Takayoshi Kinoshita

Summary

Affiliation: Osaka Prefecture University
Country: Japan

Publications

  1. doi request reprint Crystal structure of human mono-phosphorylated ERK1 at Tyr204
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 377:1123-7. 2008
  2. ncbi request reprint Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem Lett 16:55-8. 2006
  3. ncbi request reprint Structure of human Fyn kinase domain complexed with staurosporine
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 346:840-4. 2006
  4. ncbi request reprint [Application and development of structure-based drug design using X-ray analysis]
    Takayoshi Kinoshita
    Nihon Yakurigaku Zasshi 129:186-90. 2007
  5. ncbi request reprint Structural basis of compound recognition by adenosine deaminase
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Company, Ltd, 5 2 3, Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Biochemistry 44:10562-9. 2005
  6. pmc Tris(hydroxymethyl)aminomethane induces conformational change and crystal-packing contraction of porcine pancreatic elastase
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 62:623-6. 2006
  7. doi request reprint Conformational change of adenosine deaminase during ligand-exchange in a crystal
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 373:53-7. 2008
  8. ncbi request reprint Knowledge-based identification of the ERK2/STAT3 signal pathway as a therapeutic target for type 2 diabetes and drug discovery
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Chem Biol Drug Des 78:471-6. 2011
  9. doi request reprint A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Mol Cell Biochem 356:97-105. 2011
  10. doi request reprint Protein purification and preliminary crystallographic analysis of human Lyn tyrosine kinase
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Protein Expr Purif 58:318-24. 2008

Collaborators

Detail Information

Publications52

  1. doi request reprint Crystal structure of human mono-phosphorylated ERK1 at Tyr204
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 377:1123-7. 2008
    ..The structural dissection of ERK1 compared to ERK2 suggests that the structural differences in the D-motif binding site and in the backside binding site are putative targets for development of selective ERK1/ERK2 inhibitors...
  2. ncbi request reprint Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem Lett 16:55-8. 2006
    ..The compound induces structural change including movement of the glycine-rich loop and peptide flip between Met108-Glu109. As a result, the newly formed subsite can recognize small hydrophobic substituents but not hydrophilic ones...
  3. ncbi request reprint Structure of human Fyn kinase domain complexed with staurosporine
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 346:840-4. 2006
    ..The small structural differences in the staurosporine-binding and/or -unbinding region among the three kinase domains may help obtaining the selective inhibitors against the respective kinases...
  4. ncbi request reprint [Application and development of structure-based drug design using X-ray analysis]
    Takayoshi Kinoshita
    Nihon Yakurigaku Zasshi 129:186-90. 2007
  5. ncbi request reprint Structural basis of compound recognition by adenosine deaminase
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Company, Ltd, 5 2 3, Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Biochemistry 44:10562-9. 2005
    ..On the other hand, while occupied, the overall conformation remains in the open form. This structural understanding should greatly assist structure-oriented drug design and enable control of the enzymatic activity...
  6. pmc Tris(hydroxymethyl)aminomethane induces conformational change and crystal-packing contraction of porcine pancreatic elastase
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 62:623-6. 2006
    ..The fact that Tris and these four regions make a diagonal line in the ac plane may have affected the crystal-packing contraction along the a and c axes in the crystal compared with the typical crystal...
  7. doi request reprint Conformational change of adenosine deaminase during ligand-exchange in a crystal
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Biochem Biophys Res Commun 373:53-7. 2008
    ..The crystal structure shows that EHNA binds to the open form through a novel recognition of the adenine base accompanying conformational change from the closed form of the PR-ADA complex in crystalline state...
  8. ncbi request reprint Knowledge-based identification of the ERK2/STAT3 signal pathway as a therapeutic target for type 2 diabetes and drug discovery
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Chem Biol Drug Des 78:471-6. 2011
    ..Besides lowering the fasting blood glucose level, the peptide inhibitor also attenuated the blood glucose increment in the fed state, as compared with the vehicle group...
  9. doi request reprint A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Mol Cell Biochem 356:97-105. 2011
    ..These structural insights, in combination with thermodynamic and computational observations, should be helpful in developing potent and selective CK2α inhibitors...
