Hiroyuki Osada

Summary

Affiliation: RIKEN Brain Science Institute
Country: Japan

Publications

  1. doi request reprint Integrated profiling methods for identifying the targets of bioactive compounds: MorphoBase and ChemProteoBase
    Makoto Muroi
    Chemical Biology Research Group, RIKEN CSRS, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Nat Prod Rep 33:621-5. 2016
  2. ncbi request reprint High-throughput screening identifies small molecule inhibitors of molecular chaperones
    Yasumitsu Kondoh
    Chemical Biology Core Facility, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Curr Pharm Des 19:473-92. 2013
  3. ncbi request reprint Introduction of new tools for chemical biology research on microbial metabolites
    Hiroyuki Osada
    Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    Biosci Biotechnol Biochem 74:1135-40. 2010
  4. ncbi request reprint Photo-cross-linked small-molecule microarrays as chemical genomic tools for dissecting protein-ligand interactions
    Naoki Kanoh
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Chem Asian J 1:789-97. 2006
  5. ncbi request reprint The education system for chemical biology in Japanese universities
    Hiroyuki Osada
    Discovery Research Institute, RIKEN, Wako Shi, Saitama 351 0198, Japan
    ACS Chem Biol 1:492-4. 2006
  6. doi request reprint Cleavable linker for photo-cross-linked small-molecule affinity matrix
    Naoki Kanoh
    Tohoku University, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Bioconjug Chem 21:182-6. 2010
  7. doi request reprint RK-1355A and B, novel quinomycin derivatives isolated from a microbial metabolites fraction library based on NPPlot screening
    Chung Liang Lim
    1 Antibiotics Laboratory, RIKEN, Saitama, Japan 2 Industrial Biotechnology Research Laboratory, School of Biological Sciences, Universiti Sains Malaysia, Penang, Malaysia
    J Antibiot (Tokyo) 67:323-9. 2014
  8. ncbi request reprint Epoxyquinol B, a naturally occurring pentaketide dimer, inhibits NF-kappaB signaling by crosslinking TAK1
    Hiroshi Kamiyama
    Antibiotics Laboratory, RIKEN Advanced Science Institute, Wako, Saitama, Japan
    Biosci Biotechnol Biochem 72:1894-900. 2008
  9. ncbi request reprint Iejimalides show anti-osteoclast activity via V-ATPase inhibition
    Sayaka Kazami
    Antibiotics Laboratory, RIKEN Discovery Research Institute, Hirosawa, Saitama
    Biosci Biotechnol Biochem 70:1364-70. 2006
  10. pmc Isolation of new polyketide metabolites, linearolides A and B, from Streptomyces sp. RK95-74
    Masashi Ueki
    Antibiotics Laboratory, Chemical Biology Core Facility, Riken ASI, Wako, Japan
    J Antibiot (Tokyo) 66:333-7. 2013

Collaborators

Detail Information

Publications162 found, 100 shown here

  1. doi request reprint Integrated profiling methods for identifying the targets of bioactive compounds: MorphoBase and ChemProteoBase
    Makoto Muroi
    Chemical Biology Research Group, RIKEN CSRS, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Nat Prod Rep 33:621-5. 2016
    ..Here, we highlight the utility of our identification approaches, MorphoBase and ChemProteoBase. ..
  2. ncbi request reprint High-throughput screening identifies small molecule inhibitors of molecular chaperones
    Yasumitsu Kondoh
    Chemical Biology Core Facility, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Curr Pharm Des 19:473-92. 2013
    ....
  3. ncbi request reprint Introduction of new tools for chemical biology research on microbial metabolites
    Hiroyuki Osada
    Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    Biosci Biotechnol Biochem 74:1135-40. 2010
    ....
  4. ncbi request reprint Photo-cross-linked small-molecule microarrays as chemical genomic tools for dissecting protein-ligand interactions
    Naoki Kanoh
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Chem Asian J 1:789-97. 2006
    ....
  5. ncbi request reprint The education system for chemical biology in Japanese universities
    Hiroyuki Osada
    Discovery Research Institute, RIKEN, Wako Shi, Saitama 351 0198, Japan
    ACS Chem Biol 1:492-4. 2006
  6. doi request reprint Cleavable linker for photo-cross-linked small-molecule affinity matrix
    Naoki Kanoh
    Tohoku University, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Bioconjug Chem 21:182-6. 2010
    ..It also permits the efficient detection of proteins covalently bound to the immobilized small molecule...
  7. doi request reprint RK-1355A and B, novel quinomycin derivatives isolated from a microbial metabolites fraction library based on NPPlot screening
    Chung Liang Lim
    1 Antibiotics Laboratory, RIKEN, Saitama, Japan 2 Industrial Biotechnology Research Laboratory, School of Biological Sciences, Universiti Sains Malaysia, Penang, Malaysia
    J Antibiot (Tokyo) 67:323-9. 2014
    ..They showed potent antiproliferative activities against various cancer cell lines and they were also found to exhibit moderate antibacterial activity. ..
  8. ncbi request reprint Epoxyquinol B, a naturally occurring pentaketide dimer, inhibits NF-kappaB signaling by crosslinking TAK1
    Hiroshi Kamiyama
    Antibiotics Laboratory, RIKEN Advanced Science Institute, Wako, Saitama, Japan
    Biosci Biotechnol Biochem 72:1894-900. 2008
    ..We reported recently that EPQB crosslinks proteins via cysteine residues by opening its two epoxides, and our current results suggest that EPQB inhibits NF-kappaB signaling by crosslinking TAK1 itself or TAK1 through other proteins...
