Research Topics
Genomes and Genes | Takayoshi KinoshitaSummaryAffiliation: Osaka Prefecture University Country: Japan Publications
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Publications
A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinaseTakayoshi 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...
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivativeTakayoshi 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...- Structure of human Fyn kinase domain complexed with staurosporineTakayoshi 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... 
Tris(hydroxymethyl)aminomethane induces conformational change and crystal-packing contraction of porcine pancreatic elastaseTakayoshi 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...- [Application and development of structure-based drug design using X-ray analysis]Takayoshi Kinoshita
Nippon Yakurigaku Zasshi 129:186-90. 2007 - Protein purification and preliminary crystallographic analysis of human Lyn tyrosine kinaseTakayoshi 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... - Conformational change of adenosine deaminase during ligand-exchange in a crystalTakayoshi 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... - Structural basis of compound recognition by adenosine deaminaseTakayoshi 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... - Knowledge-based identification of the ERK2/STAT3 signal pathway as a therapeutic target for type 2 diabetes and drug discoveryTakayoshi 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... - Crystal structure of human mono-phosphorylated ERK1 at Tyr204Takayoshi 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... - Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolismTadashi 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... - Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modelingJunya 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... - Anti-inflammatory activity of non-nucleoside adenosine deaminase inhibitor FR234938Masako 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... - Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitorsAkinori 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... - Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acidYusuke 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... - Structure of apo-glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942Tomoya 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... - Structure of human protein kinase CK2 alpha 2 with a potent indazole-derivative inhibitorTetsuko 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... - Structural basis for the inhibitor recognition of human Lyn kinase domainNao 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... - Structure-based de novo design of non-nucleoside adenosine deaminase inhibitorsTadashi 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... - Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymeraseKouji 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+... - Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complexMakoto 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... - Structure of NADP-dependent glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942 complexed with NADPTomoya 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.... - A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridizationTadashi 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... - Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitorsTadashi 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... - 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 1Tetsuko 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... - Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitorsTadashi 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.... - Structure of bovine adenosine deaminase complexed with 6-hydroxy-1,6-dihydropurine ribosideTakayoshi 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... - Structure of the complex of porcine pancreatic elastase with a trimacrocyclic peptide inhibitor FR901451Takayoshi 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... - High-resolution structure of exo-arabinanase from Penicillium chrysogenumYuri 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... - Role of a cysteine residue in the active site of ERK and the MAPKK familyMakoto 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... - 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 crystalsTakayoshi 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... - True interaction mode of porcine pancreatic elastase with FR136706, a potent peptidyl inhibitorTakayoshi 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... - Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymeraseTakayoshi 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... - Expression, purification, crystallization and preliminary X-ray diffraction studies of human liver regucalcinMasaichi 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... - Structure of a high-resolution crystal form of human triosephosphate isomerase: improvement of crystals using the gel-tube methodTakayoshi 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... - Cloning, expression, purification, crystallization and preliminary X-ray analysis of human liver glyceraldehyde-3-phosphate dehydrogenaseMasaichi 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... - The novel gluconeogenesis inhibitor FR225654 that originates from Phoma sp. no. 00144. III. Structure determinationYoshihiro 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... - A silent mutation made possible efficient production of active human Frk tyrosine kinase in Escherichia coliXiaoyan 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... - FR207944, an antifungal antibiotic from Chaetomium sp. No. 217 II. Isolation and structure elucidationMotoo 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... - Crystallization of porcine pancreatic elastase and a preliminary neutron diffraction experimentTakayoshi 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... - Cloning, expression, purification, crystallization and preliminary diffraction analysis of the C-terminal catalytic domain of human poly(ADP-ribose) polymeraseTakayoshi 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... - Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition stateTakashi 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... - FR177391, a new anti-hyperlipidemic agent from Serratia. I. Taxonomy, fermentation, isolation, physico-chemical properties, structure elucidation and biological activitiesBunji 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... - Crystallization and preliminary X-ray diffraction studies of catalase-peroxidase from Synechococcus PCC 7942Kei 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... - The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestatTakayoshi 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... - FR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase III. Structure determinationHiroaki Mori
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, 5-2-3, Tokodai, Tsukuba 300-2698, Japan
J Antibiot (Tokyo) 56:181-5. 2003 - Solution stirring initiates nucleation and improves the quality of adenosine deaminase crystalsHiroaki 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... - [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... - Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-S(N)2' reactionsAkira 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... - Solution-stirring method improves crystal quality of human triosephosphate isomeraseHiroaki 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... - SmI2-mediated reduction of gamma,gamma-difluoro-alpha,beta-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipeptide isosteresAkira Otaka
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
J Org Chem 69:1634-45. 2004....