorly effective in the chronic phase of the disease. This limitation, along
with the large population at risk, underscores the urgent need to discover new
molecular targets and novel therapeutic agents. Recently, the T. cruzi protein
tyrosine phosphatase TcPTP1 has been implicated in the cellular differentiation
and infectivity of the parasite and is therefore a promising target for the
design of novel anti-parasitic drugs. Here, we report the X-ray crystal
structure of TcPTP1 refined to a resolution of 2.18Å, which provides
structural insights into the active site environment that can be used to
initiate structure-based drug design efforts to develop specific TcPTP1
inhibitors. Potential strategies to develop such inhibitors are also discussed.
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