  9. ncbi request reprint Iejimalides show anti-osteoclast activity via V-ATPase inhibition
    Sayaka Kazami
    Antibiotics Laboratory, RIKEN Discovery Research Institute, Hirosawa, Saitama
    Biosci Biotechnol Biochem 70:1364-70. 2006
    ..These results indicate that IEJLs are novel V-ATPase inhibitors, and that antitumor and antiosteporotic activities are exerted via V-ATPase inhibition...
  10. pmc Isolation of new polyketide metabolites, linearolides A and B, from Streptomyces sp. RK95-74
    Masashi Ueki
    Antibiotics Laboratory, Chemical Biology Core Facility, Riken ASI, Wako, Japan
    J Antibiot (Tokyo) 66:333-7. 2013
    ..Following the cultivation with new media and the peak-guided fractionation, we have found new compounds with new polyketide scaffold, named linearolides A and B. ..
  11. doi request reprint Protein disulfide isomerase-mediated disulfide bonds regulate the gelatinolytic activity and secretion of matrix metalloproteinase-9
    Maola M G Khan
    Chemical Library Validation Team, Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    Exp Cell Res 318:904-14. 2012
    ..However, the disulfide bond of the hemopexin domain and other cysteines have no significant role in secretion. These insights into the secretion of MMP-9 constitute the basis for the development of potential drugs against metastasis...
  12. doi request reprint Requirement of the conserved, hydrophobic C-terminus region for the activation of heparanase
    Ngit Shin Lai
    Antibiotics Laboratory, Advanced Science Institute, RIKEN, Saitama 351 0198, Japan
    Exp Cell Res 314:2834-45. 2008
    ..Therefore, our findings suggest that the hydrophobic C-terminus region of heparanase is a determinant for its intracellular trafficking to the Golgi apparatus, followed by secretion, activation, and tumor cell migration...
  13. ncbi request reprint Novel heparan sulfate mimetic compounds as antitumor agents
    Keisuke Ishida
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Chem Biol 11:367-77. 2004
    ..Although further investigations are needed to decipher the molecular mechanism of KI-105, it is suggested that heparanase and Cdc42 are involved in its biological effects...
  14. doi request reprint A small-molecule inhibitor shows that pirin regulates migration of melanoma cells
    Isao Miyazaki
    Chemical Library Validation Team, Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Wako, Saitama, Japan
    Nat Chem Biol 6:667-73. 2010
    ..Thus, inhibition of pirin by the small molecule has led to a greater understanding of the function of pirin and represents a new method of studying pirin-mediated signaling pathways...
  15. pmc The identification of an osteoclastogenesis inhibitor through the inhibition of glyoxalase I
    Makoto Kawatani
    Antibiotics Laboratory, Chemical Biology Department, and Biomolecular Characterization Team, Advanced Technology Support Division, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Proc Natl Acad Sci U S A 105:11691-6. 2008
    ..Furthermore, the cocrystal structure of the GLO1/M-GFN complex revealed the binding mode of M-GFN at the active site of GLO1. These results suggest that M-GFN targets GLO1, resulting in the inhibition of osteoclastogenesis...
  16. doi request reprint Specific regulation of cytokine-dependent p38 MAP kinase activation by p62/SQSTM1
    Kayoko Kawai
    Antibiotics Laboratory and Bioarchitect Research Group, DRI, RIKEN, 2 1 Hirosawa, Wako, Saitama, 351 0198, Japan
    J Biochem 143:765-72. 2008
    ..Cytokine mRNA is often stabilized via p38 pathway. In the absence of p62, IL-8 mRNA induced by IL-1beta became more fragile. These data show that p62 specifically regulates cytokine-dependent p38 signalling pathway...
  17. pmc Biochemical characterization of a novel indole prenyltransferase from Streptomyces sp. SN-593
    Shunji Takahashi
    Chemical Biology Department, Advanced Science Institute, RIKEN, Hirosawa 2 1, Wako, Saitama 351 0198, Japan
    J Bacteriol 192:2839-51. 2010
    ..Moreover, DeltaiptA mutants abolished the production of 6-DMAI-3-carbaldehyde as well as 6-dimethylallyl-L-Trp, suggesting that the iptA gene is involved in the production of 6-DMAI-3-carbaldehyde...
  18. doi request reprint RECK negatively regulates matrix metalloproteinase-9 transcription
    Satoshi Takagi
    Antibiotics Laboratory and Chemical Biology Department, Advanced Science Institute, RIKEN and Graduate School of Science and Engineering, Saitama University, Saitama, Japan
    Cancer Res 69:1502-8. 2009
    ..Moreover, the binding ability of Fra-1 and c-Jun to TRE within the MMP-9 promoter region was suppressed by RECK. Thus, these results show that RECK is a negative regulator of MMP-9 transcription...
  19. pmc Epolactaene binds human Hsp60 Cys442 resulting in the inhibition of chaperone activity
    Yoko Nagumo
    Antibiotics Laboratory, Discovery Research Institute RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Biochem J 387:835-40. 2005
    ..These results indicate that this cysteine residue is alkylated by ETB, leading to Hsp60 inactivation...
  20. ncbi request reprint Structure-based design of a selective heparanase inhibitor as an antimetastatic agent
    Keisuke Ishida
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Mol Cancer Ther 3:1069-77. 2004
    ..5 micromol/L; IC50 for migration, 3.0 micromol/L). On the other hand, RK-682 had no inhibitory effect on the invasion and migration of HT1080 cells at doses of up to 100 micromol/L...
