-
1
-
-
0025837452
-
Crystallographic analysis at 3.0 Å resolution of the binding to human thrombin of four active site-directed inhibitors
-
Banner DW, Hadvary P. 1991. Crystallographic analysis at 3.0 Å resolution of the binding to human thrombin of four active site-directed inhibitors. J Biol Chem 226:20085-20093.
-
(1991)
J Biol Chem
, vol.226
, pp. 20085-20093
-
-
Banner, D.W.1
Hadvary, P.2
-
2
-
-
0342800306
-
Thrombotic processes in cerebrovascular disease
-
Barnett HJM. 1991. Thrombotic processes in cerebrovascular disease. J Biol Chem 226:1301-1315.
-
(1991)
J Biol Chem
, vol.226
, pp. 1301-1315
-
-
Barnett, H.J.M.1
-
4
-
-
0024431034
-
The refined 1.9 A crystal structure of human α-thrombin: Interaction with D-Phe-Pro-Arg chloromethylketone and significance of the Tyr-Pro-Pro-Trp insertion segment
-
Bode W, Mayr I, Baumann U, Huber R, Stone S, Hoffsteenge J. 1989. The refined 1.9 A crystal structure of human α-thrombin: Interaction with D-Phe-Pro-Arg chloromethylketone and significance of the Tyr-Pro-Pro-Trp insertion segment. EMBO J 8:3467-3475.
-
(1989)
EMBO J
, vol.8
, pp. 3467-3475
-
-
Bode, W.1
Mayr, I.2
Baumann, U.3
Huber, R.4
Stone, S.5
Hoffsteenge, J.6
-
5
-
-
0027050807
-
The refined 1.9 Å X-ray crystal structure of D-Phe-Pro-Arg chlormethylkethone-inhibited human α-thrombin: Structure analysis, overall structure, electrostatic properties. Detailed active site geometry and structure-function relationships
-
Bode W, Turk D, Karshikov A. 1992. The refined 1.9 Å X-ray crystal structure of D-Phe-Pro-Arg chlormethylkethone-inhibited human α-thrombin: Structure analysis, overall structure, electrostatic properties. Detailed active site geometry and structure-function relationships. Protein Sci 1:426-471.
-
(1992)
Protein Sci
, vol.1
, pp. 426-471
-
-
Bode, W.1
Turk, D.2
Karshikov, A.3
-
7
-
-
0013631261
-
The X-ray structure at 2.2 Å of a ternary complex containing human α-thrombin, a hirudin peptide (54-65) and an active site inhibitor
-
Pittsburgh, Pennsylvania, August 9-14
-
Chirgadze NY, Clawson DK, Gesellchen PD, Hermann RB, Kaiser RE Jr, Olkowski JL, Sall DJ, Schevitz RW, Smith GF, Shuman RT, et al. 1992. The X-ray structure at 2.2 Å of a ternary complex containing human α-thrombin, a hirudin peptide (54-65) and an active site inhibitor. American Crystallographic Association meeting, Pittsburgh, Pennsylvania, August 9-14, Vol. 20. p 116.
-
(1992)
American Crystallographic Association Meeting
, vol.20
, pp. 116
-
-
Chirgadze, N.Y.1
Clawson, D.K.2
Gesellchen, P.D.3
Hermann, R.B.4
Kaiser R.E., Jr.5
Olkowski, J.L.6
Sall, D.J.7
Schevitz, R.W.8
Smith, G.F.9
Shuman, R.T.10
-
8
-
-
0030835791
-
The crystal structure of human α-thrombin complexed with LY178550, a non-peptidyl, active-site directed inhibitor
-
Chirgadze NY, Sall DJ, Klimkowski VJ, Clawson DK, Briggs SL, Hermann R, Smith GF, Gifford-Moore DS, Wery J-P. 1997. The crystal structure of human α-thrombin complexed with LY178550, a non-peptidyl, active-site directed inhibitor. Protein Sci 6:1412-1417.
-
(1997)
Protein Sci
, vol.6
, pp. 1412-1417
-
-
Chirgadze, N.Y.1
Sall, D.J.2
Klimkowski, V.J.3
Clawson, D.K.4
Briggs, S.L.5
Hermann, R.6
Smith, G.F.7
Gifford-Moore, D.S.8
Wery, J.-P.9
-
9
-
-
0343307745
-
Structure based design of human α-thrombin active site inhibitors: Interaction in the insertion loop region
-
Erice, Italy, May 9-19
-
Chirgadze NY, Wiley MR, Schacht AL, Shuman RT, Smith GF, Sall DL, Clawson DK, Hermann RB, Schevitz RW, Jones ND, et al. 1996. Structure based design of human α-thrombin active site inhibitors: Interaction in the insertion loop region. Experimental and computational approaches to structure-based drug design, Erice, Italy, May 9-19. p 420.
