Crystal structure of the human alpha-thrombin-haemadin complex: an exosite II-binding inhibitor.

PubWeight™: 1.08‹?› | Rank: Top 10%

🔗 View Article (PMC 305786)

Published in EMBO J on November 01, 2000

Authors

J L Richardson1, B Kröger, W Hoeffken, J E Sadler, P Pereira, R Huber, W Bode, P Fuentes-Prior

Author Affiliations

1: Max-Planck-Institut für Biochemie, D-82152 Martinsried, Department of Biotechnology, BASF Aktiengesellschaft, D-67056 Ludwigshafen, Germany. richards@biochem.mpg.de

Articles citing this

Evolutionary families of peptidase inhibitors. Biochem J (2004) 3.57

Exosites in the substrate specificity of blood coagulation reactions. J Thromb Haemost (2007) 1.61

The many faces of protease-protein inhibitor interaction. EMBO J (2005) 1.11

Isolation, cloning and structural characterisation of boophilin, a multifunctional Kunitz-type proteinase inhibitor from the cattle tick. PLoS One (2008) 1.06

Sulfated, low-molecular-weight lignins are potent inhibitorsof plasmin, in addition to thrombin and factor Xa: Novel opportunity for controlling complex pathologies. Thromb Haemost (2009) 0.97

On the specificity of heparin/heparan sulfate binding to proteins. Anion-binding sites on antithrombin and thrombin are fundamentally different. PLoS One (2012) 0.88

Unique thrombin inhibition mechanism by anophelin, an anticoagulant from the malaria vector. Proc Natl Acad Sci U S A (2012) 0.88

Fibrinogen-elongated gamma chain inhibits thrombin-induced platelet response, hindering the interaction with different receptors. J Biol Chem (2008) 0.85

Interaction of the 268-282 region of glycoprotein Ibalpha with the heparin-binding site of thrombin inhibits the enzyme activation of factor VIII. Biochem J (2003) 0.82

Crystallization and preliminary crystallographic characterization of three peptidic inhibitors in complex with α-thrombin. Acta Crystallogr Sect F Struct Biol Cryst Commun (2010) 0.79

On scaffold hopping: challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans. Bioorg Med Chem Lett (2012) 0.78

Crystallization and preliminary X-ray diffraction analysis of a protease inhibitor from the haemolymph of the Indian tasar silkworm Antheraea mylitta. Acta Crystallogr Sect F Struct Biol Cryst Commun (2006) 0.78

Tyrosine sulfation modulates activity of tick-derived thrombin inhibitors. Nat Chem (2017) 0.77

More than just one: multiplicity of Hirudins and Hirudin-like Factors in the Medicinal Leech, Hirudo medicinalis. Mol Genet Genomics (2015) 0.76

Phosphorylation of the regulatory light chain of myosin in striated muscle: methodological perspectives. Eur Biophys J (2016) 0.75

Crystallization and preliminary crystallographic characterization of the N-terminal Kunitz domain of boophilin. Acta Crystallogr Sect F Struct Biol Cryst Commun (2012) 0.75

Identification and Mechanistic Analysis of a Novel Tick-Derived Inhibitor of Thrombin. PLoS One (2015) 0.75

Articles cited by this

The CCP4 suite: programs for protein crystallography. Acta Crystallogr D Biol Crystallogr (1994) 187.88

Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell (1991) 11.51

ALSCRIPT: a tool to format multiple sequence alignments. Protein Eng (1993) 10.04

SETOR: hardware-lighted three-dimensional solid model representations of macromolecules. J Mol Graph (1993) 7.31

The coagulation cascade: initiation, maintenance, and regulation. Biochemistry (1991) 6.29

The refined 1.9 A crystal structure of human alpha-thrombin: interaction with D-Phe-Pro-Arg chloromethylketone and significance of the Tyr-Pro-Pro-Trp insertion segment. EMBO J (1989) 4.49

Rotation function calculations with GLRF program. Methods Enzymol (1997) 3.99

Natural protein proteinase inhibitors and their interaction with proteinases. Eur J Biochem (1992) 3.27

The refined 1.9-A X-ray crystal structure of D-Phe-Pro-Arg chloromethylketone-inhibited human alpha-thrombin: structure analysis, overall structure, electrostatic properties, detailed active-site geometry, and structure-function relationships. Protein Sci (1992) 3.03

Factor XI activation in a revised model of blood coagulation. Science (1991) 2.87

