Serveur sur les données et bibliothèques médicales au Maghreb (version finale)

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<title xml:lang="en">NU-6027 Inhibits Growth of
<named-content content-type="genus-species">Mycobacterium tuberculosis</named-content>
by Targeting Protein Kinase D and Protein Kinase G</title>
<author>
<name sortKey="Kidwai, Saqib" sort="Kidwai, Saqib" uniqKey="Kidwai S" first="Saqib" last="Kidwai">Saqib Kidwai</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Bouzeyen, Rania" sort="Bouzeyen, Rania" uniqKey="Bouzeyen R" first="Rania" last="Bouzeyen">Rania Bouzeyen</name>
<affiliation>
<nlm:aff id="aff2">
<addr-line>Institut Pasteur de Tunis, LTCII, LR11 IPT02, Université Tunis El Manar, Tunis, Tunisia</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Chakraborti, Sohini" sort="Chakraborti, Sohini" uniqKey="Chakraborti S" first="Sohini" last="Chakraborti">Sohini Chakraborti</name>
<affiliation>
<nlm:aff id="aff3">
<addr-line>Molecular Biophysics Unit, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Khare, Neha" sort="Khare, Neha" uniqKey="Khare N" first="Neha" last="Khare">Neha Khare</name>
<affiliation>
<nlm:aff id="aff4">
<addr-line>Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Das, Sumana" sort="Das, Sumana" uniqKey="Das S" first="Sumana" last="Das">Sumana Das</name>
<affiliation>
<nlm:aff id="aff5">
<addr-line>Department of Molecular Reproduction, Development and Genetics, Biological Sciences Building, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Priya Gosain, Tannu" sort="Priya Gosain, Tannu" uniqKey="Priya Gosain T" first="Tannu" last="Priya Gosain">Tannu Priya Gosain</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Behura, Assirbad" sort="Behura, Assirbad" uniqKey="Behura A" first="Assirbad" last="Behura">Assirbad Behura</name>
<affiliation>
<nlm:aff id="aff6">
<addr-line>Laboratory of Mycobacterial Immunology, Department of Life Science, National Institute of Technology, Rourkela, Odisha, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Meena, Chhuttan Lal" sort="Meena, Chhuttan Lal" uniqKey="Meena C" first="Chhuttan Lal" last="Meena">Chhuttan Lal Meena</name>
<affiliation>
<nlm:aff id="aff7">
<addr-line>Drug Discovery Research Centre, Translational Health Science and Technology Institute, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Dhiman, Rohan" sort="Dhiman, Rohan" uniqKey="Dhiman R" first="Rohan" last="Dhiman">Rohan Dhiman</name>
<affiliation>
<nlm:aff id="aff6">
<addr-line>Laboratory of Mycobacterial Immunology, Department of Life Science, National Institute of Technology, Rourkela, Odisha, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Essafi, Makram" sort="Essafi, Makram" uniqKey="Essafi M" first="Makram" last="Essafi">Makram Essafi</name>
<affiliation>
<nlm:aff id="aff2">
<addr-line>Institut Pasteur de Tunis, LTCII, LR11 IPT02, Université Tunis El Manar, Tunis, Tunisia</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Bajaj, Avinash" sort="Bajaj, Avinash" uniqKey="Bajaj A" first="Avinash" last="Bajaj">Avinash Bajaj</name>
<affiliation>
<nlm:aff id="aff4">
<addr-line>Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Saini, Deepak Kumar" sort="Saini, Deepak Kumar" uniqKey="Saini D" first="Deepak Kumar" last="Saini">Deepak Kumar Saini</name>
<affiliation>
<nlm:aff id="aff5">
<addr-line>Department of Molecular Reproduction, Development and Genetics, Biological Sciences Building, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Srinivasan, Narayanaswamy" sort="Srinivasan, Narayanaswamy" uniqKey="Srinivasan N" first="Narayanaswamy" last="Srinivasan">Narayanaswamy Srinivasan</name>
<affiliation>
<nlm:aff id="aff3">
<addr-line>Molecular Biophysics Unit, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Mahajan, Dinesh" sort="Mahajan, Dinesh" uniqKey="Mahajan D" first="Dinesh" last="Mahajan">Dinesh Mahajan</name>
<affiliation>
<nlm:aff id="aff7">
