Naoaki Fujii

Summary

Affiliation: St. Jude Children's Research Hospital
Country: USA

Publications

  1. ncbi request reprint Design of a selective chemical probe for class I PDZ domains
    Naoaki Fujii
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Bioorg Med Chem Lett 17:546-8. 2007
  2. ncbi request reprint An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, Thoracic Oncology Labratory, University of California San Francisco, and Department of Structural Biology, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Cancer Res 67:573-9. 2007
  3. ncbi request reprint Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactions
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143, USA
    Bioorg Med Chem Lett 17:549-52. 2007
  4. doi request reprint Small molecule inhibitors of PCNA/PIP-box interaction suppress translesion DNA synthesis
    Marcelo Actis
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Bioorg Med Chem 21:1972-7. 2013
  5. ncbi request reprint An anti-Wnt-2 monoclonal antibody induces apoptosis in malignant melanoma cells and inhibits tumor growth
    Liang You
    Thoracic Oncology Laboratory, Department of Surgery, Comprehensive Cancer Center, University of California San Francisco, 1600 Divisadero Street, San Francisco, CA 94143 1674, USA
    Cancer Res 64:5385-9. 2004
  6. ncbi request reprint A selective irreversible inhibitor targeting a PDZ protein interaction domain
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California at San Francisco, Genentech Hall, Mission Bay, 600 16th Street 2280, San Francisco, California 94143 2280, USA
    J Am Chem Soc 125:12074-5. 2003
  7. pmc Identification of small molecule proliferating cell nuclear antigen (PCNA) inhibitor that disrupts interactions with PIP-box proteins and inhibits DNA replication
    Chandanamali Punchihewa
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    J Biol Chem 287:14289-300. 2012
  8. pmc Structure-activity relationships and cancer-cell selective toxicity of novel inhibitors of glioma-associated oncogene homologue 1 (Gli1) mediated transcription
    Neeraj Mahindroo
    St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    J Med Chem 52:4277-87. 2009
  9. doi request reprint Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity
    Neeraj Mahindroo
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Bioorg Med Chem Lett 18:946-9. 2008
  10. pmc Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway
    Neeraj Mahindroo
    Departments of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Bioorg Med Chem 18:4801-11. 2010

