Two Tags in One Probe: Combining Fluorescence- and Biotin-based Detection of the Trypanosomal Cysteine Protease Rhodesain
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60077344%3A_____%2F22%3A00561246" target="_blank" >RIV/60077344:_____/22:00561246 - isvavai.cz</a>
Alternative codes found
RIV/61388963:_____/22:00561246 RIV/60076658:12310/22:43905078
Result on the web
<a href="https://doi.org/10.1002/chem.202201636" target="_blank" >https://doi.org/10.1002/chem.202201636</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/chem.202201636" target="_blank" >10.1002/chem.202201636</a>
Alternative languages
Result language
angličtina
Original language name
Two Tags in One Probe: Combining Fluorescence- and Biotin-based Detection of the Trypanosomal Cysteine Protease Rhodesain
Original language description
Rhodesain is the major cysteine protease of the protozoan parasite Trypanosoma brucei and a therapeutic target for sleeping sickness, a fatal neglected tropical disease. We designed, synthesized and characterized a bimodal activity-based probe that binds to and inactivates rhodesain. This probe exhibited an irreversible mode of action and extraordinary potency for the target protease with a k(inac)/K-i value of 37,000 M(-1)s(-1). Two reporter tags, a fluorescent coumarin moiety and a biotin affinity label, were incorporated into the probe and enabled highly sensitive detection of rhodesain in a complex proteome by in-gel fluorescence and on-blot chemiluminescence. Furthermore, the probe was employed for microseparation and quantification of rhodesain and for inhibitor screening using a competition assay. The developed bimodal rhodesain probe represents a new proteomic tool for studying Trypanosoma pathobiochemistry and antitrypanosomal drug discovery.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10606 - Microbiology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Chemistry - A European Journal
ISSN
0947-6539
e-ISSN
1521-3765
Volume of the periodical
28
Issue of the periodical within the volume
62
Country of publishing house
DE - GERMANY
Number of pages
11
Pages from-to
e202201636
UT code for WoS article
000850603500001
EID of the result in the Scopus database
2-s2.0-85137594800