  10. doi request reprint Protein purification and preliminary crystallographic analysis of human Lyn tyrosine kinase
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Gakuencho 1 1, Sakai, Osaka 599 8531, Japan
    Protein Expr Purif 58:318-24. 2008
    ..2A with synchrotron source at Photon Factory and a complete X-ray diffraction data set was collected. The coarse structure was solved by a molecular replacement method and further structural refinement is currently underway...
  11. ncbi request reprint Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism
    Tadashi Terasaka
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6, Kashima, Yodogawa ku, Osaka 532 8514, Japan
    J Med Chem 48:4750-3. 2005
    ..They demonstrated in vivo efficacy in models of inflammation and lymphoma. Furthermore, X-ray crystal structure analysis has revealed a novel induced fit to ADA...
  12. ncbi request reprint Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling
    Junya Ishida
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co Ltd, Tsukuba, Ibaraki, Japan
    Bioorg Med Chem 14:1378-90. 2006
    ..These findings provide a new structural framework for the design of selective inhibitors for PARP-1 and PARP-2...
  13. ncbi request reprint Anti-inflammatory activity of non-nucleoside adenosine deaminase inhibitor FR234938
    Masako Kuno
    Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6 Kashima, Yodogawa ku, Osaka 532 8514, Japan
    Eur J Pharmacol 534:241-9. 2006
    ..Non-nucleoside adenosine deaminase inhibitor FR234938 has good potential as a new type of anti-rheumatic and anti-inflammatory drug, by modulating host-defense concentrations of adenosine...
  14. ncbi request reprint Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitors
    Akinori Iwashita
    Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6 Kashima, Osaka 532 8514, Japan
    FEBS Lett 579:1389-93. 2005
    ..These findings provide a new structural framework for the design of selective inhibitors for PARP-1 and PARP-2...
  15. doi request reprint Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid
    Yusuke Sekiguchi
    Graduate School of Science, Osaka Prefecture University, Sakai, Osaka, Japan
    Bioorg Med Chem Lett 19:2920-3. 2009
    ..The inhibitor binds to CK2alpha with a novel binding mode, including water-mediated hydrogen bonds. This structural information may support discovery of potent CK2 inhibitors...
  16. pmc Structure of human protein kinase CK2 alpha 2 with a potent indazole-derivative inhibitor
    Tetsuko Nakaniwa
    Graduate School of Sciences, Osaka Prefecture University, Osaka 599 8530, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 65:75-9. 2009
    ..Thus, the CK2alpha-CK2beta interface is a likely target candidate for the production of selective CK2alpha1 inhibitors...
  17. pmc Structure of apo-glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942
    Tomoya Kitatani
    Department of Applied Biochemistry, Graduate School of Agriculture and Life Sciences, Osaka Prefecture University, 1 1 Gakuen cho, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 62:727-30. 2006
    ..A structural comparison with holo-GAPDHs indicated that the S-loop fixation is essential in the discrimination of NADP and NAD molecules...
  18. doi request reprint Structural basis for the inhibitor recognition of human Lyn kinase domain
    Nao Miyano
    Graduate School of Science, Osaka Prefecture University, Sakai, Osaka 599 8531, Japan
    Bioorg Med Chem Lett 19:6557-60. 2009
    ..The remarkable structural features of the staurosporine-binding region will offer valuable structural insights for the structure-based design of novel Lyn-selective inhibitors...
  19. ncbi request reprint Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors
    Tadashi Terasaka
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6 Kashima, Yodogawa ku, Osaka 532 8514, Japan
    Bioorg Med Chem Lett 13:1115-8. 2003
    ..9 microM to human ADA) as a novel inhibitor with moderate activity and good pharmacokinetics compared with the known inhibitors pentostatin and EHNA...
  20. pmc Crystal structure of human CK2α at 1.06 Å resolution
    Takayoshi Kinoshita
    Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    J Synchrotron Radiat 20:974-9. 2013
    ..Together with water molecules in the active site, these structural insights should facilitate drug discovery...