-
(1996)
Experimental and Computational Approaches to Structure-based Drug Design
, pp. 420
-
-
Chirgadze, N.Y.1
Wiley, M.R.2
Schacht, A.L.3
Shuman, R.T.4
Smith, G.F.5
Sall, D.L.6
Clawson, D.K.7
Hermann, R.B.8
Schevitz, R.W.9
Jones, N.D.10
-
10
-
-
0001965683
-
Mechanisms of platelet aggregation
-
Colman RW, Hirsh J, Marder, VJ, Salzman EW, eds. Philadelphia, Pennsylvania: J.B. Lippincott Co.
-
Colman RW, Cook JJ, Niewiarowski S. 1994a. Mechanisms of platelet aggregation. In: Colman RW, Hirsh J, Marder, VJ, Salzman EW, eds. Hemostasis and thrombosis: Basic principles and clinical practice, 3rd ed. Philadelphia, Pennsylvania: J.B. Lippincott Co. pp 508-523.
-
(1994)
Hemostasis and Thrombosis: Basic Principles and Clinical Practice, 3rd Ed.
, pp. 508-523
-
-
Colman, R.W.1
Cook, J.J.2
Niewiarowski, S.3
-
11
-
-
0002613087
-
Overview of hemostasis
-
Colman RW, Hirsh J, Marder VJ, Salzman EW, eds. Philadelphia, Pennsylvania: J.B. Lippincott Co.
-
Colman RW, Marder VJ, Salzman EW, Hirsh J. 1994b. Overview of hemostasis. In: Colman RW, Hirsh J, Marder VJ, Salzman EW, eds. Hemostasis and thrombosis: Basic principles and clinical practice, 3rd ed. Philadelphia, Pennsylvania: J.B. Lippincott Co. pp 3-18.
-
(1994)
Hemostasis and Thrombosis: Basic Principles and Clinical Practice, 3rd Ed.
, pp. 3-18
-
-
Colman, R.W.1
Marder, V.J.2
Salzman, E.W.3
Hirsh, J.4
-
12
-
-
0030043489
-
Cation-π interactions in chemistry and biology: A new view of benzene, Phe, Tyr, and Trp
-
Dougherty D. 1996 Cation-π interactions in chemistry and biology: A new view of benzene, Phe, Tyr, and Trp. Science 271:163-167.
-
(1996)
Science
, vol.271
, pp. 163-167
-
-
Dougherty, D.1
-
14
-
-
79952608525
-
Accurate bond and angle parameters for X-ray protein structure refinement
-
Engh RA, Huber R. 1991. Accurate bond and angle parameters for X-ray protein structure refinement. Acta Crystallogr A 47:392-400.
-
(1991)
Acta Crystallogr A
, vol.47
, pp. 392-400
-
-
Engh, R.A.1
Huber, R.2
-
15
-
-
77956905650
-
-
Boyer PD, ed. New York: Academic Press
-
Hartley BS, Shotton DM. 1971. In Boyer PD, ed. The enzymes, vol. 3. New York: Academic Press. pp 323-373.
-
(1971)
The Enzymes
, vol.3
, pp. 323-373
-
-
Hartley, B.S.1
Shotton, D.M.2
-
16
-
-
0003069225
-
Overview of the thrombotic process and its therapy
-
Colman RW, Hirsh J, Marder VJ, Salzman EW. eds. Philadelphia, Pennsylvania: J.B. Lippincott Co.
-
Hirsh J, Salzman EW, Marder VJ, Colman RW. 1987. Overview of the thrombotic process and its therapy. In: Colman RW, Hirsh J, Marder VJ, Salzman EW. eds. Hemostasis and thrombosis, basic principles and clinical practice, 2nd ed. Philadelphia, Pennsylvania: J.B. Lippincott Co. pp 1063-1072.
-
(1987)
Hemostasis and Thrombosis, Basic Principles and Clinical Practice, 2nd Ed.
, pp. 1063-1072
-
-
Hirsh, J.1
Salzman, E.W.2
Marder, V.J.3
Colman, R.W.4
-
17
-
-
0028276982
-
Retro-binding tripeptide thrombin active site inhibitors: Discovery, synthesis, and molecular modeling
-
Iwanowicz EJ, Lau WF, Lin J, Roberts DGM, Seller S. 1994. Retro-binding tripeptide thrombin active site inhibitors: Discovery, synthesis, and molecular modeling. J Med Chem 37:2122-2124.
