Structural and Functional Characterization of Schistosoma mansoni Cathepsin B1

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F20%3A00525103" target="_blank" >RIV/61388963:_____/20:00525103 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1007/978-1-0716-0635-3_12" target="_blank" >http://dx.doi.org/10.1007/978-1-0716-0635-3_12</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1007/978-1-0716-0635-3_12" target="_blank" >10.1007/978-1-0716-0635-3_12</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Structural and Functional Characterization of Schistosoma mansoni Cathepsin B1

Popis výsledku v původním jazyce

Schistosomiasis caused by parasitic blood flukes of the genus Schistosoma is a global health problem with over 200 million people infected. Schistosoma mansoni cathepsin B1 (SmCB1) is a gut-associated protease critical for digestion of host blood proteins as a source of nutrients. SmCB1 is a validated drug target, and inhibitors of SmCB1 represent promising anti-schistosomals. A comprehensive structural and functional characterization of SmCB1 provides a starting point for the rational design of selective and potent SmCB1 inhibitors. Here, we report optimized protocols for (1) the production of recombinant SmCB1 in the Pichia pastoris expression system and its purification, (2) the measurement of SmCB1 activity and inhibition in a kinetic fluorescence assay, and (3) the preparation and crystallization of SmCB1 in complex with a model vinyl sulfone inhibitor, and the determination of its crystal structure.

Název v anglickém jazyce

Structural and Functional Characterization of Schistosoma mansoni Cathepsin B1

Popis výsledku anglicky

Schistosomiasis caused by parasitic blood flukes of the genus Schistosoma is a global health problem with over 200 million people infected. Schistosoma mansoni cathepsin B1 (SmCB1) is a gut-associated protease critical for digestion of host blood proteins as a source of nutrients. SmCB1 is a validated drug target, and inhibitors of SmCB1 represent promising anti-schistosomals. A comprehensive structural and functional characterization of SmCB1 provides a starting point for the rational design of selective and potent SmCB1 inhibitors. Here, we report optimized protocols for (1) the production of recombinant SmCB1 in the Pichia pastoris expression system and its purification, (2) the measurement of SmCB1 activity and inhibition in a kinetic fluorescence assay, and (3) the preparation and crystallization of SmCB1 in complex with a model vinyl sulfone inhibitor, and the determination of its crystal structure.

Druh

C - Kapitola v odborné knize

CEP obor

—

OECD FORD obor

10608 - Biochemistry and molecular biology

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2020

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název knihy nebo sborníku

Schistosoma mansoni: Methods and Protocols

ISBN

978-1-0716-0634-6

Počet stran výsledku

14

Strana od-do

145-158

Počet stran knihy

265

Název nakladatele

Humana Press

Místo vydání

New York

Kód UT WoS kapitoly

000680910400013