  21. ncbi request reprint Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase
    Kouji Hattori
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6 Kashima, Yodogawa ku, Osaka 532 8514, Japan kouji_hattori po fujisawa co jp
    J Med Chem 47:4151-4. 2004
    ..The new inhibitors were shown to bind to the nicotinamide-ribose binding site (NI site) and the adenosine-ribose binding site (AD site) of NAD+...
  22. ncbi request reprint Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex
    Makoto Ohori
    Lead Discovery Research Laboratories, Astellas Pharma Inc, Miyukigaoka 21, Tsukuba, Ibaraki 305 8585, Japan
    Biochem Biophys Res Commun 336:357-63. 2005
    ..These results suggest that FR180204 is an ERK-selective and cell-permeable inhibitor, and could be useful for elucidating the roles of ERK as well as for drug development...
  23. pmc Structure of NADP-dependent glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942 complexed with NADP
    Tomoya Kitatani
    Department of Applied Biochemistry, Graduate School of Agriculture and Life Sciences, Osaka Prefecture University, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 62:315-9. 2006
    ....
  24. ncbi request reprint A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization
    Tadashi Terasaka
    Medicinal Chemistry Research Laboratories, Basic Research Laboratories, and Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6, Kashima, Yodogawa ku, Osaka 532 8514, Japan
    J Am Chem Soc 126:34-5. 2004
    ..The conceptual approach illustrated by this example promises to be broadly useful in the search for new chemical entities and can contribute greatly to improve the overall efficiency and speed of drug discovery...
  25. ncbi request reprint Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors
    Tadashi Terasaka
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6, Kashima, Yodogawa ku, Osaka 532 8514, Japan
    J Med Chem 47:2728-31. 2004
    ..8 nM, BA = 42%)]. 6 demonstrated in vivo efficacy in models of inflammation and lymphoma...
  26. doi request reprint Seven cysteine-deficient mutants depict the interplay between thermal and chemical stabilities of individual cysteine residues in mitogen-activated protein kinase c-Jun N-terminal kinase 1
    Tetsuko Nakaniwa
    Department of Biological Sciences, Graduate School of Science, Osaka University, Toyonaka, Japan
    Biochemistry 51:8410-21. 2012
    ..These findings about the role of cysteine residues should allow us to obtain a stable JNK1 and thus promote the discovery of potent JNK1 inhibitors...
  27. ncbi request reprint Structure of bovine adenosine deaminase complexed with 6-hydroxy-1,6-dihydropurine riboside
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 59:299-303. 2003
    ..A weak interaction, similar to CH-pi binding, might make it possible to open the lid. Taking account of the movement and observation of this structural feature, the aim is to design novel ADA inhibitors...
  28. ncbi request reprint Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors
    Tadashi Terasaka
    Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 2 1 6, Kashima, Yodogawa ku, Osaka 532 8514, Japan
    J Med Chem 47:3730-43. 2004
    ....
  29. doi request reprint High-resolution structure of exo-arabinanase from Penicillium chrysogenum
    Yuri Sogabe
    Graduate School of Science, Osaka Prefecture University, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr D Biol Crystallogr 67:415-22. 2011
    ..A comparison with the related enzyme Arb93A which has a quite similar overall structure suggested that Abnx has different mechanisms to funnel substrates to the active site and/or to stabilize the transition state...
  30. ncbi request reprint Improving quality and harvest period of protein crystals for structure-based drug design: effects of a gel and a magnetic field on bovine adenosine deaminase crystals
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 59:1333-5. 2003
    ..Furthermore, the harvest period for crystal growth in a magnetic field was much shorter than that with agarose gel...
  31. ncbi request reprint Role of a cysteine residue in the active site of ERK and the MAPKK family
    Makoto Ohori
    Astellas Pharma Inc, Tokodai 5 2 3, Tsukuba, Ibaraki 300 2698, Japan
    Biochem Biophys Res Commun 353:633-7. 2007
    ..These findings on the molecular recognition mechanisms of FR148083 for kinases with Cys166 should provide a novel strategy for the pharmacological intervention of MAPK cascades...