  21. ncbi request reprint Involvement of disulfide bond formation in the activation of heparanase
    Siro Simizu
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Saitama, Japan
    Cancer Res 67:7841-9. 2007
    ..Thus, the present findings will provide a basis for the further refinement of heparanase structural studies and for the development of novel heparanase inhibitors...
  22. doi request reprint Deficiency in chromosome congression by the inhibition of Plk1 polo box domain-dependent recognition
    Nobumoto Watanabe
    Chemical Biology Department, Antibiotics Laboratory, Advanced Science Institute, RIKEN, 2 1, Hirosawa, Wako, Saitama 351 0198, Japan
    J Biol Chem 284:2344-53. 2009
    ..These results demonstrate the predominant role of PBD-dependent binding on smooth chromosome congression at metaphase...
  23. doi request reprint Identification of a molecular target of a novel fungal metabolite, pyrrolizilactone, by phenotypic profiling systems
    Yushi Futamura
    Antibiotics Laboratory, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198 Japan
    Chembiochem 14:2456-63. 2013
    ..On the basis of these predictions, we determined that pyrrolizilactone is a novel type of proteasome inhibitor inhibiting the trypsin-like activity of the proteasome. ..
  24. doi request reprint Synthesis and biological activities of reveromycin A and spirofungin A derivatives
    Takeshi Shimizu
    Synthetic Organic Chemistry Laboratory, RIKEN The Institute of Physical and Chemical Research, Wako, Saitama 351 0198, Japan
    Bioorg Med Chem Lett 18:3756-60. 2008
    ..It was found that 2,3-dihydroreveromycin A is the promising derivative of reveromycin A based on the activity and stability...
  25. doi request reprint Improvement of photoaffinity SPR imaging platform and determination of the binding site of p62/SQSTM1 to p38 MAP kinase
    Akiko Saito
    Antibiotics Laboratory, Chemical Biology Department, Advanced Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama, 351 0198, Japan
    Chem Asian J 3:1607-12. 2008
    ..These SPR analysis data and empirical biologic data reveal that the binding site of p62 to p38 is the domain corresponding to 173-182...
  26. ncbi request reprint Robust and systematic drug screening method using chemical arrays and the protein library: identification of novel inhibitors of carbonic anhydrase II
    Isao Miyazaki
    Antibiotics Laboratory and Chemical Biology Department, RIKEN, Saitama, Japan
    Biosci Biotechnol Biochem 72:2739-49. 2008
    ..Using our systematic platform, we detected novel inhibitors of carbonic anhydrase II. It is suggested that our systematic platform is a rapid and robust approach to screen novel ligands for human proteins of interest...
  27. doi request reprint Application of proteomic profiling based on 2D-DIGE for classification of compounds according to the mechanism of action
    Makoto Muroi
    Chemical Library Validation Team, Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 17:460-70. 2010
    ..Thus far, combined data from 19 compounds have allowed their successful classification by cluster analysis according to the mechanism of action...
  28. ncbi request reprint p38 mitogen-activated protein kinase plays a key role in regulating MAPKAPK2 expression
    Tatsuhiko Sudo
    Antibiotics Laboratory and Bioarchitect Research Group, DRI, RIKEN, Wako, Saitama, Japan
    Biochem Biophys Res Commun 337:415-21. 2005
    ..Together, we have established cell lines that can be used in analyzing the functions of MAPKs, especially p38alpha, and show that p38 is indispensable for MAPKAPK2 expression...
  29. ncbi request reprint The phosphorylation status and anti-apoptotic activity of Bcl-2 are regulated by ERK and protein phosphatase 2A on the mitochondria
    Yuki Tamura
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    FEBS Lett 569:249-55. 2004
    ..Thus, the present findings suggest that ERK and PP2A are physiological regulators of Bcl-2 phosphorylation, and these enzymes exert an influence on the anti-apoptotic function of Bcl-2...
  30. doi request reprint Osteoclast-targeting small molecules for the treatment of neoplastic bone metastases
    Makoto Kawatani
    Antibiotics Laboratory, Chemical Biology Department, Advanced Science Institute, RIKEN, Wako Shi, Saitama, Japan
    Cancer Sci 100:1999-2005. 2009
    ..This review focuses on promising small molecules that disrupt osteoclast function and introduces our chemical/biological approach for identifying osteoclast-targeting small molecular inhibitors...
  31. ncbi request reprint Fumagillin suppresses HIV-1 infection of macrophages through the inhibition of Vpr activity
    Nobumoto Watanabe
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1, Hirosawa, Wako, 351 0198, Japan
    FEBS Lett 580:2598-602. 2006
    ..Fumagillin not only reversed the growth inhibitory activity of Vpr in yeast and human cells, but also inhibited Vpr-dependent viral gene expression upon the infection of human macrophages...
  32. doi request reprint Reveromycin A biosynthesis uses RevG and RevJ for stereospecific spiroacetal formation
    Shunji Takahashi
    Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    Nat Chem Biol 7:461-8. 2011
    ..Our findings provide insights into the creation of a variety of biologically active spiroacetal compounds for drug leads...
  33. pmc Vipirinin, a coumarin-based HIV-1 Vpr inhibitor, interacts with a hydrophobic region of VPR
    Eugene Boon Beng Ong
    From the Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    J Biol Chem 286:14049-56. 2011
    ..Our findings exposed a targeting site on Vpr and delineated a convenient approach to explore other targeting sites on the protein using small molecule inhibitors as bioprobes...
