Last update 01 Nov 2024

CysEP x DHODH

Last update 01 Nov 2024

Basic Info

Related Targets

CysEPDHODH

Drugs associated with CysEP x DHODH

N-tert butylisoquine

Target

CysEP x DHODH

Mechanism

CysEP inhibitors [+2]

Active Org.-

Originator Org.

The University of Liverpool

Active Indication-

Inactive Indication

Malaria

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with CysEP x DHODH

NCT00675064 / CompletedPhase 1

Single-blind, Placebo-controlled, Randomized Study Testing Single Ascending Doses of GSK369796 in Healthy Subjects

This study will examine safety of single doses of GSK369796 in healthy subjects, along with some test to examine how quickly GSK369796 gets in your blood, and how long it takes your body to get rid of it.

Start Date02 May 2008

Sponsor / Collaborator

GSK Plc

[+1]

100 Clinical Results associated with CysEP x DHODH

100 Translational Medicine associated with CysEP x DHODH

0 Patents (Medical) associated with CysEP x DHODH

Literatures (Medical) associated with CysEP x DHODH

01 Jun 2015·Natural Product CommunicationsQ4 · MEDICINE

Computational and Investigative Study of Flavonoids Active against Trypanosoma cruzi and Leishmania spp

Q4 · MEDICINE

ArticleOA

Author: Scotti, Marcus Tullius ; Junior, Francisco J.B.M. ; da Silva, Marcelo S. ; Scotti, Luciana ; Ribeiro, Frederico F.

Flavonoid compounds active against Trypanosoma cruzi and Leishmania species were submitted to several methodologies in silico: docking with the enzymes cruzain and trypanothione reductase (from T. cruzi), and N-myristoyltransferase, dihydroorotate dehydrogenase, and trypanothiona reductase (from Leishmania spp). Molecular maps of the complexes and the ligands were calculated. In order to compare and evaluate the antioxidant activity of the flavonoids with their antiprotozoal activity, quantum parameters were calculated. Considering the energies, interactions, and hydrophobic surfaces calculated, the flavonoids chrysin dimethyl ether against T. cruzi, and ladanein against Leishmania sp. presented the best results. The antioxidant activity did not show any correlation with anti-parasitic activity; only chrysin and its dimethyl ether showed favorable anti-parasitic results. This study hopes to contribute to existing research on these natural products against these tropical parasites.

31 Aug 2014·Current Clinical Pharmacology

An In-Silico Investigation of Anti-Chagas Phytochemicals

Article

Author: McCulley, Stephanie F. ; Setzer, William N.

Over 18 million people in tropical and subtropical America are afflicted by American trypanosomiasis or Chagas disease. In humans, symptoms of the disease include fever, swelling, and heart and brain damage, usually leading to death. There is currently no effective treatment for this disease. Plant products continue to be rich sources of clinically useful drugs, and the biodiversity of the Neotropics suggests great phytomedicinal potential. Screening programs have revealed numerous plant species and phytochemical agents that have shown in-vitro or in-vivo antitrypanosomal activity, but the biochemical targets of these phytochemicals are not known. In this work, we present a molecular docking analysis of Neotropical phytochemicals, which have already demonstrated antiparasitic activity against Trypanosoma cruzi, with potential druggable protein targets of the parasite. Several protein targets showed in-silico selectivity for trypanocidal phytochemicals, including trypanothione reductase, pteridine reductase 2, lipoamide dehydrogenase, glucokinase, dihydroorotate dehydrogenase, cruzain, dihydrofolate-reductase/thymidylate-synthase, and farnesyl diphosphate synthase. Some of the phytochemical ligands showed notable docking preference for trypanothione reductase, including flavonoids, fatty-acid-derived oxygenated hydrocarbons, geranylgeraniol and the lignans ganschisandrine and eupomatenoid-6.

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