The structure of a complex of recombinant hirudin and human alpha-thrombin. Science (1990) 2.71

Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature (1999) 2.27

How the protease thrombin talks to cells. Proc Natl Acad Sci U S A (1999) 2.21

Structural basis for the anticoagulant activity of the thrombin-thrombomodulin complex. Nature (2000) 2.04

Blood coagulation factors V and VIII: structural and functional similarities and their relationship to hemorrhagic and thrombotic disorders. Blood (1988) 2.01

Structure of the hirugen and hirulog 1 complexes of alpha-thrombin. J Mol Biol (1991) 1.89

Peptide exosite inhibitors of factor VIIa as anticoagulants. Nature (2000) 1.77

Crystal structure of the thrombin-hirudin complex: a novel mode of serine protease inhibition. EMBO J (1990) 1.65

A player of many parts: the spotlight falls on thrombin's structure. Thromb Res (1993) 1.64

Quantitative evaluation of the contribution of ionic interactions to the formation of the thrombin-hirudin complex. Biochemistry (1989) 1.61

The ornithodorin-thrombin crystal structure, a key to the TAP enigma? EMBO J (1996) 1.53

Two heads are better than one: crystal structure of the insect derived double domain Kazal inhibitor rhodniin in complex with thrombin. EMBO J (1995) 1.45

Structure of the thrombin complex with triabin, a lipocalin-like exosite-binding inhibitor derived from a triatomine bug. Proc Natl Acad Sci U S A (1997) 1.38

Thrombomodulin as a model of molecular mechanisms that modulate protease specificity and function at the vessel surface. FASEB J (1995) 1.36

Single amino acid substitutions dissociate fibrinogen-clotting and thrombomodulin-binding activities of human thrombin. Proc Natl Acad Sci U S A (1991) 1.35

Molecular mapping of the heparin-binding exosite of thrombin. Proc Natl Acad Sci U S A (1994) 1.22

New insights into the regulation of the blood clotting cascade derived from the X-ray crystal structure of bovine meizothrombin des F1 in complex with PPACK. Structure (1997) 1.17

Thrombin structure and function: why thrombin is the primary target for antithrombotics. Blood Coagul Fibrinolysis (1991) 1.15

Triabin, a highly potent exosite inhibitor of thrombin. J Biol Chem (1995) 1.14

Multiple active forms of thrombin. IV. Relative activities of meizothrombins. J Biol Chem (1990) 1.13

Thrombin, thrombomodulin and TAFI in the molecular link between coagulation and fibrinolysis. Thromb Haemost (1997) 1.13

Solution structure of recombinant hirudin and the Lys-47----Glu mutant: a nuclear magnetic resonance and hybrid distance geometry-dynamical simulated annealing study. Biochemistry (1989) 1.13

Glycosaminoglycan contributions to both protein C activation and thrombin inhibition involve a common arginine-rich site in thrombin that includes residues arginine 93, 97, and 101. J Biol Chem (1994) 1.09

Functional characterization of recombinant human meizothrombin and Meizothrombin(desF1). Thrombomodulin-dependent activation of protein C and thrombin-activatable fibrinolysis inhibitor (TAFI), platelet aggregation, antithrombin-III inhibition. J Biol Chem (1997) 1.01

Conformation of recombinant desulfatohirudin in aqueous solution determined by nuclear magnetic resonance. Biochemistry (1989) 0.98

The Asp(272)-Glu(282) region of platelet glycoprotein Ibalpha interacts with the heparin-binding site of alpha-thrombin and protects the enzyme from the heparin-catalyzed inhibition by antithrombin III. J Biol Chem (2000) 0.94

The structures and proteolytic specificities of autolysed human thrombin. Biochem J (1986) 0.93

Changes in interactions in complexes of hirudin derivatives and human alpha-thrombin due to different crystal forms. Protein Sci (1993) 0.93

Isolation, sequence analysis, and cloning of haemadin. An anticoagulant peptide from the Indian leech. J Biol Chem (1993) 0.90

Novel hirudin variants from the leech Hirudinaria manillensis. Amino acid sequence, cDNA cloning and genomic organization. Eur J Biochem (1993) 0.90

Interaction of the N-terminal region of hirudin with the active-site cleft of thrombin. Biochemistry (1992) 0.90

Hirudins and the role of thrombin: lessons from leeches. Trends Pharmacol Sci (1988) 0.88