  34. pmc M-phase kinases induce phospho-dependent ubiquitination of somatic Wee1 by SCFbeta-TrCP
    Nobumoto Watanabe
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Proc Natl Acad Sci U S A 101:4419-24. 2004
    ..These results also establish the existence of a feedback loop between Cdc2 and Wee1A in somatic cells that depends on ubiquitination and protein degradation and ensures the rapid activation of Cdc2 when cells are ready to divide...
  35. ncbi request reprint A point mutation in ftmD blocks the fumitremorgin biosynthetic pathway in Aspergillus fumigatus strain Af293
    Naoki Kato
    Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Saitama, Japan
    Biosci Biotechnol Biochem 77:1061-7. 2013
    ..The mutated FtmD retained enzymatic activity but did not function under physiological conditions, resulting in blockage of the FTM pathway in A. fumigatus Af293...
  36. doi request reprint The application of the chemical array for biological study
    Isao Miyazaki
    Chemical Biology Department, RIKEN, Saitama, Japan
    Methods Mol Biol 669:95-107. 2010
    ..We present initial studies of fragment-based approach to binding assay by using the chemical array format...
  37. doi request reprint Morphobase, an encyclopedic cell morphology database, and its use for drug target identification
    Yushi Futamura
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 19:1620-30. 2012
    ..Furthermore, we demonstrate the applicability of this system in identifying NPD6689, NPD8617, and NPD8969 as tubulin inhibitors...
  38. doi request reprint Protuboxepin A, a marine fungal metabolite, inducing metaphase arrest and chromosomal misalignment in tumor cells
    Yukihiro Asami
    Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology KRIBB, 30 Yeongudanji ro, Ochang, Cheongwon, Chungbuk 363 883, Republic of Korea Chemical Biology Department, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Bioorg Med Chem 20:3799-806. 2012
    ..These results indicate that protuboxepin A has a potential of being a new and effective anti-cancer drug...
  39. doi request reprint Fungal metabolite, epoxyquinol B, crosslinks proteins by epoxy-thiol conjugation
    Hiroshi Kamiyama
    Antibiotics Laboratory, RIKEN Discovery Research Institute, Hirosawa, Wako, Saitama, Japan
    J Antibiot (Tokyo) 61:94-7. 2008
    ..Furthermore, EPQB crosslinked binding proteins through the cysteine residues. These results suggest that EPQB inhibits receptor kinases by crosslinking with other protein or by intramolecular crosslinking...
  40. doi request reprint A p38 mitogen-activated protein kinase inhibitor screening method using growth recovery of Escherichia coli as an index
    Kayoko Kawai
    Antibiotics Laboratory and Bioarchitect Research Group, RIKEN Advanced Science Institute, Wako, Saitama 351 0198, Japan
    Anal Biochem 388:128-33. 2009
    ..This study demonstrates that this is a promising and economical inhibitor screening method not only for p38 but also for other proteins...
  41. doi request reprint Identification of cytochrome P450s required for fumitremorgin biosynthesis in Aspergillus fumigatus
    Naoki Kato
    Chemical Biology Department, Advanced Science Institute, RIKEN, Wako, Saitama 351 0198, Japan
    Chembiochem 10:920-8. 2009
    ..Additionally, we demonstrated that the other two cytochrome P450 genes, ftmC and ftmG, were involved in hydroxylation of the indole ring and successive hydroxylation of fumitremorgin C, respectively...
  42. doi request reprint Identification of a novel Vpr-binding compound that inhibits HIV-1 multiplication in macrophages by chemical array
    Kyoji Hagiwara
    Viral Infectious Diseases Research Unit, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Biochem Biophys Res Commun 403:40-5. 2010
    ..Collectively, our results strongly suggest that chemical array is a useful method for screening anti-viral compounds...
  43. doi request reprint Identification of a small-molecule inhibitor of DNA topoisomerase II by proteomic profiling
    Makoto Kawatani
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Saitama 351 0198, Japan
    Chem Biol 18:743-51. 2011
    ..These results indicate that BNS-22 targets TOP2 and acts as its catalytic inhibitor...
  44. pmc Azaspirene, a fungal product, inhibits angiogenesis by blocking Raf-1 activation
    Yukihiro Asami
    Antibiotics Laboratory, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Cancer Sci 99:1853-8. 2008
    ..Taken together, these results demonstrate that azaspirene is a novel inhibitor of angiogenesis and Raf-1 activation that contains a unique carbon skeleton in its molecular structure...
  45. ncbi request reprint Immobilization of natural products on glass slides by using a photoaffinity reaction and the detection of protein-small-molecule interactions
    Naoki Kanoh
    Antibiotics Laboratory, Discovery Research Institute, RIKEN The Institute of Physical and Chemical Research, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Angew Chem Int Ed Engl 42:5584-7. 2003
  46. pmc Formation and dissociation of the BSS1 protein complex regulates plant development via brassinosteroid signaling
    Setsuko Shimada
    Antibiotics Laboratory, RIKEN, Wako, Saitama 351 0198, Japan Synthetic Genomics Research Team, Biomass Engineering Program Cooperation Division, RIKEN Center for Sustainable Resource Science, Tsurumi, Yokohama, Kanagawa 230 0045, Japan
    Plant Cell 27:375-90. 2015
    ..Our study suggests that the BSS1/BOP1 protein complex inhibits the transport of BIL1/BZR1 to the nucleus from the cytosol and negatively regulates BR signaling. ..
