Navigation überspringen
Universitätsbibliothek Heidelberg
Status: Bibliographieeintrag

Verfügbarkeit
Standort: ---
Exemplare: ---
heiBIB
 Online-Ressource
Verfasst von:Panecka-Hofman, Joanna [VerfasserIn]   i
 Poehner, Ina [VerfasserIn]   i
 Wade, Rebecca C. [VerfasserIn]   i
Titel:Anti-trypanosomatid structure-based drug design - lessons learned from targeting the folate pathway
Verf.angabe:Joanna Panecka-Hofman, Ina Poehner, Rebecca C. Wade
E-Jahr:2022
Jahr:07 Oct 2022
Umfang:17 S.
Fussnoten:Gesehen am 17.01.2023
Titel Quelle:Enthalten in: Expert opinion on drug discovery
Ort Quelle:Abingdon : Taylor & Francis Group, 2006
Jahr Quelle:2022
Band/Heft Quelle:17(2022), 9, Seite 1029-1045
ISSN Quelle:1746-045X
Abstract:Introduction Trypanosomatidic parasitic infections in humans and animals caused by Trypanosoma brucei, Trypanosoma cruzi, and Leishmania species pose a significant health and economic burden in developing countries. There are few effective and accessible treatments for these diseases, and the existing therapies suffer from problems, such as parasite resistance and side effects. Structure-based drug design (SBDD) is one of the strategies that has been applied to discover new compounds targeting trypanosomatid-borne diseases.Areas covered We review the current literature (mostly over the last 5 years, searched in the PubMed database on 11 November 2021) on the application of structure-based drug design approaches to identify new anti-trypanosomatidic compounds that interfere with a validated target biochemical pathway, the trypanosomatid folate pathway.Expert opinion The application of structure-based drug design approaches to perturb the trypanosomatid folate pathway has successfully provided many new inhibitors with good selectivity profiles, most of which are natural products or their derivatives or have scaffolds of known drugs. However, the inhibitory effect against the target protein(s) often does not translate to anti-parasitic activity. Further progress is hampered by our incomplete understanding of parasite biology and biochemistry, which is necessary to complement SBDD in a multiparameter optimization approach to discovering selective anti-parasitic drugs.
DOI:doi:10.1080/17460441.2022.2113776
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext: https://doi.org/10.1080/17460441.2022.2113776
 DOI: https://doi.org/10.1080/17460441.2022.2113776
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:Dihydrofolate reductase
 folate pathway
 molecular docking
 molecular dynamics
 pteridine reductase 1
 structure-based drug design
 trypanosomatids
 virtual screening
K10plus-PPN:1831210142
Verknüpfungen:→ Zeitschrift

Permanenter Link auf diesen Titel (bookmarkfähig):  https://katalog.ub.uni-heidelberg.de/titel/69006831   QR-Code
zum Seitenanfang