The structure of a complex of bovine alpha-thrombin and recombinant hirudin at 2.8-A resolution. J Biol Chem (1992) 0.88

Anticoagulant thrombins. Trends Cardiovasc Med (1998) 0.87

Primary structure and function of novel O-glycosylated hirudins from the leech Hirudinaria manillensis. Biochemistry (1992) 0.87

Bothroalternin, a thrombin inhibitor from the venom of Bothrops alternatus. Toxicon (1998) 0.85

From natural to synthetic multisite thrombin inhibitors. Biopolymers (1999) 0.84

Bothrojaracin: a potent two-site-directed thrombin inhibitor. Biochemistry (1996) 0.82

Hirunorms are true hirudin mimetics. The crystal structure of human alpha-thrombin-hirunorm V complex. Protein Sci (1998) 0.81

Thrombolytic therapy in acute myocardial infarction--selected recent developments. Ann Hematol (1994) 0.81

Hirudin: amino-terminal residues play a major role in the interaction with thrombin. J Biol Chem (1991) 0.79

Thrombin inhibitors as antithrombotic agents: the importance of rapid inhibition. J Enzyme Inhib (1995) 0.79

Binding of hirudin to meizothrombin. Protein Eng (1998) 0.78

On the isolation of the thrombin inhibitor hirudin. Thromb Res (1985) 0.78

Articles by these authors

Crystal structure of the 20S proteasome from the archaeon T. acidophilum at 3.4 A resolution. Science (1995) 12.94

Structure of 20S proteasome from yeast at 2.4 A resolution. Nature (1997) 12.73

X-ray structure analysis of a membrane protein complex. Electron density map at 3 A resolution and a model of the chromophores of the photosynthetic reaction center from Rhodopseudomonas viridis. J Mol Biol (1984) 8.85

The complete genome of the hyperthermophilic bacterium Aquifex aeolicus. Nature (1998) 7.77

A gated channel into the proteasome core particle. Nat Struct Biol (2000) 5.42

Structure of the protein subunits in the photosynthetic reaction centre of Rhodopseudomonas viridis at 3Å resolution. Nature (2012) 5.22

Mutations in GPC3, a glypican gene, cause the Simpson-Golabi-Behmel overgrowth syndrome. Nat Genet (1996) 4.62

The refined 1.9 A crystal structure of human alpha-thrombin: interaction with D-Phe-Pro-Arg chloromethylketone and significance of the Tyr-Pro-Pro-Trp insertion segment. EMBO J (1989) 4.49

Fourier Domain Mode Locking (FDML): A new laser operating regime and applications for optical coherence tomography. Opt Express (2006) 4.49

The structures of HsIU and the ATP-dependent protease HsIU-HsIV. Nature (2000) 4.46

Gamma/delta cells. Annu Rev Immunol (1993) 4.35

Structure of the gene for human von Willebrand factor. J Biol Chem (1989) 4.22

Structure of bovine pancreatic trypsin inhibitor. Results of joint neutron and X-ray refinement of crystal form II. J Mol Biol (1984) 4.14

von Willebrand disease (VWD): evidence-based diagnosis and management guidelines, the National Heart, Lung, and Blood Institute (NHLBI) Expert Panel report (USA). Haemophilia (2008) 3.83

Gene deletions correlate with the development of alloantibodies in von Willebrand disease. J Clin Invest (1987) 3.73

Proteasome from Thermoplasma acidophilum: a threonine protease. Science (1995) 3.62

Human alpha 1-proteinase inhibitor. Crystal structure analysis of two crystal modifications, molecular model and preliminary analysis of the implications for function. J Mol Biol (1984) 3.60

The 3.2-A crystal structure of the human IgG1 Fc fragment-Fc gammaRIII complex. Nature (2000) 3.53

Cloning and characterization of two cDNAs coding for human von Willebrand factor. Proc Natl Acad Sci U S A (1985) 3.41

Crystallographic refinement and atomic models of two different forms of citrate synthase at 2.7 and 1.7 A resolution. J Mol Biol (1982) 3.28

Natural protein proteinase inhibitors and their interaction with proteinases. Eur J Biochem (1992) 3.27

Structural analysis of human IgG-Fc glycoforms reveals a correlation between glycosylation and structural integrity. J Mol Biol (2003) 3.25

Crystallographic refinement and atomic models of the intact immunoglobulin molecule Kol and its antigen-binding fragment at 3.0 A and 1.0 A resolution. J Mol Biol (1980) 3.25