-
(1994)
J Med Chem
, vol.37
, pp. 2122-2124
-
-
Iwanowicz, E.J.1
Lau, W.F.2
Lin, J.3
Roberts, D.G.M.4
Seller, S.5
-
18
-
-
0031838598
-
Thrombin and factor Xa inhibitors
-
Kaiser B. 1998. Thrombin and factor Xa inhibitors. Drugs Future 23:423-436.
-
(1998)
Drugs Future
, vol.23
, pp. 423-436
-
-
Kaiser, B.1
-
19
-
-
0002066971
-
Oral thrombin inhibitors: Challenges and progress
-
Kimball SD. 1999. Oral thrombin inhibitors: Challenges and progress. Handb Exp Pharmacol (Antithrombot) 132:367-396.
-
(1999)
Handb Exp Pharmacol (Antithrombot)
, vol.132
, pp. 367-396
-
-
Kimball, S.D.1
-
20
-
-
0001770304
-
Thrombin and hemostasis
-
Machovich R, ed. Boca Raton, Florida: CRC Press, Inc.
-
Machovich R. 1984. Thrombin and hemostasis. In: Machovich R, ed. The thrombin, vol. 1. Boca Raton, Florida: CRC Press, Inc. pp 1-22.
-
(1984)
The Thrombin
, vol.1
, pp. 1-22
-
-
Machovich, R.1
-
21
-
-
0027296861
-
Molecular basis for the inhibition of human α-thrombin by the macrocyclic peptide cyclotheonamide A
-
Maryanoff BE, Qiu X, Padmanabhan KP, Tulinsky A, Almond HR Jr, Andrade-Gordon P, Greco MN, Kauffman JA, Nicolaou KC, Liu A, et al. 1993. Molecular basis for the inhibition of human α-thrombin by the macrocyclic peptide cyclotheonamide A. Proc Natl Acad Sci USA 90:8048-8052.
-
(1993)
Proc Natl Acad Sci USA
, vol.90
, pp. 8048-8052
-
-
Maryanoff, B.E.1
Qiu, X.2
Padmanabhan, K.P.3
Tulinsky, A.4
Almond H.R., Jr.5
Andrade-Gordon, P.6
Greco, M.N.7
Kauffman, J.A.8
Nicolaou, K.C.9
Liu, A.10
-
22
-
-
0031771350
-
Progress towards the discovery of orally active thrombin inhibitors
-
Menear K. 1998. Progress towards the discovery of orally active thrombin inhibitors. Curr Med Chem 5:457-468.
-
(1998)
Curr Med Chem
, vol.5
, pp. 457-468
-
-
Menear, K.1
-
24
-
-
0031059866
-
Processing of X-ray diffraction data collected in oscillation mode
-
Otwinowski Z, Minor W. 1997. Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol 276:307-326.
-
(1997)
Methods Enzymol
, vol.276
, pp. 307-326
-
-
Otwinowski, Z.1
Minor, W.2
-
25
-
-
0030693872
-
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure activity relationships, and binding orientation
-
Sall DL, Bastian JA, Briggs SL, Buben JA. Chirgadze NY, Clawson DK, Denney ML, Giera DD, Gifford-Moore DS, Harper RW, et al. 1997. Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure activity relationships, and binding orientation. J Med Chem 40:3489-3493.
-
(1997)
J Med Chem
, vol.40
, pp. 3489-3493
-
-
Sall, D.L.1
Bastian, J.A.2
Briggs, S.L.3
Buben, J.A.4
Chirgadze, N.Y.5
Clawson, D.K.6
Denney, M.L.7
Giera, D.D.8
Gifford-Moore, D.S.9
Harper, R.W.10
-
26
-
-
0343307740
-
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Structural modification of the C-3 side chain as a means to increase potency and selectivity
-
Forthcoming
-
Sall DJ, Bastian JA Chirgadze NY, Denney ML, Fisher MJ, Gifford-Moore DS, Harper RW, Klimkowski VJ, Kohn TJ, Lin HS, et al. 2000. Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Structural modification of the C-3 side chain as a means to increase potency and selectivity. J Med Chem. Forthcoming.
-
(2000)
J Med Chem.
-
-
Sall, D.J.1
Bastian, J.A.2
Chirgadze, N.Y.3
Denney, M.L.4
Fisher, M.J.5
Gifford-Moore, D.S.6
Harper, R.W.7
Klimkowski, V.J.8
Kohn, T.J.9
Lin, H.S.10
-
27
-
-
0032558508
-
2) binding site
-
2) binding site. Bioorg Med Chem Lett 8:2527-2532.
