Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets (Q27636521)

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P A Sprengeler

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C Luong

3

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E Verner

4

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K Elrod

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M Kirtley

6

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J Janc

7

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J R Spencer

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J G Breitenbucher

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H Hui

10

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D McGee

11

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D Allen

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A Martelli

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R L Mackman

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

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publication date

November 2001

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published in

Chemistry and Biology

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volume

8

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issue

11

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page(s)

1107-21

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cites work

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

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

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Prevention of prostate-cancer metastasis in vivo by a novel synthetic inhibitor of urokinase-type plasminogen activator (uPA).

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

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

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Identification of novel inhibitors of urokinase via NMR-based screening

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

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7 January 2021

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

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7 January 2021

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

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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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Structure and specific binding of trypsin: comparison of inhibited derivatives and a model for substrate binding

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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

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7 January 2021

Structure of an acyl-enzyme intermediate during catalysis: (guanidinobenzoyl)trypsin

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The Entropic Cost of Bound Water in Crystals and Biomolecules

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Just add water! The effect of water on the specificity of protein-ligand binding sites and its potential application to drug design

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Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors

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De novo design and discovery of cyclic HIV protease inhibitors capable of displacing the active-site structural water molecule

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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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7 January 2021

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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7 January 2021

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

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7 January 2021