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Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors.
Bhusal, Ram Prasad; Patel, Krunal; Kwai, Brooke X C; Swartjes, Anne; Bashiri, Ghader; Reynisson, Jóhannes; Sperry, Jonathan; Leung, Ivanhoe K H.
Afiliação
  • Bhusal RP; School of Chemical Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand . Email: j.sperry@auckland.ac.nz (JS) ; Email: i.leung@auckland.ac.nz (IKHL).
  • Patel K; School of Chemical Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand . Email: j.sperry@auckland.ac.nz (JS) ; Email: i.leung@auckland.ac.nz (IKHL).
  • Kwai BXC; School of Chemical Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand . Email: j.sperry@auckland.ac.nz (JS) ; Email: i.leung@auckland.ac.nz (IKHL).
  • Swartjes A; School of Chemical Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand . Email: j.sperry@auckland.ac.nz (JS) ; Email: i.leung@auckland.ac.nz (IKHL).
  • Bashiri G; Institute for Molecules and Materials , Radboud University , Heyendaalseweg 135 , 6525 AJ , Nijmegen , The Netherlands.
  • Reynisson J; School of Biological Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand.
  • Sperry J; Maurice Wilkins Centre for Molecular Biodiscovery , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand.
  • Leung IKH; School of Chemical Sciences , The University of Auckland , Private Bag 92019, Victoria Street West , Auckland 1142 , New Zealand . Email: j.sperry@auckland.ac.nz (JS) ; Email: i.leung@auckland.ac.nz (IKHL).
Medchemcomm ; 8(11): 2155-2163, 2017 Nov 01.
Article em En | MEDLINE | ID: mdl-30108733
ABSTRACT
The enzymes isocitrate lyase (ICL) isoforms 1 and 2 are essential for Mycobacterium tuberculosis survival within macrophages during latent tuberculosis (TB). As such, ICLs are attractive therapeutic targets for the treatment of tuberculosis. However, there are few biophysical assays that are available for accurate kinetic and inhibition studies of ICL in vitro. Herein we report the development of a combined NMR spectroscopy and thermal shift assay to study ICL inhibitors for both screening and inhibition constant (IC50) measurement. Operating this new assay in tandem with virtual high-throughput screening has led to the discovery of several new ICL1 inhibitors.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2017 Tipo de documento: Article