  32. pmc Structure of the complex of porcine pancreatic elastase with a trimacrocyclic peptide inhibitor FR901451
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 61:808-11. 2005
    ..Structural comparison of PPE with human leukocyte elastase (HLE) implies that the inhibitor binds to HLE in a similar manner to the FR901451-PPE complex. This structural insight may help in the design of potent elastase inhibitors...
  33. pmc Structure of a high-resolution crystal form of human triosephosphate isomerase: improvement of crystals using the gel-tube method
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 61:346-9. 2005
    ..2 A resolution. Crystal form 2 contained a homodimer in the asymmetric unit, which was biologically essential. Its overall structure was similar to that of 1hti except for the flexible loop, which was located at the active centre Lys13...
  34. ncbi request reprint Expression, purification, crystallization and preliminary X-ray diffraction studies of human liver regucalcin
    Masaichi Warizaya
    Exploratory Research Laboratory, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 60:2019-21. 2004
    ..38 A, beta = 99.86 degrees . Two molecules most probably exist in the asymmetric unit, corresponding to V(M) = 2.2 A(3) Da(-1). Heavy-atom derivative data were collected and the Pb derivative showed one high-occupancy site per molecule...
  35. ncbi request reprint True interaction mode of porcine pancreatic elastase with FR136706, a potent peptidyl inhibitor
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3, Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem Lett 13:21-4. 2003
    ..This novel interaction mode may lead to design of new types of inhibitors...
  36. ncbi request reprint Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3, Tokodai, Tsukuba, 300 2698, Ibaraki, Japan
    FEBS Lett 556:43-6. 2004
    ..Consequently, a corn-shaped hydrophobic subsite, which consists of the side chains of Leu769, Ile879, Pro881, and the methylene chain of Arg878, newly emerges from the well-known active site...
  37. ncbi request reprint Cloning, expression, purification, crystallization and preliminary X-ray analysis of human liver glyceraldehyde-3-phosphate dehydrogenase
    Masaichi Warizaya
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 60:567-8. 2004
    ..It is planned to crystallize human liver GAPDH in the presence of phosphate ions and/or some kind of inhibitor in order to fix the flexible region...
  38. ncbi request reprint A silent mutation made possible efficient production of active human Frk tyrosine kinase in Escherichia coli
    Xiaoyan Yang
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Sakai, Osaka, Japan
    Biosci Biotechnol Biochem 74:125-8. 2010
    ..This result of active protein production should promote drug discovery studies, including highthrough-put screening and structure-based drug design...
  39. ncbi request reprint The novel gluconeogenesis inhibitor FR225654 that originates from Phoma sp. no. 00144. III. Structure determination
    Yoshihiro Ohtsu
    Fermentation Research Laboratories, Fujisawa Pharmaceutical Co, Ltd
    J Antibiot (Tokyo) 58:479-82. 2005
    ..00144. Spectroscopic analysis concluded that FR225654 has a highly oxygenated trans-decalin ring and beta-keto-enol in its main part, and has a characteristic side chain possessing a conjugated carboxylic acid and tri-substituted olefin...
  40. ncbi request reprint FR207944, an antifungal antibiotic from Chaetomium sp. No. 217 II. Isolation and structure elucidation
    Motoo Kobayashi
    Fermentation Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, Tokyo, Japan
    Biosci Biotechnol Biochem 69:1029-32. 2005
    ..Determination of the relative stereochemistry of fuscoatroside was made formally by comparison with WF11605 (16-Oxo-FR207944). We confirmed the stereochemistry on the basis of single crystal X-ray analysis...
  41. pmc Crystallization of porcine pancreatic elastase and a preliminary neutron diffraction experiment
    Takayoshi Kinoshita
    Department of Biological Science, Graduate School of Science, Osaka Prefecture University, 1 1 Gakuen cho, Naka ku, Sakai, Osaka 599 8531, Japan
    Acta Crystallogr Sect F Struct Biol Cryst Commun 63:315-7. 2007
    ..The data set was integrated and scaled to 2.3 A resolution in space group P2(1)2(1)2(1), with unit-cell parameters a = 51.2, b = 57.8, c = 75.6 A...