-
(1998)
Bioorg Med Chem Lett
, vol.8
, pp. 2527-2532
-
-
Sall, D.J.1
Briggs, S.2
Chirgadze, N.Y.3
Clawson, D.K.4
Gifford-Moore, D.S.5
Klimkowski, V.J.6
McCowan, J.R.7
Smith, G.F.8
Wikel, J.9
-
29
-
-
0343743298
-
Tripeptide arginal thrombin inhibitors: Structure based modification of the proline (P2) residue
-
The College of William and Mary, Williamsburg, Virginia, June 11-15
-
Schacht AL, Wiley MR, Chirgadze NY, Clawson DK, Coffman WJ, Craft TJ, Gifford-Moore DS, Jones ND, Kurz KD, Moore R, et al. 1995. Tripeptide arginal thrombin inhibitors: Structure based modification of the proline (P2) residue. 34th National Organic Symposium, The College of William and Mary, Williamsburg, Virginia, June 11-15.
-
(1995)
34th National Organic Symposium
-
-
Schacht, A.L.1
Wiley, M.R.2
Chirgadze, N.Y.3
Clawson, D.K.4
Coffman, W.J.5
Craft, T.J.6
Gifford-Moore, D.S.7
Jones, N.D.8
Kurz, K.D.9
Moore, R.10
-
30
-
-
0013491735
-
Diffraction data collection with R-AXIS II, an X-ray detecting system using imaging plate
-
Shibata A. 1990. Diffraction data collection with R-AXIS II, an X-ray detecting system using imaging plate. Rigaku J 7:28-32.
-
(1990)
Rigaku J
, vol.7
, pp. 28-32
-
-
Shibata, A.1
-
31
-
-
0026091628
-
The structure of hirugen and hirulog 1 complexes of α-thrombin
-
Skrzypczak-Janjun E, Carpenos V, Ravichandran KG, Tulinsky A, Westbrook M, Maraganore JM. 1991. The structure of hirugen and hirulog 1 complexes of α-thrombin. J Mol Biol 221:1379-1393.
-
(1991)
J Mol Biol
, vol.221
, pp. 1379-1393
-
-
Skrzypczak-Janjun, E.1
Carpenos, V.2
Ravichandran, K.G.3
Tulinsky, A.4
Westbrook, M.5
Maraganore, J.M.6
-
32
-
-
8944231643
-
A family of arginal thrombin inhibitors related to Efegatran
-
Smith GF, Craft TJ, Gifford-Moore DS, Coffman WJ, Kurz KD, Roberts E, Shuman RT, Sandusky GE, Jones ND, Chirgadze NY, Jackson CV. 1996. A family of arginal thrombin inhibitors related to Efegatran. Semin Thromb Hemost 22:173-183.
-
(1996)
Semin Thromb Hemost
, vol.22
, pp. 173-183
-
-
Smith, G.F.1
Craft, T.J.2
Gifford-Moore, D.S.3
Coffman, W.J.4
Kurz, K.D.5
Roberts, E.6
Shuman, R.T.7
Sandusky, G.E.8
Jones, N.D.9
Chirgadze, N.Y.10
Jackson, C.V.11
-
33
-
-
0001254068
-
Efegatran: A new cardiovascular anticoagulant
-
Pifarre R, ed. Philadelphia, Pennsylvania: Hanley & Belfus, Inc.
-
Smith GF, Gifford-Moore D, Craft TJ, Chirgadze N, Ruterbories KJ, Lindstrom TD, Satterwhite JH. 1997. Efegatran: A new cardiovascular anticoagulant. In: Pifarre R, ed. New anticoagulants for the cardiovascular patient. Philadelphia, Pennsylvania: Hanley & Belfus, Inc. pp 265-300.
-
(1997)
New Anticoagulants for the Cardiovascular Patient
, pp. 265-300
-
-
Smith, G.F.1
Gifford-Moore, D.2
Craft, T.J.3
Chirgadze, N.4
Ruterbories, K.J.5
Lindstrom, T.D.6
Satterwhite, J.H.7
-
34
-
-
0031978808
-
Antithrombotic agents
-
Uzan A. 1998. Antithrombotic agents. Emerging Drags 3:189-208.
-
(1998)
Emerging Drags
, vol.3
, pp. 189-208
-
-
Uzan, A.1
-
35
-
-
0032337527
-
Structure-affinity relationship of thrombin inhibitors
-
Want R, Liu L, Lai L, Tang Y. 1998. Structure-affinity relationship of thrombin inhibitors. Wuli Huaxue Xuebao 14:887-892.
-
(1998)
Wuli Huaxue Xuebao
, vol.14
, pp. 887-892
-
-
Want, R.1
Liu, L.2
Lai, L.3
Tang, Y.4
|