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135 related items for PubMed ID: 9622548

  • 1. Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.
    Bone R, Lu T, Illig CR, Soll RM, Spurlino JC.
    J Med Chem; 1998 Jun 04; 41(12):2068-75. PubMed ID: 9622548
    [Abstract] [Full Text] [Related]

  • 2. The crystal structures of human alpha-thrombin complexed with active site-directed diamino benzo[b]thiophene derivatives: a binding mode for a structurally novel class of inhibitors.
    Chirgadze NY, Sall DJ, Briggs SL, Clawson DK, Zhang M, Smith GF, Schevitz RW.
    Protein Sci; 2000 Jan 04; 9(1):29-36. PubMed ID: 10739244
    [Abstract] [Full Text] [Related]

  • 3. Think twice: understanding the high potency of bis(phenyl)methane inhibitors of thrombin.
    Baum B, Muley L, Heine A, Smolinski M, Hangauer D, Klebe G.
    J Mol Biol; 2009 Aug 21; 391(3):552-64. PubMed ID: 19520086
    [Abstract] [Full Text] [Related]

  • 4. In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
    Costanzo MJ, Almond HR, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.
    J Med Chem; 2005 Mar 24; 48(6):1984-2008. PubMed ID: 15771442
    [Abstract] [Full Text] [Related]

  • 5. Hirunorms are true hirudin mimetics. The crystal structure of human alpha-thrombin-hirunorm V complex.
    De Simone G, Lombardi A, Galdiero S, Nastri F, Della Morte R, Staiano N, Pedone C, Bolognesi M, Pavone V.
    Protein Sci; 1998 Feb 24; 7(2):243-53. PubMed ID: 9521099
    [Abstract] [Full Text] [Related]

  • 6. A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.
    Katz BA, Elrod K, Luong C, Rice MJ, Mackman RL, Sprengeler PA, Spencer J, Hataye J, Janc J, Link J, Litvak J, Rai R, Rice K, Sideris S, Verner E, Young W.
    J Mol Biol; 2001 Apr 13; 307(5):1451-86. PubMed ID: 11292354
    [Abstract] [Full Text] [Related]

  • 7. Human alpha-thrombin inhibition by the active site titrant N alpha-(N,N-dimethylcarbamoyl)-alpha-azalysine p-nitrophenyl ester: a comparative kinetic and X-ray crystallographic study.
    Nardini M, Pesce A, Rizzi M, Casale E, Ferraccioli R, Balliano G, Milla P, Ascenzi P, Bolognesi M.
    J Mol Biol; 1996 May 24; 258(5):851-9. PubMed ID: 8637015
    [Abstract] [Full Text] [Related]

  • 8. The methyl group of N(alpha)(Me)Arg-containing peptides disturbs the active-site geometry of thrombin, impairing efficient cleavage.
    Friedrich R, Steinmetzer T, Huber R, Stürzebecher J, Bode W.
    J Mol Biol; 2002 Mar 01; 316(4):869-74. PubMed ID: 11884127
    [Abstract] [Full Text] [Related]

  • 9. Crystal structure of the complex of human alpha-thrombin and nonhydrolyzable bifunctional inhibitors, hirutonin-2 and hirutonin-6.
    Zdanov A, Wu S, DiMaio J, Konishi Y, Li Y, Wu X, Edwards BF, Martin PD, Cygler M.
    Proteins; 1993 Nov 01; 17(3):252-65. PubMed ID: 8272424
    [Abstract] [Full Text] [Related]

  • 10. Novel non-covalent thrombin inhibitors incorporating P(1) 4,5,6,7-tetrahydrobenzothiazole arginine side chain mimetics.
    Marinko P, Krbavcic A, Mlinsek G, Solmajer T, Bakija AT, Stegnar M, Stojan J, Kikelj D.
    Eur J Med Chem; 2004 Mar 01; 39(3):257-65. PubMed ID: 15051174
    [Abstract] [Full Text] [Related]

  • 11. Design of weakly basic thrombin inhibitors incorporating novel P1 binding functions: molecular and X-ray crystallographic studies.
    De Simone G, Menchise V, Omaggio S, Pedone C, Scozzafava A, Supuran CT.
    Biochemistry; 2003 Aug 05; 42(30):9013-21. PubMed ID: 12885234
    [Abstract] [Full Text] [Related]