Structure of the complex formed by bovine trypsin and bovine pancreatic trypsin inhibitor. II. Crystallographic refinement at 1.9 A resolution. J Mol Biol (1974) 3.17

The proteasome. Annu Rev Biophys Biomol Struct (1999) 3.13

Structure of von Willebrand factor-cleaving protease (ADAMTS13), a metalloprotease involved in thrombotic thrombocytopenic purpura. J Biol Chem (2001) 3.02

Crystallographic structure studies of an IgG molecule and an Fc fragment. Nature (1976) 3.00

Crystal structure of the thermosome, the archaeal chaperonin and homolog of CCT. Cell (1998) 2.94

Structure of the tetrameric restriction endonuclease NgoMIV in complex with cleaved DNA. Nat Struct Biol (2000) 2.82

Crystal structure of a carbon monoxide dehydrogenase reveals a [Ni-4Fe-5S] cluster. Science (2001) 2.78

Amino acid sequence of human von Willebrand factor. Biochemistry (1986) 2.73

The structure of a complex of recombinant hirudin and human alpha-thrombin. Science (1990) 2.71

Structure and mechanism of the aberrant ba(3)-cytochrome c oxidase from thermus thermophilus. EMBO J (2000) 2.71

Structure determination and refinement of human alpha class glutathione transferase A1-1, and a comparison with the Mu and Pi class enzymes. J Mol Biol (1993) 2.66

The metzincins--topological and sequential relations between the astacins, adamalysins, serralysins, and matrixins (collagenases) define a superfamily of zinc-peptidases. Protein Sci (1995) 2.63

Peripheral T lymphocytes: expansion potential and homeostatic regulation of pool sizes and CD4/CD8 ratios in vivo. Eur J Immunol (1989) 2.58

Phosphotransferase and substrate binding mechanism of the cAMP-dependent protein kinase catalytic subunit from porcine heart as deduced from the 2.0 A structure of the complex with Mn2+ adenylyl imidodiphosphate and inhibitor peptide PKI(5-24). EMBO J (1993) 2.54

Human C1 inhibitor: primary structure, cDNA cloning, and chromosomal localization. Biochemistry (1986) 2.52

Amplified, frequency swept lasers for frequency domain reflectometry and OCT imaging: design and scaling principles. Opt Express (2005) 2.48

The 2.0 A X-ray crystal structure of chicken egg white cystatin and its possible mode of interaction with cysteine proteinases. EMBO J (1988) 2.48

Primary structure of human neutrophil elastase. Proc Natl Acad Sci U S A (1987) 2.45

The refined 2.4 A X-ray crystal structure of recombinant human stefin B in complex with the cysteine proteinase papain: a novel type of proteinase inhibitor interaction. EMBO J (1990) 2.44

High-level biosynthetic substitution of methionine in proteins by its analogs 2-aminohexanoic acid, selenomethionine, telluromethionine and ethionine in Escherichia coli. Eur J Biochem (1995) 2.44

X-ray crystallographic structure of the light-harvesting biliprotein C-phycocyanin from the thermophilic cyanobacterium Mastigocladus laminosus and its resemblance to globin structures. J Mol Biol (1985) 2.42

Crystal structure of P22 tailspike protein: interdigitated subunits in a thermostable trimer. Science (1994) 2.41

The structure of alpha-thrombin inhibited by a 15-mer single-stranded DNA aptamer. J Biol Chem (1993) 2.39

The blue oxidases, ascorbate oxidase, laccase and ceruloplasmin. Modelling and structural relationships. Eur J Biochem (1990) 2.37

X-ray crystal structures of cytosolic glutathione S-transferases. Implications for protein architecture, substrate recognition and catalytic function. Eur J Biochem (1994) 2.37

The three-dimensional structure of class pi glutathione S-transferase in complex with glutathione sulfonate at 2.3 A resolution. EMBO J (1991) 2.36

Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology (2001) 2.36

The cystatins: protein inhibitors of cysteine proteinases. FEBS Lett (1991) 2.33

The refined crystal structure of bovine beta-trypsin at 1.8 A resolution. II. Crystallographic refinement, calcium binding site, benzamidine binding site and active site at pH 7.0. J Mol Biol (1975) 2.24

Crystal structure analysis of oxidized Pseudomonas aeruginosa azurin at pH 5.5 and pH 9.0. A pH-induced conformational transition involves a peptide bond flip. J Mol Biol (1991) 2.19

