(Q24310684)

1

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Christine Luong

2

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Joseph D Ho

3

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John R Somoza

4

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Erik Gjerstad

5

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Jie Tang

6

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Steven R Williams

7

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Erik Verner

8

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Wendy B Young

10

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Paul A Sprengeler

11

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Hedy Chan

12

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Kyle Mortara

13

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James W Janc

14

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Mary E McGrath

Journal of Molecular Biology

15

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language of work or name

English

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publication date

19 November 2004

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published in

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volume

344

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issue

2

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page(s)

527-47

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cites work

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The urokinase-type plasminogen activator system in cancer metastasis: A review

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High-throughput screening of enzyme inhibitors: automatic determination of tight-binding inhibition constants.

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The 2.3 A crystal structure of the catalytic domain of recombinant two-chain human tissue-type plasminogen activator

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Structure of extracellular tissue factor complexed with factor VIIa inhibited with a BPTI mutant

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Recruiting Zn2+ to mediate potent, specific inhibition of serine proteases

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Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design

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A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site

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Expression and purification of a soluble tissue factor fusion protein with an epitope for an unusual calcium-dependent antibody

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Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex

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On the size of the active site in proteases. I. Papain

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The influence of residue 190 in the S1 site of trypsin-like serine proteases on substrate selectivity is universally conserved

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Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors

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Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-directed Serine Protease Inhibitors

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Hydrogen bond stereochemistry in protein structure and function

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Development of potent and selective factor Xa inhibitors

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Optimization of a screening lead for factor VIIa/TF.

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Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines

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2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

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4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors

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Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.

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Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite

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The structure of the extracellular region of human hepsin reveals a serine protease domain and a novel scavenger receptor cysteine-rich (SRCR) domain

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Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator

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Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets

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An ester bond linking a fragment of a serine proteinase to its serpin inhibitor.

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A novel approach to serine protease inhibition: kinetic characterization of inhibitors whose potencies and selectivities are dramatically enhanced by Zinc(II).

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Contribution of multicentered short hydrogen bond arrays to potency of active site-directed serine protease inhibitors

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Design and synthesis of potent and highly selective thrombin inhibitors

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Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses

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Aromatic amidines. Comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin

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Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.

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Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator

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Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors

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Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex

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Design, Synthesis, and Crystal Structure of Selective 2-Pyridone Tissue Factor VIIa Inhibitors

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Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors

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Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors

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Design of benzamidine-type inhibitors of factor Xa

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Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.

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Human beta-tryptase is a ring-like tetramer with active sites facing a central pore

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Design of potent selective zinc-mediated serine protease inhibitors

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Free R value: a novel statistical quantity for assessing the accuracy of crystal structures

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The crystal structure of the complex of blood coagulation factor VIIa with soluble tissue factor

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Determination of the operational molarity of solutions of bovine α-chymotrypsin, trypsin, thrombin and factor Xa by spectrofluorimetric titration

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Structural basis for chemical inhibition of human blood coagulation factor Xa

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(4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase

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X-ray structure of active site-inhibited clotting factor Xa. Implications for drug design and substrate recognition

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Re-engineering of human urokinase provides a system for structure-based drug design at high resolution and reveals a novel structural subsite

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Polyoma middle T-induced vascular tumor formation: the role of the plasminogen activator/plasmin system

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Crystal structure of the catalytic domain of human plasmin complexed with streptokinase

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7 January 2021

Inhibitors of the protease domain of urokinase-type plasminogen activator

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