Inhibitor-vermittelte Dimerisierung eines essenziellen Redoxproteins in Trypanosomatiden

Steverding, Dietmar (2019) Inhibitor-vermittelte Dimerisierung eines essenziellen Redoxproteins in Trypanosomatiden. Naturwissenschaftliche Rundschau, 72. pp. 262-264. ISSN 0028-1050

PDF (Accepted_Version) - Accepted Version Restricted to Repository staff only until 31 December 2099. Request a copy

Abstract

Trypanosomatiden sind einzellige Parasiten, die beim Menschen schwere Erkrankungen verursachen. Ein vielversprechender Angriffspunkt für potenzielle Arzneistoffe ist das Tryparedoxin, ein essenzielles Redoxprotein, das bei der Inaktivierung von Hydroperoxiden in den Zellen der Parasiten eine wichtige Rolle spielt. Das Thienopyrimidinon-Derivat CFT, ein irreversibler Inhibitor, bindet kovalent an Tryparedoxin und vernetzt es zum Dimer, das durch mehrere Wechselwirkungen zwischen Inhibitor-Protein, Inhibitor-Inhibitor und Protein-Protein stabilisiert wird. Die strukturellen Grundlagen dieser Interaktionen könnten für die Entwicklung wirksamerer Inhibitoren gegen Tryparedoxin hilfreich sein. Trypanosomatides are single-celled parasites that cause serious diseases such as sleeping sickness and chagas disease in humans. A promising point of attack for potential drugs is tryparedoxin, an essential redox protein that plays an important role in the inactivation of hydroperoxides in the cells of the parasites. The thienopyrimidinone derivative CFT, an irreversible inhibitor, binds covalently to tryparedoxin and links it to the dimer, which is stabilized by several interactions between inhibitor protein, inhibitor inhibitor and protein protein. The structural basis of these interactions could be helpful for the development of more effective inhibitors against tryparedoxin.

Item Type:	Article
Uncontrolled Keywords:	sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School:	Faculty of Medicine and Health Sciences > Norwich Medical School
UEA Research Groups:	Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology
Depositing User:	LivePure Connector
Date Deposited:	03 May 2019 15:30
Last Modified:	24 May 2022 13:25
URI:	https://ueaeprints.uea.ac.uk/id/eprint/70830
DOI:

Actions (login required)

View Item