Open Access
Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors
Antonio C B Burtoloso
1
,
Sérgio de Albuquerque
2
,
Mark Furber
3
,
Juliana C Gomes
1
,
Cristiana Gonçalez
2
,
Peter W. Kenny
4
,
Andrei Leitão
5
,
José Carlos Quilles
4
,
Jean F R Ribeiro
4
,
Josmar R Rocha
4
3
AstraZeneca, Mölndal, Sweden
|
Publication type: Journal Article
Publication date: 2017-02-21
scimago Q1
wos Q1
SJR: 1.370
CiteScore: 7.0
Impact factor: 3.4
ISSN: 19352727, 19352735
PubMed ID:
28222138
Infectious Diseases
Public Health, Environmental and Occupational Health
Abstract
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Anti-trypanosomal activity against the CL Brener strain of T. cruzi was observed in the 0.1 μM to 1 μM range for three nitrile-based cysteine protease inhibitors based on two scaffolds known to be associated with cathepsin K inhibition. The two compounds showing the greatest potency against the trypanosome were characterized by EC50 values (0.12 μM and 0.25 μM) that were an order of magnitude lower than the corresponding Ki values measured against cruzain, a recombinant form of cruzipain, in an enzyme inhibition assay. This implies that the anti-trypanosomal activity of these two compounds may not be explained only by the inhibition of the cruzain enzyme, thereby triggering a putative polypharmacological profile towards cysteine proteases.
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29
Total citations:
29
Citations from 2024:
3
(10%)
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GOST
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Burtoloso A. C. B. et al. Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors // PLoS Neglected Tropical Diseases. 2017. Vol. 11. No. 2. p. e0005343.
GOST all authors (up to 50)
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Burtoloso A. C. B., de Albuquerque S., Furber M., Gomes J. C., Gonçalez C., Kenny P. W., Leitão A., Montanari C. A., Quilles J. C., Ribeiro J. F. R., Rocha J. R. Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors // PLoS Neglected Tropical Diseases. 2017. Vol. 11. No. 2. p. e0005343.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1371/journal.pntd.0005343
UR - https://doi.org/10.1371/journal.pntd.0005343
TI - Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors
T2 - PLoS Neglected Tropical Diseases
AU - Burtoloso, Antonio C B
AU - de Albuquerque, Sérgio
AU - Furber, Mark
AU - Gomes, Juliana C
AU - Gonçalez, Cristiana
AU - Kenny, Peter W.
AU - Leitão, Andrei
AU - Montanari, Carlos Alberto
AU - Quilles, José Carlos
AU - Ribeiro, Jean F R
AU - Rocha, Josmar R
PY - 2017
DA - 2017/02/21
PB - Public Library of Science (PLoS)
SP - e0005343
IS - 2
VL - 11
PMID - 28222138
SN - 1935-2727
SN - 1935-2735
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_Burtoloso,
author = {Antonio C B Burtoloso and Sérgio de Albuquerque and Mark Furber and Juliana C Gomes and Cristiana Gonçalez and Peter W. Kenny and Andrei Leitão and Carlos Alberto Montanari and José Carlos Quilles and Jean F R Ribeiro and Josmar R Rocha},
title = {Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors},
journal = {PLoS Neglected Tropical Diseases},
year = {2017},
volume = {11},
publisher = {Public Library of Science (PLoS)},
month = {feb},
url = {https://doi.org/10.1371/journal.pntd.0005343},
number = {2},
pages = {e0005343},
doi = {10.1371/journal.pntd.0005343}
}
Cite this
MLA
Copy
Burtoloso, Antonio C. B., et al. “Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors.” PLoS Neglected Tropical Diseases, vol. 11, no. 2, Feb. 2017, p. e0005343. https://doi.org/10.1371/journal.pntd.0005343.
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