Crystal structure of a thermostable type B DNA polymerase from Thermococcus gorgonarius. Proc Natl Acad Sci U S A (1999) 2.19

Refined crystal structure of ascorbate oxidase at 1.9 A resolution. J Mol Biol (1992) 2.18

Jellyfish responsible for Irukandji syndrome. QJM (2006) 2.18

Mechanism of inhibition of the human matrix metalloproteinase stromelysin-1 by TIMP-1. Nature (1997) 2.17

Structural homology of reaction centers from Rhodopseudomonas sphaeroides and Rhodopseudomonas viridis as determined by x-ray diffraction. Proc Natl Acad Sci U S A (1986) 2.16

Structural basis for the activation of human procaspase-7. Proc Natl Acad Sci U S A (2001) 2.14

Pyrobaculum aerophilum sp. nov., a novel nitrate-reducing hyperthermophilic archaeum. Appl Environ Microbiol (1993) 2.13

Induction of specific storage organelles by von Willebrand factor propolypeptide. Cell (1991) 2.09

Structure of human des(1-45) factor Xa at 2.2 A resolution. J Mol Biol (1993) 2.07

Refined structure of the hirudin-thrombin complex. J Mol Biol (1991) 2.06

Refined three-dimensional structures of two cyanobacterial C-phycocyanins at 2.1 and 2.5 A resolution. A common principle of phycobilin-protein interaction. J Mol Biol (1987) 2.06

Structural basis for the anticoagulant activity of the thrombin-thrombomodulin complex. Nature (2000) 2.04

Crystal structure of a DNA-dependent RNA polymerase (DNA primase). Nat Struct Biol (2001) 2.03

Structure of astacin and implications for activation of astacins and zinc-ligation of collagenases. Nature (1992) 2.02

The refined 2.15 A X-ray crystal structure of human liver cathepsin B: the structural basis for its specificity. EMBO J (1991) 1.99

Structural and functional aspects of domain motions in proteins. CRC Crit Rev Biochem (1984) 1.99

The molecular structure of a dimer composed of the variable portions of the Bence-Jones protein REI refined at 2.0-A resolution. Biochemistry (1975) 1.98

Use of yeast artificial chromosome clones for mapping and walking within human chromosome segment 18q21.3. Proc Natl Acad Sci U S A (1989) 1.95

The transition of bovine trypsinogen to a trypsin-like state upon strong ligand binding. The refined crystal structures of the bovine trypsinogen-pancreatic trypsin inhibitor complex and of its ternary complex with Ile-Val at 1.9 A resolution. J Mol Biol (1978) 1.95

Requirement for gammadelta T cells in allergic airway inflammation. Science (1998) 1.93

Lesions of the posterior paraventricular thalamus block habituation of hypothalamic-pituitary-adrenal responses to repeated restraint. J Neuroendocrinol (2002) 1.91

X-ray crystal structure of the blue oxidase ascorbate oxidase from zucchini. Analysis of the polypeptide fold and a model of the copper sites and ligands. J Mol Biol (1989) 1.90

Three-dimensional structure of the complex between pancreatic secretory trypsin inhibitor (Kazal type) and trypsinogen at 1.8 A resolution. Structure solution, crystallographic refinement and preliminary structural interpretation. J Mol Biol (1982) 1.90

The ternary microplasmin-staphylokinase-microplasmin complex is a proteinase-cofactor-substrate complex in action. Nat Struct Biol (1998) 1.85

Mistletoe therapy in oncology. Cochrane Database Syst Rev (2008) 1.84

Multi-step binding of ADAMTS-13 to von Willebrand factor. J Thromb Haemost (2009) 1.84

cDNA sequences for human von Willebrand factor reveal five types of repeated domains and five possible protein sequence polymorphisms. Biochemistry (1986) 1.83

The helping hand of collagenase-3 (MMP-13): 2.7 A crystal structure of its C-terminal haemopexin-like domain. J Mol Biol (1996) 1.82

Bovine chymotrypsinogen A X-ray crystal structure analysis and refinement of a new crystal form at 1.8 A resolution. J Mol Biol (1985) 1.81

Crystal structure of gingipain R: an Arg-specific bacterial cysteine proteinase with a caspase-like fold. EMBO J (1999) 1.79

Crystal structure of bovine trypsinogen at 1-8 A resolution. II. Crystallographic refinement, refined crystal structure and comparison with bovine trypsin. J Mol Biol (1977) 1.79