<addr-line>Drug Discovery Research Centre, Translational Health Science and Technology Institute, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Singh, Ramandeep" sort="Singh, Ramandeep" uniqKey="Singh R" first="Ramandeep" last="Singh">Ramandeep Singh</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
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<idno type="pmid">31285226</idno>
<idno type="pmc">6709498</idno>
<idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6709498</idno>
<idno type="RBID">PMC:6709498</idno>
<idno type="doi">10.1128/AAC.00996-19</idno>
<date when="2019">2019</date>
<idno type="wicri:Area/Pmc/Corpus">000131</idno>
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<analytic>
<title xml:lang="en" level="a" type="main">NU-6027 Inhibits Growth of
<named-content content-type="genus-species">Mycobacterium tuberculosis</named-content>
by Targeting Protein Kinase D and Protein Kinase G</title>
<author>
<name sortKey="Kidwai, Saqib" sort="Kidwai, Saqib" uniqKey="Kidwai S" first="Saqib" last="Kidwai">Saqib Kidwai</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Bouzeyen, Rania" sort="Bouzeyen, Rania" uniqKey="Bouzeyen R" first="Rania" last="Bouzeyen">Rania Bouzeyen</name>
<affiliation>
<nlm:aff id="aff2">
<addr-line>Institut Pasteur de Tunis, LTCII, LR11 IPT02, Université Tunis El Manar, Tunis, Tunisia</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Chakraborti, Sohini" sort="Chakraborti, Sohini" uniqKey="Chakraborti S" first="Sohini" last="Chakraborti">Sohini Chakraborti</name>
<affiliation>
<nlm:aff id="aff3">
<addr-line>Molecular Biophysics Unit, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Khare, Neha" sort="Khare, Neha" uniqKey="Khare N" first="Neha" last="Khare">Neha Khare</name>
<affiliation>
<nlm:aff id="aff4">
<addr-line>Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Das, Sumana" sort="Das, Sumana" uniqKey="Das S" first="Sumana" last="Das">Sumana Das</name>
<affiliation>
<nlm:aff id="aff5">
<addr-line>Department of Molecular Reproduction, Development and Genetics, Biological Sciences Building, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Priya Gosain, Tannu" sort="Priya Gosain, Tannu" uniqKey="Priya Gosain T" first="Tannu" last="Priya Gosain">Tannu Priya Gosain</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Behura, Assirbad" sort="Behura, Assirbad" uniqKey="Behura A" first="Assirbad" last="Behura">Assirbad Behura</name>
<affiliation>
<nlm:aff id="aff6">
<addr-line>Laboratory of Mycobacterial Immunology, Department of Life Science, National Institute of Technology, Rourkela, Odisha, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Meena, Chhuttan Lal" sort="Meena, Chhuttan Lal" uniqKey="Meena C" first="Chhuttan Lal" last="Meena">Chhuttan Lal Meena</name>
<affiliation>
<nlm:aff id="aff7">
<addr-line>Drug Discovery Research Centre, Translational Health Science and Technology Institute, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Dhiman, Rohan" sort="Dhiman, Rohan" uniqKey="Dhiman R" first="Rohan" last="Dhiman">Rohan Dhiman</name>
<affiliation>
<nlm:aff id="aff6">
<addr-line>Laboratory of Mycobacterial Immunology, Department of Life Science, National Institute of Technology, Rourkela, Odisha, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Essafi, Makram" sort="Essafi, Makram" uniqKey="Essafi M" first="Makram" last="Essafi">Makram Essafi</name>
<affiliation>
<nlm:aff id="aff2">
<addr-line>Institut Pasteur de Tunis, LTCII, LR11 IPT02, Université Tunis El Manar, Tunis, Tunisia</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Bajaj, Avinash" sort="Bajaj, Avinash" uniqKey="Bajaj A" first="Avinash" last="Bajaj">Avinash Bajaj</name>
<affiliation>
<nlm:aff id="aff4">
<addr-line>Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Saini, Deepak Kumar" sort="Saini, Deepak Kumar" uniqKey="Saini D" first="Deepak Kumar" last="Saini">Deepak Kumar Saini</name>
<affiliation>
<nlm:aff id="aff5">
