What is it about?
Identification of compounds that are activated by EthA and then inhibit PyrG in Mtb.
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Why is it important?
Integration of screening, molecular, biochemical, structural, chemistry and computational efforts lead to lead compounds. that inhibit PyrG and a crystal structure.
Perspectives
My contribution to this large collaborative project was the docking and identification of additional compounds to test. THis alone was important as it suggests that compounds already screened versus Mtb may be hitting this target and they may not require EthA for activation. The work was funded by the EC FP7.
Dr Sean Ekins
Collaborations in Chemistry
Read the Original
This page is a summary of: Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG, Chemistry & Biology, July 2015, Elsevier,
DOI: 10.1016/j.chembiol.2015.05.016.
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