  • 12. Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.
    Tucker TJ, Lumma WC, Mulichak AM, Chen Z, Naylor-Olsen AM, Lewis SD, Lucas R, Freidinger RM, Kuo LC.
    J Med Chem; 1997 Mar 14; 40(6):830-2. PubMed ID: 9083470
    [No Abstract] [Full Text] [Related]

  • 13. Crystal structures of thrombin with thiazole-containing inhibitors: probes of the S1' binding site.
    Matthews JH, Krishnan R, Costanzo MJ, Maryanoff BE, Tulinsky A.
    Biophys J; 1996 Nov 14; 71(5):2830-9. PubMed ID: 8913620
    [Abstract] [Full Text] [Related]

  • 14. The crystal structure of human alpha-thrombin complexed with LY178550, a nonpeptidyl, active site-directed inhibitor.
    Chirgadze NY, Sall DJ, Klimkowski VJ, Clawson DK, Briggs SL, Hermann R, Smith GF, Gifford-Moore DS, Wery JP.
    Protein Sci; 1997 Jul 14; 6(7):1412-7. PubMed ID: 9232642
    [Abstract] [Full Text] [Related]

  • 15. Highly selective mechanism-based thrombin inhibitors: structures of thrombin and trypsin inhibited with rigid peptidyl aldehydes.
    Krishnan R, Zhang E, Hakansson K, Arni RK, Tulinsky A, Lim-Wilby MS, Levy OE, Semple JE, Brunck TK.
    Biochemistry; 1998 Sep 01; 37(35):12094-103. PubMed ID: 9724521
    [Abstract] [Full Text] [Related]

  • 16. Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
    Boatman PD, Ogbu CO, Eguchi M, Kim HO, Nakanishi H, Cao B, Shea JP, Kahn M.
    J Med Chem; 1999 Apr 22; 42(8):1367-75. PubMed ID: 10212122
    [Abstract] [Full Text] [Related]

  • 17. Design and synthesis of novel biologically active thrombin receptor non-peptide mimetics based on the pharmacophoric cluster Phe/Arg/NH2 of the Ser42-Phe-Leu-Leu-Arg46 motif sequence: platelet aggregation and relaxant activities.
    Alexopoulos K, Fatseas P, Melissari E, Vlahakos D, Roumelioti P, Mavromoustakos T, Mihailescu S, Paredes-Carbajal MC, Mascher D, Matsoukas J.
    J Med Chem; 2004 Jun 17; 47(13):3338-52. PubMed ID: 15189031
    [Abstract] [Full Text] [Related]

  • 18. Crystallographic determination of the structures of human alpha-thrombin complexed with BMS-186282 and BMS-189090.
    Malley MF, Tabernero L, Chang CY, Ohringer SL, Roberts DG, Das J, Sack JS.
    Protein Sci; 1996 Feb 17; 5(2):221-8. PubMed ID: 8745399
    [Abstract] [Full Text] [Related]

  • 19. Bovine thrombin complexed with an uncleavable analog of residues 7-19 of fibrinogen A alpha: geometry of the catalytic triad and interactions of the P1', P2', and P3' substrate residues.
    Martin PD, Malkowski MG, DiMaio J, Konishi Y, Ni F, Edwards BF.
    Biochemistry; 1996 Oct 08; 35(40):13030-9. PubMed ID: 8855938
    [Abstract] [Full Text] [Related]

  • 20. Human alpha-thrombin inhibition by the highly selective compounds N-ethoxycarbonyl-D-Phe-Pro-alpha-azaLys p-nitrophenyl ester and N-carbobenzoxy-Pro-alpha-azaLys p-nitrophenyl ester: a kinetic, thermodynamic and X-ray crystallographic study.
    De Simone G, Balliano G, Milla P, Gallina C, Giordano C, Tarricone C, Rizzi M, Bolognesi M, Ascenzi P.
    J Mol Biol; 1997 Jun 20; 269(4):558-69. PubMed ID: 9217260
    [Abstract] [Full Text] [Related]

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