<addr-line>Department of Molecular Reproduction, Development and Genetics, Biological Sciences Building, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Srinivasan, Narayanaswamy" sort="Srinivasan, Narayanaswamy" uniqKey="Srinivasan N" first="Narayanaswamy" last="Srinivasan">Narayanaswamy Srinivasan</name>
<affiliation>
<nlm:aff id="aff3">
<addr-line>Molecular Biophysics Unit, Indian Institute of Science, Bangalore, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Mahajan, Dinesh" sort="Mahajan, Dinesh" uniqKey="Mahajan D" first="Dinesh" last="Mahajan">Dinesh Mahajan</name>
<affiliation>
<nlm:aff id="aff7">
<addr-line>Drug Discovery Research Centre, Translational Health Science and Technology Institute, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
<author>
<name sortKey="Singh, Ramandeep" sort="Singh, Ramandeep" uniqKey="Singh R" first="Ramandeep" last="Singh">Ramandeep Singh</name>
<affiliation>
<nlm:aff id="aff1">
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</nlm:aff>
</affiliation>
</author>
</analytic>
<series>
<title level="j">Antimicrobial Agents and Chemotherapy</title>
<idno type="ISSN">0066-4804</idno>
<idno type="eISSN">1098-6596</idno>
<imprint>
<date when="2019">2019</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
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<textClass></textClass>
</profileDesc>
</teiHeader>
<front>
<div type="abstract" xml:lang="en">
<p>Tuberculosis (TB) is a global health concern, and this situation has further worsened due to the emergence of drug-resistant strains and the failure of BCG vaccine to impart protection. There is an imperative need to develop highly sensitive, specific diagnostic tools, novel therapeutics, and vaccines for the eradication of TB. In the present study, a chemical screen of a pharmacologically active compound library was performed to identify antimycobacterial compounds.</p>
</div>
</front>
</TEI>
<pmc article-type="research-article">
<pmc-comment>The publisher of this article does not allow downloading of the full text in XML form.</pmc-comment>
<front>
<journal-meta>
<journal-id journal-id-type="nlm-ta">Antimicrob Agents Chemother</journal-id>
<journal-id journal-id-type="iso-abbrev">Antimicrob. Agents Chemother</journal-id>
<journal-id journal-id-type="hwp">aac</journal-id>
<journal-id journal-id-type="pmc">aac</journal-id>
<journal-id journal-id-type="publisher-id">AAC</journal-id>
<journal-title-group>
<journal-title>Antimicrobial Agents and Chemotherapy</journal-title>
</journal-title-group>
<issn pub-type="ppub">0066-4804</issn>
<issn pub-type="epub">1098-6596</issn>
<publisher>
<publisher-name>American Society for Microbiology</publisher-name>
<publisher-loc>1752 N St., N.W., Washington, DC</publisher-loc>
</publisher>
</journal-meta>
<article-meta>
<article-id pub-id-type="pmid">31285226</article-id>
<article-id pub-id-type="pmc">6709498</article-id>
<article-id pub-id-type="publisher-id">00996-19</article-id>
<article-id pub-id-type="doi">10.1128/AAC.00996-19</article-id>
<article-categories>
<subj-group subj-group-type="heading">
<subject>Mechanisms of Action: Physiological Effects</subject>
</subj-group>
</article-categories>
<title-group>
<article-title>NU-6027 Inhibits Growth of
<named-content content-type="genus-species">Mycobacterium tuberculosis</named-content>
by Targeting Protein Kinase D and Protein Kinase G</article-title>
<alt-title alt-title-type="running-head">Mechanism of Action of NU-6027 against
<named-content content-type="genus-species">M. tuberculosis</named-content>
</alt-title>
<alt-title alt-title-type="short-authors">Kidwai et al.</alt-title>
</title-group>
<contrib-group>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Kidwai</surname>
<given-names>Saqib</given-names>
</name>
<xref ref-type="aff" rid="aff1">
<sup>a</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Bouzeyen</surname>
<given-names>Rania</given-names>
</name>
<xref ref-type="aff" rid="aff2">
<sup>b</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="yes">
<name>
<surname>Chakraborti</surname>
