(Q50136424)

25 February 2018

title

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

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25 February 2018

author name string

Nienaber VL

1

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25 February 2018

Davidson D

2

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25 February 2018

Edalji R

3

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25 February 2018

Giranda VL

4

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25 February 2018

Klinghofer V

5

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25 February 2018

Henkin J

6

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25 February 2018

Magdalinos P

7

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25 February 2018

Mantei R

8

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25 February 2018

Merrick S

9

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25 February 2018

Severin JM

10

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25 February 2018

Smith RA

11

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25 February 2018

Stewart K

12

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25 February 2018

Walter K

13

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25 February 2018

Wang J

14

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25 February 2018

Wendt M

15

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25 February 2018

Weitzberg M

16

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25 February 2018

Zhao X

17

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25 February 2018

Rockway T

18

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25 February 2018

publication date

1 May 2000

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25 February 2018

published in

Structure

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25 February 2018

volume

8

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25 February 2018

issue

5

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25 February 2018

page(s)

553-563

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25 February 2018

Tumor-associated urokinase-type plasminogen activator: biological and clinical significance

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Bone matrix degradation by the plasminogen activation system. Possible mechanism of bone destruction in arthritis

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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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Inhibition of establishment of primary and micrometastatic tumors by a urokinase plasminogen activator receptor antagonist

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Overexpression of plasminogen activator inhibitor 2 in human melanoma cells inhibits spontaneous metastasis in scid/scid mice

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Absence of host plasminogen activator inhibitor 1 prevents cancer invasion and vascularization.

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Optimal subsite occupancy and design of a selective inhibitor of urokinase.

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7 January 2021

The crystal structure of the catalytic domain of human urokinase-type plasminogen activator

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7 January 2021

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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7 January 2021

The synthesis of three 4-substituted benzo[b]thiophene-2-carboxamidines as potent and selective inhibitors of urokinase

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

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7 January 2021

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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7 January 2021

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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Thrombin active site inhibitors

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7 January 2021

Structural basis for chemical inhibition of human blood coagulation factor Xa

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7 January 2021

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

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7 January 2021

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 human des(1-45) factor Xa at 2.2 A resolution

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7 January 2021

Structural mapping of the active site specificity determinants of human tissue-type plasminogen activator. Implications for the design of low molecular weight substrates and inhibitors

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7 January 2021

Inhibitory effect of amidino-substituted heterocyclic compounds on the amidase activity of plasmin and of high and low molecular weight urokinase and on urokinase-induced plasminogen activation

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7 January 2021

Enzyme flexibility, solvent and 'weak' interactions characterize thrombin-ligand interactions: implications for drug design

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7 January 2021

Crystal structures of factor Xa specific inhibitors in complex with trypsin: structural grounds for inhibition of factor Xa and selectivity against thrombin

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7 January 2021

Syntheses and selective inhibitory activities of terphenyl-bisamidines for serine proteases

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7 January 2021

Update on computer-aided drug design

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7 January 2021

Structure-based drug design: progress, results and challenges

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7 January 2021

A player of many parts: the spotlight falls on thrombin's structure.

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7 January 2021

Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile

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7 January 2021

Cloning, characterization and nucleotide sequences of two cDNAs encoding human pancreatic trypsinogens

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7 January 2021

Processing of X-ray diffraction data collected in oscillation mode

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7 January 2021

Accurate bond and angle parameters for X-ray protein structure refinement

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7 January 2021

Protein folding and association: insights from the interfacial and thermodynamic properties of hydrocarbons

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7 January 2021

10.1016/S0969-2126(00)00136-2

Identifiers

DOI

1 reference

25 February 2018

1 reference

25 February 2018