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Synthesis and biological evaluation of reversible inhibitors of IdeS, a bacterial cysteine protease and virulence determinant

Berggren, Kristina; Johansson, Björn LU ; Fex, Tomas; Kihlberg, Jan; Björck, Lars LU and Luthman, Kristina (2009) In Bioorganic & Medicinal Chemistry 17(9). p.3463-3470
Abstract
Analogues of the irreversible protease inhibitors TPCK and TLCK have been synthesized and tested as inhibitors of the bacterial cysteine protease IdeS excreted by Streptococcus pyogenes. Eight compounds were identified as inhibitors of IdeS in an in vitro assay. The most potent compounds contained an aldehyde function, thus acting as efficient reversible inhibitors, nitrile and azide derivatives showed moderate activity. (C) 2009 Elsevier Ltd. All rights reserved.
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
IdeS, Cysteine proteases, Reversible inhibitors, Streptococcus pyogenes
in
Bioorganic & Medicinal Chemistry
volume
17
issue
9
pages
3463 - 3470
publisher
Elsevier
external identifiers
  • wos:000265683700025
  • scopus:65349158258
ISSN
0968-0896
DOI
10.1016/j.bmc.2009.03.026
language
English
LU publication?
yes
id
1cc418d8-1458-4455-bf8a-cfcf63c43848 (old id 1426453)
date added to LUP
2009-06-29 15:16:20
date last changed
2017-01-01 04:36:16
@article{1cc418d8-1458-4455-bf8a-cfcf63c43848,
  abstract     = {Analogues of the irreversible protease inhibitors TPCK and TLCK have been synthesized and tested as inhibitors of the bacterial cysteine protease IdeS excreted by Streptococcus pyogenes. Eight compounds were identified as inhibitors of IdeS in an in vitro assay. The most potent compounds contained an aldehyde function, thus acting as efficient reversible inhibitors, nitrile and azide derivatives showed moderate activity. (C) 2009 Elsevier Ltd. All rights reserved.},
  author       = {Berggren, Kristina and Johansson, Björn and Fex, Tomas and Kihlberg, Jan and Björck, Lars and Luthman, Kristina},
  issn         = {0968-0896},
  keyword      = {IdeS,Cysteine proteases,Reversible inhibitors,Streptococcus pyogenes},
  language     = {eng},
  number       = {9},
  pages        = {3463--3470},
  publisher    = {Elsevier},
  series       = {Bioorganic & Medicinal Chemistry},
  title        = {Synthesis and biological evaluation of reversible inhibitors of IdeS, a bacterial cysteine protease and virulence determinant},
  url          = {http://dx.doi.org/10.1016/j.bmc.2009.03.026},
  volume       = {17},
  year         = {2009},
}