  42. ncbi request reprint Cloning, expression, purification, crystallization and preliminary diffraction analysis of the C-terminal catalytic domain of human poly(ADP-ribose) polymerase
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 60:109-11. 2004
    ..Gly-Ser-catPARP was found to be more suitable for X-ray crystallography and crystals showed diffraction to at least 3.5 A resolution...
  43. doi request reprint Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state
    Takashi Matsumoto
    PharmAxess, Inc, 3 9 12, Matsubara cho, Akishima, Tokyo 196 8666, Japan
    J Biochem 151:541-9. 2012
    ..AH1 and AH2 were found to enclose the γ-phosphate, the leaving group of ATP. A comparison with the related enzymes, MAP2K1 and MAP2K4 reveals that MAP2K6 has the unique auto-inhibition mechanism mediated by the three activation helices...
  44. ncbi request reprint Crystallization and preliminary X-ray diffraction studies of catalase-peroxidase from Synechococcus PCC 7942
    Kei Wada
    Research Institute for Advanced Science and Technology, Osaka Prefecture University, Sakai, Osaka 599 8570, Japan
    Acta Crystallogr D Biol Crystallogr 58:157-9. 2002
    ..3, c = 202.0 A. The calculated V(M) value based on a dimer in the asymmetric unit was 1.9 A(3) Da(-1). A native data set was collected to 2.3 A resolution from a frozen crystal using synchrotron radiation at SPring-8...
  45. ncbi request reprint FR177391, a new anti-hyperlipidemic agent from Serratia. I. Taxonomy, fermentation, isolation, physico-chemical properties, structure elucidation and biological activities
    Bunji Sato
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, Tsukuba, Ibaraki, Japan
    J Antibiot (Tokyo) 58:634-9. 2005
    ..Structural elucidation by spectroscopic methods and X-ray crystallographic analysis of its propylamide derivative revealed that FR177391 was a chlorinated macrocyclic lactone...
  46. ncbi request reprint The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat
    Takayoshi Kinoshita
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 5 2 3, Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Acta Crystallogr D Biol Crystallogr 58:622-6. 2002
    ..Such structural information is key to understanding the mode of action of this class of inhibitors and for rational design of better therapeutics...
  47. ncbi request reprint FR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase III. Structure determination
    Hiroaki Mori
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 5 2 3, Tokodai, Tsukuba 300 2698, Japan
    J Antibiot (Tokyo) 56:181-5. 2003
  48. ncbi request reprint Solution stirring initiates nucleation and improves the quality of adenosine deaminase crystals
    Hiroaki Adachi
    Department of Electrical Engineering, Osaka University, 2 1 Yamadaoka, Suita, Osaka 565 0871, Japan
    Acta Crystallogr D Biol Crystallogr 61:759-62. 2005
    ..The results reported here indicate that the solution-stirring technique promotes nucleation and improves the quality of protein crystals...
  49. ncbi request reprint Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-S(N)2' reactions
    Akira Otaka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    J Org Chem 67:6152-61. 2002
    ..The present synthetic methodology affords trans-Xaa-Pro alkene-type dipeptide isosteres in high yield with relatively simple manipulation...
  50. ncbi request reprint SmI2-mediated reduction of gamma,gamma-difluoro-alpha,beta-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipeptide isosteres
    Akira Otaka
    Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    J Org Chem 69:1634-45. 2004
    ....
  51. ncbi request reprint Solution-stirring method improves crystal quality of human triosephosphate isomerase
    Hiroaki Adachi
    SOSHO Project Crystal Design Project, Osaka University, 2 1 Yamadaoka, Suita, Osaka 565 0871, Japan
    J Biosci Bioeng 101:83-6. 2006
    ..8 A. These results clearly show that the solution-stirring method is valuable and useful for protein crystallization because of its effectiveness and simplicity...
  52. ncbi request reprint [New progress in crystallization technology of membrane protein and introduction of pharamaceutical innovation value chain]
    Tsuyoshi Inoue
    Graduate School of Engineering Osaka University, Yamada oka, Suita City, Japan
    Yakugaku Zasshi 128:497-505. 2008
    ..In this paper, we report the recent research work on the crystallization of membrane proteins and the development of a method for in silico drug discovery...