<given-names>Sohini</given-names>
</name>
<xref ref-type="aff" rid="aff3">
<sup>c</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="yes">
<name>
<surname>Khare</surname>
<given-names>Neha</given-names>
</name>
<xref ref-type="aff" rid="aff4">
<sup>d</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="yes">
<name>
<surname>Das</surname>
<given-names>Sumana</given-names>
</name>
<xref ref-type="aff" rid="aff5">
<sup>e</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Priya Gosain</surname>
<given-names>Tannu</given-names>
</name>
<xref ref-type="aff" rid="aff1">
<sup>a</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Behura</surname>
<given-names>Assirbad</given-names>
</name>
<xref ref-type="aff" rid="aff6">
<sup>f</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Meena</surname>
<given-names>Chhuttan Lal</given-names>
</name>
<xref ref-type="aff" rid="aff7">
<sup>g</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Dhiman</surname>
<given-names>Rohan</given-names>
</name>
<xref ref-type="aff" rid="aff6">
<sup>f</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Essafi</surname>
<given-names>Makram</given-names>
</name>
<xref ref-type="aff" rid="aff2">
<sup>b</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Bajaj</surname>
<given-names>Avinash</given-names>
</name>
<xref ref-type="aff" rid="aff4">
<sup>d</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Saini</surname>
<given-names>Deepak Kumar</given-names>
</name>
<xref ref-type="aff" rid="aff5">
<sup>e</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Srinivasan</surname>
<given-names>Narayanaswamy</given-names>
</name>
<xref ref-type="aff" rid="aff3">
<sup>c</sup>
</xref>
</contrib>
<contrib contrib-type="author" equal-contrib="no">
<name>
<surname>Mahajan</surname>
<given-names>Dinesh</given-names>
</name>
<xref ref-type="aff" rid="aff7">
<sup>g</sup>
</xref>
</contrib>
<contrib contrib-type="author" corresp="yes" equal-contrib="no">
<name>
<surname>Singh</surname>
<given-names>Ramandeep</given-names>
</name>
<xref ref-type="aff" rid="aff1">
<sup>a</sup>
</xref>
</contrib>
<aff id="aff1">
<label>a</label>
<addr-line>Tuberculosis Research Laboratory, Vaccine and Infectious Disease Research Centre, Translational Health Science and Technology Institute, NCR Biotech Science Cluster, Faridabad, Haryana, India</addr-line>
</aff>
<aff id="aff2">
<label>b</label>
<addr-line>Institut Pasteur de Tunis, LTCII, LR11 IPT02, Université Tunis El Manar, Tunis, Tunisia</addr-line>
</aff>
<aff id="aff3">
<label>c</label>
<addr-line>Molecular Biophysics Unit, Indian Institute of Science, Bangalore, India</addr-line>
</aff>
<aff id="aff4">
<label>d</label>
<addr-line>Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, Faridabad, Haryana, India</addr-line>
</aff>
<aff id="aff5">
<label>e</label>
<addr-line>Department of Molecular Reproduction, Development and Genetics, Biological Sciences Building, Indian Institute of Science, Bangalore, India</addr-line>
</aff>
<aff id="aff6">
<label>f</label>
<addr-line>Laboratory of Mycobacterial Immunology, Department of Life Science, National Institute of Technology, Rourkela, Odisha, India</addr-line>
</aff>
<aff id="aff7">
<label>g</label>
<addr-line>Drug Discovery Research Centre, Translational Health Science and Technology Institute, Faridabad, Haryana, India</addr-line>
</aff>
</contrib-group>
<author-notes>
<corresp id="cor1">Address correspondence to Ramandeep Singh,
<email>ramandeep@thsti.res.in</email>
.</corresp>
<fn fn-type="equal">
<p>S.C., N.K., and S.D. contributed equally to this work.</p>
</fn>
<fn fn-type="other">
<p>
<bold>Citation</bold>
Kidwai S, Bouzeyen R, Chakraborti S, Khare N, Das S, Priya Gosain T, Behura A, Meena CL, Dhiman R, Essafi M, Bajaj A, Saini DK, Srinivasan N, Mahajan D, Singh R. 2019. NU-6027 inhibits growth of
<italic>Mycobacterium tuberculosis</italic>
by targeting protein kinase D and protein kinase G. Antimicrob Agents Chemother 63:e00996-19.