  47. ncbi request reprint Photo-cross-linked small-molecule affinity matrix for facilitating forward and reverse chemical genetics
    Naoki Kanoh
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Angew Chem Int Ed Engl 44:3559-62. 2005
  48. pmc Proteomic profiling of small-molecule inhibitors reveals dispensability of MTH1 for cancer cell survival
    Tatsuro Kawamura
    Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science CSRS, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Sci Rep 6:26521. 2016
    ..Taken together, we conclude that the cytotoxicity of MTH1 inhibitors is attributable to off-target effects and that MTH1 is not essential for cancer cell survival. ..
  49. doi request reprint Identification of small molecule inhibitors of p27(Kip1) ubiquitination by high-throughput screening
    Li Ching Ooi
    Antibiotics Laboratory, RIKEN, Hirosawa, Wako Shi, Saitama, Japan School of Biological Sciences, Universiti Sains Malaysia, Penang, Malaysia
    Cancer Sci 104:1461-7. 2013
    ..Our approach indicates a potential strategy for restoring p27(Kip1) levels in human cancers...
  50. ncbi request reprint The potential of protein disulfide isomerase as a therapeutic drug target
    Maola M G Khan
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    Oncol Res 19:445-53. 2011
    ..In this review, we will describe the potential of PDI as a therapeutic drug target...
  51. ncbi request reprint Phoslactomycin targets cysteine-269 of the protein phosphatase 2A catalytic subunit in cells
    Takayuki Teruya
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Wako, Saitama, Japan
    FEBS Lett 579:2463-8. 2005
    ..These results suggest that PLMA is a PP2A-selective inhibitor and is therefore expected to be useful for future investigation of PP2A function in cells...
  52. ncbi request reprint Exploitation of heparanase inhibitors from microbial metabolites using an efficient visual screening system
    Keisuke Ishida
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    J Antibiot (Tokyo) 57:136-42. 2004
    ..RK-682 was identified in the fermentation broth as a heparanase inhibitor, IC50 = 17 microM...
  53. doi request reprint Verticilactam, a new macrolactam isolated from a microbial metabolite fraction library
    Toshihiko Nogawa
    Chemical Biology Department, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Org Lett 12:4564-7. 2010
    ..The structure was determined on the basis of NMR and mass spectrometric measurements. 1 had a unique 16-membered macrolactam skeleton including a β-keto-amide moiety...
  54. ncbi request reprint SPR imaging of photo-cross-linked small-molecule arrays on gold
    Naoki Kanoh
    Antibiotics Laboratory and Beam Application Team, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Anal Chem 78:2226-30. 2006
    ..Interactions of estrogenic and androgenic substances with estrogen receptor alpha were observed using this platform...
  55. doi request reprint Structure-affinity relationship study of bleomycins and Shble protein by use of a chemical array
    Isao Miyazaki
    Antibiotics Laboratory and Chemical Biology Department, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Chembiochem 10:845-52. 2009
    ..These results provide insight into the structural requirements for recognition of BLMs by Shble protein...
  56. doi request reprint Discovery of a small molecule PDI inhibitor that inhibits reduction of HIV-1 envelope glycoprotein gp120
    Maola M G Khan
    Chemical Library Validation Team, Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Saitama, Japan
    ACS Chem Biol 6:245-51. 2011
    ..Moreover, we found that both compounds can inhibit PDI-mediated reduction of HIV-1 envelope glycoprotein gp120...
  57. doi request reprint Deamino-hydroxy-phoslactomycin B, a biosynthetic precursor of phoslactomycin, induces myeloid differentiation in HL-60 cells
    Siro Simizu
    Antibiotics Laboratory and Chemical Biology Department, Advanced Science Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Biochem Biophys Res Commun 383:406-10. 2009
    ..Moreover, treatment with ATRA and 1alpha, 25(OH)2D3 induced retinoic acid receptor-beta and 1alpha, 25(OH)2D3 24-hydroxylase, respectively, whereas HPLM did not, suggesting that HPLM is a novel differentiation inducer...
  58. ncbi request reprint Actin stress fiber retraction and aggresome formation is a common cellular response to actin toxins
    Sayaka Kazami
    Chemical Library Validation Team, Chemical Biology Core Facility, RIKEN Advanced Science Institute, Saitama
    Biosci Biotechnol Biochem 75:1853-5. 2011
    ..Because cytochalasin D and mycalolide also induced aggresome formation, these results suggest that actin aggresome formation is a common cellular response to actin toxins...
  59. doi request reprint Furaquinocins I and J: novel polyketide isoprenoid hybrid compounds from Streptomyces reveromyceticus SN-593
    Suresh Panthee
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Wakoshi, Saitama, Japan
    J Antibiot (Tokyo) 64:509-13. 2011
    ..The main difference between 1, 2 and 3 was the type of residue attached to C-13; these were a carboxyl, a carboxamide and a methyl residue, respectively...
  60. ncbi request reprint RK-95113, a new angiogenesis inhibitor produced by Aspergillus fumigatus
    Yukihiro Asami
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    J Antibiot (Tokyo) 59:724-8. 2006
    ....
  61. doi request reprint Octaminomycins A and B, Cyclic Octadepsipeptides Active against Plasmodium falciparum
    Jun Pil Jang
    RIKEN Global Research Cluster, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    J Nat Prod . 2017
    ..Notably, octaminomycins A (1) and B (2) showed good in vitro antiplasmodial activity against chloroquine-sensitive as well as chloroquine-resistant strains with no cytotoxicity up to 30 μM...
  62. pmc Structure-function analyses of cytochrome P450revI involved in reveromycin A biosynthesis and evaluation of the biological activity of its substrate, reveromycin T
    Shunji Takahashi
    From the Chemical Biology Group, RIKEN Center for Sustainable Resource Science, Saitama 351 0198, Japan, the Antibiotics Laboratory, RIKEN, Saitama 351 0198, Japan
    J Biol Chem 289:32446-58. 2014
    ..Structure-based P450revI engineering for novel hydroxylation and subsequent hemisuccinylation will help facilitate the development of RM derivatives with anti-osteoclast activity. ..
