Synthesis and biological evaluation of reversible inhibitors of IdeS, a bacterial cysteine protease and virulence determinant
(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:
https://lup.lub.lu.se/record/1426453
- author
- Berggren, Kristina ; Johansson, Björn LU ; Fex, Tomas ; Kihlberg, Jan ; Björck, Lars LU and Luthman, Kristina
- organization
- publishing date
- 2009
- 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
- 2016-04-01 11:51:08
- date last changed
- 2022-01-26 19:14:43
@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}}, keywords = {{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}}, doi = {{10.1016/j.bmc.2009.03.026}}, volume = {{17}}, year = {{2009}}, }