Naoaki Fujii, PhD
Naoaki Fujii, PhD

Naoaki Fujii, PhD

Associate Member, St. Jude Faculty



BS – Tokai University, Japan (1986)
MS – Tokyo Institute of Technology, Japan (1988)
PhD – Osaka University, Japan (1998)

Research Interests

  • Functional small molecule inhibitor of Dishevelled
  • Small molecular agents targeting DNA replication and translesion DNA synthesis 

Selected Publications

Kamadurai HB, Deng A, Qiu Y, Harrison J, Souphron J, Miller D, Actis M, Rodrigues P, Fujii N, MacDonald C, Kurinov I, Piper R, Kuhlman B, Hammel M, Schulman BA. Structure of a HECT E3~Ubiquitin-substrate complex. eLife e00828, 2013.

Bosco-Clément G, Zhang F, Chen Z, Zhou HM, Li H, Mikami I, Hirata T, Yagui-Beltran A, Lui N, Do HT, Cheng T, Tseng HH, Choi H, Fang LT, Kim IJ, Yue D,Wang C, Zheng Q, Fujii N, Mann M, Jablons DM, He B. Targeting Gli transcription activation by small molecule suppresses tumor growth. Oncogene doi:10.1038/onc.2013.164, 2013.

Inoue A, Kikuchi S, Hishiki A, Shao Y, Heath R, Evison BJ, Actis M, Canman CE, Hashimoto H, Fujii N. A small molecule inhibitor of monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibits repair of interstrand DNA crosslink, enhances DNA double-strand break, and sensitizes cancer cells to cisplatin. J Biol Chem doi: 10.1074/jbc.M113.520429, 2014.

Actis M, Inoue A, Evison B, Perry S, Punchihewa C, Fujii N. Small molecule inhibitors of PCNA/PIP-box interaction suppress translesion DNA synthesis. Bioorg Med Chem 21:1972-7, 2013. PMID 23395113.

Hajjhusseina H, Gardner LA, Fujii N, Anderson NM, Bahouth SW. The Hydrophobic Amino Acid Cluster at the Cytoplasmic End of Transmembrane Helix III Modulates the Coupling of the β1-Adrenergic Receptor to Gs. Journal of Receptors and Signal Transduction Jan 25, 2013. PMID: 23351074

Punchihewa C, Inoue A, Hishiki A, Fujikawa Y, Connelly M, Evison B, Shao Y, Heath R, Kuraoka I, Rodrigues P, Hashimoto H, Kawanishi M, Sato M, Yagi T, Fujii N. Identification of Small Molecule Proliferating Cell Nuclear Antigen (PCNA) Inhibitor That Disrupts Interactions with PIP-box Proteins and Inhibits DNA Replication. J Biol Chem 287:14289-14300, 2012. PMID22383522.

Zhang W, Fujii N, Naren AP. Recent advances and new perspectives in targeting CFTR for therapy of cystic fibrosis and enterotoxin-induced secretory diarrheas. Future Med Chem 4:329-345, 2012. PMID22393940.

Zhang W, Penmatsa H, Ren A, Punchihewa C, Lemoff A, Yan B, Fujii N, Naren AP. Functional regulation of cystic fibrosis transmembrane conductance regulator-containing macromolecular complexes: a small-molecule inhibitor approach. Biochem J 435:451-462, 2011. PMID21299497.

Actis M, Connelly MC, Mayasundari A, Punchihewa C, Fujii N. A Structure-Activity Relationship Study of Small-Molecule Inhibitors of GLI1-Mediated Transcription. Biopolymers 95:24-30, 2011. PMID20872873.

Mayasundari A., Fujii N. Efficient formation of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines: A novel route to TWS119, a glycogen synthase kinase-3beta inhibitor. Tetrahedron Letters 51:3597-8, 2010.

Mahindroo N, Connelly MC, Punchihewa C, Yang L, Yan B, Fujii N. Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway. Bioorg Med Chem 18:4801-11, 2010.

Punchihewa C, Ferreira AM, Cassell R, Rodrigues P, Fujii N. Sequence requirement and subtype specificity in the high-affinity interaction between human Frizzled and Dishevelled proteins. Protein Science 18:994-1002, 2009.

Mahindroo N, Punchihewa C, Fujii N. Hedgehog-Gli signaling pathway inhibitors as anticancer agents. Journal of Medicinal Chemistry 52:3829-3845, 2009.

Mahindroo N, Connelly MC, Punchihewa C, Kimura H, Smeltzer MP, Wu S, Fujii N. Structure-Activity Relationships and Cancer-Cell Selective Toxicity of Novel Inhibitors of Glioma-Associated Oncogene Homolog 1 (Gli1)-Mediated Transcription. Journal of Medicinal Chemistry 52:4277-4287, 2009.

You L, Xu Z, Punchihewa C, Jablons DM, Fujii N. Evaluation of a chemical library of small-molecule Dishevelled antagonists that suppress tumor growth by down-regulating Tcf-mediated transcription. Molecular Cancer Therapeutics 7:1633-1638, 2008.

Mahindroo N, Punchihewa C, Bail AM, Fujii N. Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity. Bioorganic & Medicinal Chemistry Letters 946-949, 2008.

