Sergio C Chai

Summary

Affiliation: Indiana University
Country: USA

Publications

  1. pmc Analysis of the stoichiometric metal activation of methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, USA
    BMC Biochem 10:32. 2009
  2. pmc Catalysis and inhibition of Mycobacterium tuberculosis methionine aminopeptidase
    Jing Ping Lu
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, Indiana 46202, USA
    J Med Chem 53:1329-37. 2010
  3. pmc Synthesis and structure-function analysis of Fe(II)-form-selective antibacterial inhibitors of Escherichia coli methionine aminopeptidase
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 19:1080-3. 2009
  4. pmc Metal-mediated inhibition is a viable approach for inhibiting cellular methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 19:6862-4. 2009
  5. pmc Discovery of inhibitors of Escherichia coli methionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, USA
    J Med Chem 51:6110-20. 2008
  6. pmc Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 21:7151-4. 2011
  7. pmc Determination of binding affinity of metal cofactor to the active site of methionine aminopeptidase based on quantitation of functional enzyme
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Anal Biochem 395:263-4. 2009
  8. pmc Growth inhibition of Escherichia coli and methicillin-resistant Staphylococcus aureus by targeting cellular methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Eur J Med Chem 46:3537-40. 2011
  9. pmc A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 20:2129-32. 2010
  10. pmc Hydrophilic residues are crucial for ribosomal protein L11 (RPL11) interaction with zinc finger domain of MDM2 and p53 protein activation
    Qi Zhang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine Simon Cancer Center, Indianapolis, Indiana 46032, USA
    J Biol Chem 286:38264-74. 2011

Collaborators

  • Qi Zhuang Ye
  • Hui Xiao
  • Qi Zhang
  • Wen Long Wang
  • Ji Hoon Lee
  • Hai Yuan
  • Jing Ping Lu
  • Wonpil Im
  • Sunhwan Jo
  • H Howard Xu
  • Hua Lu
  • Misook Oh
  • Hyun Suk Lim
  • Christopher K Lam
  • Min Huang
  • Thomas D Hurley
  • Hong Zhen He

Detail Information

Publications13

  1. pmc Analysis of the stoichiometric metal activation of methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, USA
    BMC Biochem 10:32. 2009
    ..Herein, we report a mathematical model and detailed analysis of the stoichiometric activation of MetAP by metal cofactors...
  2. pmc Catalysis and inhibition of Mycobacterium tuberculosis methionine aminopeptidase
    Jing Ping Lu
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, Indiana 46202, USA
    J Med Chem 53:1329-37. 2010
    ..Finally, X-ray structures of MtMetAP1c in complex with three metalloform-selective inhibitors were analyzed, which showed different binding modes and different interactions with metal ions and active site residues...
  3. pmc Synthesis and structure-function analysis of Fe(II)-form-selective antibacterial inhibitors of Escherichia coli methionine aminopeptidase
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 19:1080-3. 2009
    ..coli AS19 strain. These findings provide useful information for the design and discovery of more effective MetAP inhibitors for therapeutic applications...
  4. pmc Metal-mediated inhibition is a viable approach for inhibiting cellular methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 19:6862-4. 2009
    ..Contrary to previous beliefs, this shows that metal-mediated inhibition is a viable approach for discovering MetAP inhibitors that are effective for therapeutic application...
  5. pmc Discovery of inhibitors of Escherichia coli methionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, USA
    J Med Chem 51:6110-20. 2008
    ..Our data indicate that Fe(II) is the likely metal used by MetAP in the cellular environment, and MetAP inhibitors need to inhibit this metalloform of MetAP effectively to be therapeutically useful...
  6. pmc Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors
    Wen Long Wang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 21:7151-4. 2011
    ..These findings are consistent with our previous conclusion that Fe(II) is the likely metal used by MetAP in bacterial cells and provide new lead structures that can be further developed as novel antibacterial agents...
  7. pmc Determination of binding affinity of metal cofactor to the active site of methionine aminopeptidase based on quantitation of functional enzyme
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Anal Biochem 395:263-4. 2009
    ..We applied this concept to methionine aminopeptidase from Mycobacterium tuberculosis and showed that it is a monometalated enzyme with a K(D) of 0.13 microM for Co(2+)...
  8. pmc Growth inhibition of Escherichia coli and methicillin-resistant Staphylococcus aureus by targeting cellular methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Eur J Med Chem 46:3537-40. 2011
    ..coli cells. These findings can serve as foundation for the development of novel therapeutics against an ever increasing threat by drug resistant staphylococcal infections...
  9. pmc A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 20:2129-32. 2010
    ..This cell-based assay is applicable to those cellular targets with poorly defined native cofactor, increasing the chances of identifying inhibitors that can inhibit the cellular target...
  10. pmc Hydrophilic residues are crucial for ribosomal protein L11 (RPL11) interaction with zinc finger domain of MDM2 and p53 protein activation
    Qi Zhang
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine Simon Cancer Center, Indianapolis, Indiana 46032, USA
    J Biol Chem 286:38264-74. 2011
    ....
  11. pmc Two methionine aminopeptidases from Acinetobacter baumannii are functional enzymes
    Hai Yuan
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bioorg Med Chem Lett 21:3395-8. 2011
    ..The similarity of their catalysis and inhibition to other MetAP enzymes confirmed that both may function as competent MetAP enzymes in A. baumannii and either or both may serve as the potential drug target...
  12. pmc Novel pyrrolopyrimidine-based α-helix mimetics: cell-permeable inhibitors of protein−protein interactions
    Ji Hoon Lee
    Department of Biochemistry and Molecular Biology, and Indiana University Simon Cancer Center, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States
    J Am Chem Soc 133:676-9. 2011
    ..Using a fluorescence polarization-based assay, we identified cell-permeable, dual MDMX/MDM2 inhibitors, demonstrating that the designed molecules can act as α-helix mimetics...
  13. pmc FE(II) is the native cofactor for Escherichia coli methionine aminopeptidase
    Sergio C Chai
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, USA
    J Biol Chem 283:26879-85. 2008
    ..Therefore, we conclude that Fe(II) is the likely metal used by MetAP in E. coli and other bacterial cells...