  63. pmc Detection of oxygen addition peaks for terpendole E and related indole-diterpene alkaloids in a positive-mode ESI-MS
    Yayoi Hongo
    Global Research Cluster, RIKEN, Wako, Japan
    J Mass Spectrom 49:537-42. 2014
    ..Terpendoles that are preferentially protonated at indole tend to form oxygen addition peaks, suggesting that the protonation feature contributes to the oxygen additions in some degrees...
  64. pmc A novel mitochondrial DnaJ/Hsp40 family protein BIL2 promotes plant growth and resistance against environmental stress in brassinosteroid signaling
    Davaapurev Bekh-Ochir
    RIKEN Advanced Science Institute, 2 1 Hirosawa, Saitama, Wako 351 0198, Japan
    Planta 237:1509-25. 2013
    ..BIL2 participates in resistance against salinity stress and strong light stress. Our results indicate that BIL2 induces cell elongation during BR signaling through the promotion of ATP synthesis in mitochondria...
  65. ncbi request reprint Brasilicardin A, a natural immunosuppressant, targets amino Acid transport system L
    Takeo Usui
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 13:1153-60. 2006
    ..These results suggest that the immunosuppressive activity of BraA is induced by amino acid deprivation via the inhibition of system L and that the amino acid transporter is a target for immunosuppressant...
  66. doi request reprint Genetic safeguard against mycotoxin cyclopiazonic acid production in Aspergillus oryzae
    Naoki Kato
    Chemical Biology Department, Advanced Science Institute, RIKEN, Wako, Saitama, Japan
    Chembiochem 12:1376-82. 2011
    ..The detoxifying properties of cpaH, which have been lost in the A. flavus pathway, reflect the relationship of the two species...
  67. pmc Cyclin-dependent kinase (CDK) phosphorylation destabilizes somatic Wee1 via multiple pathways
    Nobumoto Watanabe
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Proc Natl Acad Sci U S A 102:11663-8. 2005
    ..Using a specific inhibitor of CK2, we showed that the phosphorylation-dependent degradation of Wee1A is important for the proper onset of mitosis...
  68. ncbi request reprint Chemical modification of reveromycin A and its biological activities
    Takeshi Shimizu
    Synthetic Organic Chemistry Laboratory, RIKEN The Institute of Physical and Chemical Research, Wako, Saitama, Japan
    Bioorg Med Chem Lett 12:3363-6. 2002
    ..The C5 hydroxyl group and C24 carboxyl group are particularly important for these activities...
  69. doi request reprint Target identification of small molecules based on chemical biology approaches
    Yushi Futamura
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Wako Shi, Saitama 351 0198, Japan
    Mol Biosyst 9:897-914. 2013
    ..In this review, we describe and summarize recent progress in both affinity-based (direct) and phenotypic profiling (indirect) approaches for chemical biology target identification...
  70. doi request reprint Construction of a microbial natural product library for chemical biology studies
    Naoki Kato
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Curr Opin Chem Biol 16:101-8. 2012
    ..Our chemical library contributes to the discovery of molecular probes for increasing our understanding of complex biological processes and for eventually developing new drug leads...
  71. ncbi request reprint Amphidinolide h, a potent cytotoxic macrolide, covalently binds on actin subdomain 4 and stabilizes actin filament
    Takeo Usui
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 11:1269-77. 2004
    ..These results indicate that AmpH is a novel actin inhibitor that covalently binds on actin...
  72. doi request reprint Terpendole E, a kinesin Eg5 inhibitor, is a key biosynthetic intermediate of indole-diterpenes in the producing fungus Chaunopycnis alba
    Takayuki Motoyama
    Chemical Biology Core Facility, Chemical Biology Department, RIKEN Advanced Science Institute, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 19:1611-9. 2012
    ..We successfully overproduced terpendole E by disrupting the terP gene. We propose that terpendole E is a key biosynthetic intermediate of terpendoles and related indole-diterpenes...
  73. pmc Fluorescence image screening for chemical compounds modifying cholesterol metabolism and distribution
    Reiko Ishitsuka
    Lipid Biology Laboratory, RIKEN Advanced Science Institute, Wako Shi, Saitama 351 0198, Japan
    J Lipid Res 52:2084-94. 2011
    ..Furthermore, it is suitable for high-throughput analysis for drug discovery...
  74. ncbi request reprint Suppression of apoptosis by cyclophilin D via stabilization of hexokinase II mitochondrial binding in cancer cells
    Kiyotaka Machida
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Hirosawa 2 1, Saitama 351 0198, Japan
    J Biol Chem 281:14314-20. 2006
    ..Based on the above, we propose here that cyclophilin D suppresses apoptotic cell death via a mitochondrial hexokinase II-dependent mechanism in cancer cells...
  75. ncbi request reprint Development and application of bioprobes for Mammalian cell cycle analyses
    Hiroyuki Osada
    Antibiotics Laboratory, RIKEN, Hirosawa 2 1, Wako Shi, Saitama 351 0198, Japan
    Curr Med Chem 10:727-32. 2003
    ..On the contrary, cyclotryprostatin D, structurally related to tryprostatin A, enhanced the tubulin polymerization. Terpendole E inhibited the motor activity of mitotic kinesin, Eg5 and induced monoastral spindle in M phase...
