Research Topics
Genomes and GenesSpecies | Naoaki FujiiSummaryAffiliation: St. Jude Children's Research Hospital Country: USA Publications
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Publications
An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growthNaoaki 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...- Design of a selective chemical probe for class I PDZ domainsNaoaki 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... - Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactionsNaoaki 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... - A selective irreversible inhibitor targeting a PDZ protein interaction domainNaoaki 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... 
Identification of small molecule proliferating cell nuclear antigen (PCNA) inhibitor that disrupts interactions with PIP-box proteins and inhibits DNA replicationChandanamali 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...
Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domainsAnand 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...- Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activityNeeraj 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... - Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathwayNeeraj 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... - Sequence requirement and subtype specificity in the high-affinity interaction between human frizzled and dishevelled proteinsChandanamali 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... - A structure-activity relationship study of small-molecule inhibitors of GLI1-mediated transcriptionMarcelo 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... - Functional regulation of cystic fibrosis transmembrane conductance regulator-containing macromolecular complexes: a small-molecule inhibitor approachWeiqiang 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... - Structure-activity relationships and cancer-cell selective toxicity of novel inhibitors of glioma-associated oncogene homologue 1 (Gli1) mediated transcriptionNeeraj 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... - Recent advances and new perspectives in targeting CFTR for therapy of cystic fibrosis and enterotoxin-induced secretory diarrheasWeiqiang 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... - Investigation of the PDZ domain ligand binding site using chemically modified peptidesKathleen 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... - Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzainNaoaki 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... - 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.... - Evaluation of a chemical library of small-molecule Dishevelled antagonists that suppress tumor growth by down-regulating T-cell factor-mediated transcriptionLiang 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... - An anti-Wnt-2 monoclonal antibody induces apoptosis in malignant melanoma cells and inhibits tumor growthLiang 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... - Role of electrostatic interactions in PDZ domain ligand recognitionBaruch 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... - Partial acetylation of lysine residues improves intraprotein cross-linkingXin Guo
Department of Pharmaceutics and Medicinal Chemistry, University of the Pacific, Stockton, CA 95211, USA
Anal Chem 80:951-60. 2008....