Mayasundari A, Ferreira AM, He L, Mahindroo N, Bashford D, Fujii N. Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains. Bioorganic & Medicinal Chemistry Letters 942-945, 2008.

Fujii N (corresponding author), You L, Xu Z, Uematsu K, Shan J, He B, Mikami I, Edmondson L, Neale G, Zheng J, Guy RK, Jablons DM. An antagonist of Dishevelled protein-protein interaction suppresses ß-catenin –dependent tumor cell growth. Cancer Research 573-579, 2007.

Guo X, Bandyopadhyay P, Schilling B, Young MM, Fujii N, Aynechi T, Guy RK, Kuntz ID, Gibson BW. Partial acetylation of lysine residues improves intraprotein cross-linking. Anal Chem 951-960, 2008.

Fujii N (corresponding author), Shelat A, Hall RA, Guy RK. Design of a Selective Chemical Probe for Class I PDZ Domains. Bioorganic & Medicinal Chemistry Letters 546-548, 2007.

Fujii N, Haresco JJ, Novak KAP, Gage R, Pedemonte N, Stokoe D, Kuntz ID, Guy RK. Rational Design of a Nonpeptide General Chemical Scaffold for Reversible Inhibition of PDZ Domain Interactions. Bioorganic & Medicinal Chemistry Letters 549-552, 2007.

Fujii N, Mallari JP, Hansell EJ, Mackey Z, Doyle P, Zhou YM, Gut J, Rosenthal PJ, McKerrow JH, Guy RK. Discovery of Potent Thiosemicarbazone Inhibitors of Rhodesain and Cruzain. Bioorganic & Medicinal Chemistry Letters 15:121-123, 2005.

Hattori K, Tanaka A, Fujii N, Takasugi H, Tenda Y, Tomita M, Nakazato S, Nakano K, Kato Y, Kono Y, Murai H, Sakane K. Discovery of Diphenyloxazole and Ornithine Derivatives as Highly Potent and Selective Human Prostaglandin EP4 Receptor Antagonists. Journal of Medicinal Chemistry 3103-3106, 2005.

You L, He B, Xu Z, Uematsu K, Mazieres J, Fujii N, Mikami I, Reguart N, McIntosh JK, Kashani-Sabet M, McCormick F, Jablons DM. An anti-Wnt-2 Monoclonal Antibody Induces Apoptosis in Malignant Melanoma Cells and Inhibits Tumor Growth. Cancer Res 5385-5389, 2004.

Fujii N, Jacobsen RB, Wood NL, Schoeniger JS, Guy RK. A Novel Protein Crosslinking Reagent for the Determination of Moderate Resolution Protein Structures by Mass Spectrometry (MS3-D). Bioorganic & Medicinal Chemistry Letters 427-429, 2004.

Fujii N, Haresco JJ, Novak KAP, Stokoe D, Kuntz ID, Guy RK. A Selective Irreversible Inhibitor Targeting a PDZ Protein Interaction Domain. Journal of the American Chemical Society 12074-12075, 2003.

Fujii N, Haresco JJ, Novak KAP, Stokoe D, Kuntz ID, Guy RK. A Selective Irreversible Inhibitor Targeting a PDZ Protein Interaction Domain. Journal of the American Chemical Society 125:12074-12075, 2003.

Harris BZ, Lau FW, Fujii N, Guy RK, Lim WA. Role of Electrostatic Interactions in PDZ Domain Ligand Recognition. Biochemistry 2797-2805, 2003.

Novak KAP, Fujii N, Guy RK. Investigation of the PDZ domain ligand binding site using chemically modified peptides. Bioorganic & Medicinal Chemistry Letters 2471-2474, 2002.

Show More

Fujii N, Kakiuchi F, Yamada A, Chatani N, Murai S. Asymmetric intramolecular C-H/olefin coupling: asymmetric cyclization reactions of 1,5-dienes catalyzed by rhodium complexes. Chemistry Letters 425-426, 1997.

Fujii N, Kakiuchi F, Yamada A, Chatani N, Murai S. Asymmetric intramolecular C-H/olefin coupling: asymmetric cyclization reactions of 1,5-dienes catalyzed by rhodium complexes. Chemistry Letters 425-426, 1997.

Fujii N, Kakiuchi F, Chatani N, Murai S. Transition metal-catalyzed intramolecular C-H/olefin coupling. Chemistry Letters 939-940, 1996.

Asaoka M, Sonoda S, Fujii N, Takei H. Diastereoselective 1,4-addition of various nucleophiles to 5-trimethylsilyl-2-cyclohexenone: synthesis of (+)-ramulosin. Tetrahedron 46: 1541-1552, 1990.

Asaoka M, Fujii N, Shima K, Takei H. 3-Substituted-g-butyrolactones from 5-trimethylsilyl-2-cyclohexenone. Synthesis of (-)-enterolactone. Chemistry Letters 805-808, 1988.

Asaoka M, Fujii N, Takei H. Synthesis of (R)-(-)-O-methyljoubertiamine. Chemistry Letters 1655-1656, 1988.

Asaoka M, Shima K, Fujii N, Takei H. Synthesis of (+)-a-curcumene, (+)-curcumone, and (-)-methyl citronellate starting from optically pure 5-trimethylsilyl-2-cyclohexenone. Tetrahedron 44: 4757-4766, 1988.

Last update: January 2014