  76. pmc Limonoid compounds inhibit sphingomyelin biosynthesis by preventing CERT protein-dependent extraction of ceramides from the endoplasmic reticulum
    Francoise Hullin-Matsuda
    Lipid Biology Laboratory, RIKEN Advanced Science Institute, Wako, Saitama 351 0198, Japan
    J Biol Chem 287:24397-411. 2012
    ..Our study shows that certain limonoids are novel inhibitors of SM biosynthesis and suggests that some biological activities of these limonoids are related to their effect on the ceramide metabolism...
  77. ncbi request reprint Reveromycin A inhibits osteolytic bone metastasis of small-cell lung cancer cells, SBC-5, through an antiosteoclastic activity
    Hiroaki Muguruma
    Department of Internal Medicine and Molecular Therapeutics, University of Tokushima Graduate School, Tokushima, and Antibiotics Laboratory, Discovery Research Institute, RIKEN, Saitama, Japan
    Clin Cancer Res 11:8822-8. 2005
    ..The purpose of this study was to determine therapeutic effect of a novel antibiotic, reveromycin A, against osteolytic bone metastasis of human small cell lung cancer (SBC-5) cells...
  78. ncbi request reprint [Development of novel angiogenesis inhibitors targeting VEGF (vascular endothelial growth factor) for cancer chemotherapy]
    Hideaki Kakeya
    Antibiotics Laboratory, Discovery Research Institute, RIKEN
    Nihon Rinsho 62:1264-70. 2004
    ....
  79. ncbi request reprint Heparanase as a molecular target of cancer chemotherapy
    Siro Simizu
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Wako, Saitama 351 0198, Japan
    Cancer Sci 95:553-8. 2004
    ....
  80. ncbi request reprint Improvement of transformation efficiency by strategic circumvention of restriction barriers in Streptomyces griseus
    Hirokazu Suzuki
    Chemical Biology Department, Advanced Science Institute, RIKEN, Saitama 351 0198, Japan
    J Microbiol Biotechnol 21:675-8. 2011
    ..griseus DNA, which was readily introduced into S. griseus. The results of this study raise the possibility of a promising approach to establish efficient transformation in several streptomycetes...
  81. pmc Identification of a strong binding site for kinesin on the microtubule using mutant analysis of tubulin
    Seiichi Uchimura
    Brain Development Research Group, Brain Science Institute, RIKEN, Wako, Saitama, Japan
    EMBO J 25:5932-41. 2006
    ..Our results implicate residues E410, D417, and E421 as crucial for the kinesin-microtubule interaction in the strong binding state, thereby governing the size of kinesin stall force...
  82. doi request reprint Discovery of novel antiviral agents directed against the influenza A virus nucleoprotein using photo-cross-linked chemical arrays
    Kyoji Hagiwara
    Viral Infectious Diseases Unit, RIKEN, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Biochem Biophys Res Commun 394:721-7. 2010
    ..Collectively, these results strongly suggest that chemical arrays are convenient tools for the screening of viral product inhibitors...
  83. ncbi request reprint RECK-mediated suppression of tumor cell invasion is regulated by glycosylation in human tumor cell lines
    Siro Simizu
    Antibiotics Laboratory, Discovery Research Institute, RIKEN and Graduate School of Science and Engineering, Saitama University, Japan
    Cancer Res 65:7455-61. 2005
    ..Thus, these findings indicate that glycosylation mediates RECK suppression of tumor cell invasion by multiple mechanisms such as suppressing MMP-9 secretion and inhibiting MMP-2 activation...
  84. ncbi request reprint [Biosynthesis of natural products from microbes]
    Naoki Kato
    Tanpakushitsu Kakusan Koso 52:1724-9. 2007
  85. ncbi request reprint Novel non-peptide inhibitors targeting death receptor-mediated apoptosis
    Hideaki Kakeya
    Antibiotics Laboratory, RIKEN Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Bioorg Med Chem Lett 13:3743-6. 2003
    ..Inhibitory activities of the derivatives towards death receptor-mediated apoptosis both in type I and type II cells were investigated, revealing that novel non-peptide inhibitors, RKTS-33 and RKTS-34, are effective as ECH...
  86. doi request reprint Cobtorin target analysis reveals that pectin functions in the deposition of cellulose microfibrils in parallel with cortical microtubules
    Arata Yoneda
    Biomass Engineering Program, RIKEN, 1 7 22, Suehiro cho, Tsurumi ku, Yokohama, Kanagawa 230 0045, Japan
    Plant J 64:657-67. 2010
    ..These results suggest that control over the properties of pectin is important for the deposition of cellulose microfibrils and/or the maintenance of their orientation parallel with the cortical microtubules...
  87. ncbi request reprint [Forward and reverse chemical genetics utilizing naturally occurring bioprobes]
    Naoki Kanoh
    Tanpakushitsu Kakusan Koso 50:1037-42. 2005
  88. ncbi request reprint Structure-activity relationships of epolactaene derivatives: structural requirements for inhibition of Hsp60 chaperone activity
    Yoko Nagumo
    Antibiotics Laboratory, RIKEN Discovery Research Institute, Wako, Saitama 351 0198, Japan
    Bioorg Med Chem Lett 14:4425-9. 2004
    ..We also identified the important structural framework of epolactaene/ETB (epolactaene tertiary butyl ester) for not only binding to Hsp60 but also inhibiting Hsp60 chaperone activity...
  89. doi request reprint A novel yeast cell-based screen identifies flavone as a tankyrase inhibitor
    Yoko Yashiroda
    Chemical Genomics Research Group Chemical Genetics Laboratory, RIKEN Advanced Science Institute, Wako, Saitama 351 0198, Japan
    Biochem Biophys Res Commun 394:569-73. 2010
    ..This system allows rapid identification of inhibitory activity against tankyrase 1 and is amenable to high-throughput screening using robotics...
