Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection

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dc.contributor.author Juvale, Kapil
dc.contributor.author Purushothaman, Gayathri
dc.contributor.author Singh, Vijay
dc.contributor.author Shaik, Althaf
dc.contributor.author Ravi, Srimadhavi
dc.contributor.author Thiruvenkatam, Vijay
dc.contributor.author Kirubakaran, Sivapriya
dc.date.accessioned 2019-06-18T10:49:52Z
dc.date.available 2019-06-18T10:49:52Z
dc.date.issued 2019-01
dc.identifier.citation Juvale, Kapil; Purushothaman, Gayathri; Singh, Vijay; Shaik, Althaf; Ravi, Srimadhavi; Thiruvenkatam, Vijay and Kirubakaran, Sivapriya, "Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection�, Scientific Reports, DOI: 10.1038/s41598-018-37490-x, vol. 9, no. 1, Jan. 2019. en_US
dc.identifier.uri https://doi.org/10.1038/s41598-018-37490-x
dc.identifier.uri https://repository.iitgn.ac.in/handle/123456789/4433
dc.description.abstract Helicobacter pylori�(H. pylori), the major cause of several gastric disorders has been recognied as a type I carcinogen. By virtue of resistance developed by�H. pylori�strains, currently used antibiotic based treatments rather demonstrate high failure rates. Hence, there is an emerging need for identification of new targets to treat�H. pyloriinfection. Inosine-5?-monophosphate dehydrogenase (IMPDH) has been studied as a potential target to treat�H. pylori�infection. Here, a detailed enzyme kinetic study of recombinant expressed�H. pylori�inosine-5?-monophosphate dehydrogenase (HpIMPDH) is presented. A new in-house synthesized indole-based scaffold is identified as an inhibitor for�HpIMPDH. These indole-based compounds showed non-competitive inhibition against IMP and NAD+�whereas the benzimidazole compounds were found be uncompetitive inhibitors. The new indole scaffold ensures specificity due to its high selectivity for bacterial IMPDH over human IMPDH II. Our work aims to overcome the drawback of existing inhibitors by introducing new indole scaffold for targeting bacterial IMPDH.
dc.description.statementofresponsibility by Kapil Juvale, Gayathri Purushothaman, Vijay Singh, Althaf Shaik, Srimadhavi Ravi, Vijay Thiruvenkatam and Sivapriya Kirubakaran
dc.format.extent vol. 9, no. 1
dc.language.iso en en_US
dc.publisher Nnature en_US
dc.title Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection en_US
dc.type Article en_US


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