<ext-link ext-link-type="uri" xlink:href="https://doi.org/10.1128/AAC.00996-19">https://doi.org/10.1128/AAC.00996-19</ext-link>
.</p>
</fn>
</author-notes>
<pub-date pub-type="epreprint">
<day>8</day>
<month>7</month>
<year>2019</year>
</pub-date>
<pub-date pub-type="epub">
<day>23</day>
<month>8</month>
<year>2019</year>
</pub-date>
<pub-date pub-type="collection">
<month>9</month>
<year>2019</year>
</pub-date>
<volume>63</volume>
<issue>9</issue>
<elocation-id>e00996-19</elocation-id>
<history>
<date date-type="received">
<day>16</day>
<month>5</month>
<year>2019</year>
</date>
<date date-type="accepted">
<day>30</day>
<month>6</month>
<year>2019</year>
</date>
</history>
<permissions>
<copyright-statement>Copyright © 2019 American Society for Microbiology.</copyright-statement>
<copyright-year>2019</copyright-year>
<copyright-holder>American Society for Microbiology</copyright-holder>
<license license-type="asm" xlink:href="https://doi.org/10.1128/ASMCopyrightv2">
<license-p>
<ext-link ext-link-type="uri" xlink:href="https://doi.org/10.1128/ASMCopyrightv2">All Rights Reserved</ext-link>
.</license-p>
</license>
</permissions>
<self-uri content-type="pdf" xlink:href="AAC.00996-19.pdf"></self-uri>
<abstract abstract-type="precis">
<p>Tuberculosis (TB) is a global health concern, and this situation has further worsened due to the emergence of drug-resistant strains and the failure of BCG vaccine to impart protection. There is an imperative need to develop highly sensitive, specific diagnostic tools, novel therapeutics, and vaccines for the eradication of TB. In the present study, a chemical screen of a pharmacologically active compound library was performed to identify antimycobacterial compounds.</p>
</abstract>
<abstract>
<title>ABSTRACT</title>
<p>Tuberculosis (TB) is a global health concern, and this situation has further worsened due to the emergence of drug-resistant strains and the failure of BCG vaccine to impart protection. There is an imperative need to develop highly sensitive, specific diagnostic tools, novel therapeutics, and vaccines for the eradication of TB. In the present study, a chemical screen of a pharmacologically active compound library was performed to identify antimycobacterial compounds. The phenotypic screen identified a few novel small-molecule inhibitors, including NU-6027, a known CDK-2 inhibitor. We demonstrate that NU-6027 inhibits
<named-content content-type="genus-species">Mycobacterium bovis</named-content>
BCG growth
<italic>in vitro</italic>
and also displayed cross-reactivity with
<named-content content-type="genus-species">Mycobacterium tuberculosis</named-content>
protein kinase D (PknD) and protein kinase G (PknG). Comparative structural and sequence analysis along with docking simulation suggest that the unique binding site stereochemistry of PknG and PknD accommodates NU-6027 more favorably than other
<named-content content-type="genus-species">M. tuberculosis</named-content>
Ser/Thr protein kinases. Further, we also show that NU-6027 treatment induces the expression of proapoptotic genes in macrophages. Finally, we demonstrate that NU-6027 inhibits
<named-content content-type="genus-species">M. tuberculosis</named-content>
growth in both macrophage and mouse tissues. Taken together, these results indicate that NU-6027 can be optimized further for the development of antimycobacterial agents.</p>
</abstract>
<kwd-group>
<title>KEYWORDS</title>
<kwd>
<italic>Mycobacterium tuberculosis</italic>
</kwd>
<kwd>NU-6027</kwd>
<kwd>serine threonine protein kinases</kwd>
<kwd>apoptosis</kwd>
</kwd-group>
<funding-group>
<award-group id="award1">
<funding-source>
<institution-wrap>
<institution>Department of Biotechnology, Ministry of Science and Technology (DBT)</institution>
</institution-wrap>
</funding-source>
<award-id>BT/IN/Indo-Tunisia/01/20</award-id>
<principal-award-recipient>
<name>
<surname>Singh</surname>
<given-names>Ramandeep</given-names>
</name>
</principal-award-recipient>
</award-group>
<award-group id="award2">
<funding-source>
<institution-wrap>
<institution>Department of Science and Technology, Ministry of Science and Technology (DST)</institution>
<institution-id>https://doi.org/10.13039/501100001409</institution-id>
</institution-wrap>
</funding-source>
<award-id>EEQ/2016/000205</award-id>
<principal-award-recipient>
<name>
<surname>Dhiman</surname>
<given-names>Rohan</given-names>
</name>
</principal-award-recipient>
</award-group>
<award-group id="award3">
<funding-source>
<institution-wrap>
<institution>Department of Science and Technology, Ministry of Science and Technology (DST)</institution>
<institution-id>https://doi.org/10.13039/501100001409</institution-id>
</institution-wrap>
</funding-source>
<award-id>EMR/2016/000048</award-id>
<principal-award-recipient>
<name>
<surname>Dhiman</surname>
<given-names>Rohan</given-names>
</name>
</principal-award-recipient>
</award-group>
</funding-group>
<counts>
<count count="1" count-type="supplementary-material"></count>
<fig-count count="7"></fig-count>
<table-count count="1"></table-count>
<equation-count count="0"></equation-count>
<ref-count count="87"></ref-count>
<page-count count="20"></page-count>
<word-count count="13249"></word-count>
</counts>
<custom-meta-group>
<custom-meta>
<meta-name>cover-date</meta-name>
<meta-value>September 2019</meta-value>
</custom-meta>
</custom-meta-group>
</article-meta>
</front>
</pmc>
</record>

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