  90. ncbi request reprint Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents
    Keisuke Ishida
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Bioorg Med Chem Lett 14:2505-9. 2004
    ..Cell growth, migration, and invasion of HT1080 cells were also inhibited by KI-111 at almost equal concentrations...
  91. ncbi request reprint [Mode of action and molecular target of ECH, a specific inhibitor of death receptor-dependent apoptosis]
    Yasunobu Miyake
    Antibiotic Laboratory, Discovery Research Institute, RIKEN
    Nihon Rinsho 62:1283-9. 2004
    ..Moreover novel non-peptide inhibitors, RKTS-33 & RKTS-34 that are chemically synthesized derivatives of ECH have been developed...
  92. ncbi request reprint A novel action of terpendole E on the motor activity of mitotic Kinesin Eg5
    Junko Nakazawa
    Antibiotics Laboratory, RIKEN Institute for Discovery Research, Hirosawa 2 1, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 10:131-7. 2003
    ..Taken together, we demonstrate that TerE is a novel Eg5 inhibitor isolated from a fungal strain...
  93. ncbi request reprint Exip, a splicing variant of p38alpha, participates in interleukin-1 receptor proximal complex and downregulates NF-kappaB pathway
    Yuki Yagasaki
    Antibiotics Laboratory and Bioarchitect Research Group, DRI, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    FEBS Lett 575:136-40. 2004
    ..Together, these results demonstrate that Exip can be a new component of NF-kappaB pathway, and contribute to a comprehensive understanding of the signal transduction pathway in the inflammatory responses...
  94. ncbi request reprint The anticancer natural product pironetin selectively targets Lys352 of alpha-tubulin
    Takeo Usui
    Antibiotics Laboratory, RIKEN Discovery Research Institute, 2 1 Hirosawa, Wako Shi, Saitama 351 0198, Japan
    Chem Biol 11:799-806. 2004
    ..This is the first compound that covalently binds to the alpha subunit of tubulin and Lys352 of alpha-tubulin and inhibits the interaction of tubulin heterodimers...
  95. ncbi request reprint Dephosphorylation of Bcl-2 by protein phosphatase 2A results in apoptosis resistance
    Siro Simizu
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Cancer Sci 95:266-70. 2004
    ..Thus, not only the expression level, but also the dephosphorylation status may have important implications for the oncogenic activity of Bcl-2...
  96. ncbi request reprint Enzymatic generation of the antimetabolite gamma,gamma-dichloroaminobutyrate by NRPS and mononuclear iron halogenase action in a streptomycete
    Masashi Ueki
    Antibiotics Laboratory, RIKEN Institute, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Chem Biol 13:1183-91. 2006
    ..This four-enzyme system analogously converts the proS-methyl group of valine to the dichloromethyl product regio- and stereospecifically...
  97. ncbi request reprint 4-isoavenaciolide covalently binds and inhibits VHR, a dual-specificity phosphatase
    Kazunori Ueda
    Antibiotics Laboratory, RIKEN, Hirosawa 2 1, Wako Shi, 351 0198, Saitama, Japan
    FEBS Lett 525:48-52. 2002
    ..These results suggest that 4-iA is a cysteine-targeting inhibitor of protein phosphatases with a common HCX5RS/T motif in the catalytic site...
  98. ncbi request reprint Biotransformation of the mycotoxin, zearalenone, to a non-estrogenic compound by a fungal strain of Clonostachys sp
    Hideaki Kakeya
    Antibiotics Laboratory, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Biosci Biotechnol Biochem 66:2723-6. 2002
    ..Moreover, cleavage product 2 did not show potent estrogenic activity like that of 1 and 17beta-estradiol in the human breast cancer MCF-7 cell proliferation assay...
  99. ncbi request reprint Nordihydroguaiaretic acid, of a new family of microtubule-stabilizing agents, shows effects differentiated from paclitaxel
    Machiko Nakamura
    Animal and Cellular Systems Laboratory, RIKEN, Institute of Physical and Chemical Research, Hirosawa 2 1, Wako Shi, Saitama 351 0198, Japan
    Biosci Biotechnol Biochem 67:151-7. 2003
    ..NDGA seemed to bind to tubulin, but did not compete for [3H]paclitaxel binding to tubulin. These observations indicate that NDGA belongs to a novel family of microtubule-stabilizing drugs...
  100. ncbi request reprint Mutational analysis of growth arrest and cellular localization of human immunodeficiency virus type 1 Vpr in the budding yeast, Saccharomyces cerevisiae
    Junko Nakazawa
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Wako, Saitama, Japan
    J Gen Appl Microbiol 51:245-56. 2005
    ..We also identified several amino acid residues, the mutation of which cancels growth inhibitory activity, and/or alters localization, both in yeast and mammalian cells, suggesting the importance of these residues for the phenotypes...
  101. ncbi request reprint Epoxycyclohexenone inhibits Fas-mediated apoptosis by blocking activation of pro-caspase-8 in the death-inducing signaling complex
    Yasunobu Miyake
    Antibiotics Laboratory, Discovery Research Institute, RIKEN, Wako Shi, Saitama 351 0198, Japan
    J Biol Chem 278:11213-20. 2003
    ..Thus, our results suggest that ECH blocks the self-activation of pro-caspase-8 in the death-inducing signaling complex and thus selectively inhibits death receptor-mediated apoptosis...