Collaborators

Detail Information

Publications22

  1. ncbi request reprint Design of a selective chemical probe for class I PDZ domains
    Naoaki Fujii
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Bioorg Med Chem Lett 17:546-8. 2007
    ..A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome...
  2. ncbi request reprint An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, Thoracic Oncology Labratory, University of California San Francisco, and Department of Structural Biology, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Cancer Res 67:573-9. 2007
    ..FJ9 is thus among the first non-peptide inhibitors to show therapeutic efficacy through disruption of PDZ protein-protein interactions...
  3. ncbi request reprint Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactions
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143, USA
    Bioorg Med Chem Lett 17:549-52. 2007
    ..The 10a scaffold inhibited the interaction between MAGI-3 and PTEN and showed cellular activities that are consistent with the inhibition of NHERF-1 function...
  4. doi request reprint Small molecule inhibitors of PCNA/PIP-box interaction suppress translesion DNA synthesis
    Marcelo Actis
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Bioorg Med Chem 21:1972-7. 2013
    ..PCNA inhibitors increased γH2AX induction and cell viability reduction mediated by cisplatin. Taken together, these findings suggest that inhibitors of PCNA/PIP-box interaction could chemosensitize cells to cisplatin by inhibiting TLS...
  5. ncbi request reprint An anti-Wnt-2 monoclonal antibody induces apoptosis in malignant melanoma cells and inhibits tumor growth
    Liang You
    Thoracic Oncology Laboratory, Department of Surgery, Comprehensive Cancer Center, University of California San Francisco, 1600 Divisadero Street, San Francisco, CA 94143 1674, USA
    Cancer Res 64:5385-9. 2004
    ..In an in vivo study, this monoclonal anti-Wnt-2 antibody suppresses tumor growth in a xenograft model. These findings suggest that the anti-Wnt-2 monoclonal antibody may be useful for the treatment of patients with malignant melanoma...
  6. ncbi request reprint A selective irreversible inhibitor targeting a PDZ protein interaction domain
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California at San Francisco, Genentech Hall, Mission Bay, 600 16th Street 2280, San Francisco, California 94143 2280, USA
    J Am Chem Soc 125:12074-5. 2003
    ..In cells, the inhibitor can be shown to release PTEN from sequestration by MAGI3 and consequently upregulate the PKB signaling pathway...
  7. pmc Identification of small molecule proliferating cell nuclear antigen (PCNA) inhibitor that disrupts interactions with PIP-box proteins and inhibits DNA replication
    Chandanamali Punchihewa
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    J Biol Chem 287:14289-300. 2012
    ..When cells were treated with a combination of cisplatin and T2AA, a significant increase in phospho(Ser(139))histone H2AX induction and cell growth inhibition was observed...
  8. pmc Structure-activity relationships and cancer-cell selective toxicity of novel inhibitors of glioma-associated oncogene homologue 1 (Gli1) mediated transcription
    Neeraj Mahindroo
    St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    J Med Chem 52:4277-87. 2009
    ..These compounds decreased the viability of several cancer cell lines but were less active in the noncancerous BJ-hTERT cells...
  9. doi request reprint Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity
    Neeraj Mahindroo
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Bioorg Med Chem Lett 18:946-9. 2008
    ..These compounds inhibit Tcf-mediated transcription activated by exogenous Dvl via the biochemical antagonism. We confirmed tumor cell-selective activation of caspases by these compounds...
  10. pmc Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway
    Neeraj Mahindroo
    Departments of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Bioorg Med Chem 18:4801-11. 2010
    ..6 μM and 1.6 μM of IC₅₀, respectively, and in Rh30 cells that endogenously overexpress Gli1, and were selective to Gli1 over Gli2...
  11. pmc Sequence requirement and subtype specificity in the high-affinity interaction between human frizzled and dishevelled proteins
    Chandanamali Punchihewa
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, Tennessee 38105 36781, USA
    Protein Sci 18:994-1002. 2009
    ..Molecular modeling and circular dichroism studies indicated that the Fz peptides that bind to Dvl PDZ domain form specific conformations that are different from those of nonbinding peptides...
  12. doi request reprint Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains
    Anand Mayasundari
    Department of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Bioorg Med Chem Lett 18:942-5. 2008
    ..Comparison of the peptide sequence homology between the native ligand of NHERF1 PDZ domains and an indole-based non-peptide chemical scaffold allowed the design of a small-molecule antagonist of NHERF1 PDZ domains...
  13. pmc Functional regulation of cystic fibrosis transmembrane conductance regulator-containing macromolecular complexes: a small-molecule inhibitor approach
    Weiqiang Zhang
    Department of Physiology, University of Tennessee Health Science Center, Memphis, TN 38163, USA
    Biochem J 435:451-62. 2011
    ..The present study might help to identify novel therapeutic targets to treat diseases associated with dysfunctional CFTR Cl- channels...
  14. doi request reprint A structure-activity relationship study of small-molecule inhibitors of GLI1-mediated transcription
    Marcelo Actis
    Medicinal Chemistry Center, Departments of Chemical Biology and Therapeutics, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Biopolymers 95:24-30. 2011
    ..Among them, sulfone 30 inhibited Gli-luciferase reporter in C3H10T1/2 cells that were exogenously transfected with GLI1 and in Rh30 cells that endogenously overexpress GLI1...
  15. pmc Recent advances and new perspectives in targeting CFTR for therapy of cystic fibrosis and enterotoxin-induced secretory diarrheas
    Weiqiang Zhang
    Department of Physiology, University of Tennessee Health Science Center, Memphis, TN 38163, USA
    Future Med Chem 4:329-45. 2012
    ..Also importantly, new ideas and methodologies are emerging. Targeting CFTR-containing macromolecular complexes is one such novel approach...
  16. ncbi request reprint Investigation of the PDZ domain ligand binding site using chemically modified peptides
    Kathleen A P Novak
    Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143 0446, USA
    Bioorg Med Chem Lett 12:2471-4. 2002
    ..Analogues of the ligand carboxy terminus revealed that the full hydrogen bond network of the GLGF loop is important in ligand binding...
  17. doi request reprint The hydrophobic amino acid cluster at the cytoplasmic end of transmembrane helix III modulates the coupling of the β(1)-adrenergic receptor to G(s)
    Hassan Hajjhussein
    Department of Pharmacology, The University of Tennessee Health Sciences Center, Memphis, TN 38163, USA
    J Recept Signal Transduct Res 33:79-88. 2013
    ..These results indicate that mutations in the G(s)α-binding pocket of the GPCR interfered with receptor coupling to G(s) and with its downstream signaling cascades...
  18. ncbi request reprint Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94143, USA
    Bioorg Med Chem Lett 15:121-3. 2005
    ..Among the active inhibitors, several potently inhibited proliferation of cultures of T. brucei. However, only modest activity was observed in inhibition of proliferation of T. cruzi or P. falciparum...
  19. ncbi request reprint A novel protein crosslinking reagent for the determination of moderate resolution protein structures by mass spectrometry (MS3-D)
    Naoaki Fujii
    Department of Pharmaceutical Chemistry, University of California at San Francisco, San Francisco, CA 94143, USA
    Bioorg Med Chem Lett 14:427-9. 2004
    ....
  20. ncbi request reprint Evaluation of a chemical library of small-molecule Dishevelled antagonists that suppress tumor growth by down-regulating T-cell factor-mediated transcription
    Liang You
    Thoracic Oncology Laboratory, Department of Surgery, Comprehensive Cancer Center, University of California at San Francisco, San Francisco, California, USA
    Mol Cancer Ther 7:1633-8. 2008
    ..A new compound (24) that met the criteria for high biochemical antagonism, T-cell factor-mediated transcription, and induction of tumor-selective apoptosis was found to significantly suppress the growth of tumor xenografts in mice...
  21. ncbi request reprint Role of electrostatic interactions in PDZ domain ligand recognition
    Baruch Z Harris
    Program in Biological Sciences, Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California 94143, USA
    Biochemistry 42:2797-805. 2003
    ..Peptides with a free carboxy terminus, or presented within a specific structural context, can satisfy these requirements...
  22. doi request reprint Partial acetylation of lysine residues improves intraprotein cross-linking
    Xin Guo
    Department of Pharmaceutics and Medicinal Chemistry, University of the Pacific, Stockton, CA 95211, USA
    Anal Chem 80:951-60. 2008
    ....