Asset Details
Do you wish to reserve the book?
A novel multiple-stage antimalarial agent that inhibits protein synthesis
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
A novel multiple-stage antimalarial agent that inhibits protein synthesis
Do you wish to request the book?
A novel multiple-stage antimalarial agent that inhibits protein synthesis
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
A novel multiple-stage antimalarial agent that inhibits protein synthesis
2015
Overview
There is an urgent need for new drugs to treat malaria, with broad therapeutic potential and novel modes of action, to widen the scope of treatment and to overcome emerging drug resistance. Here we describe the discovery of DDD107498, a compound with a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the
Plasmodium
parasite, with good pharmacokinetic properties and an acceptable safety profile. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.
The description of a compound (DDD107498) with antimalarial activity against multiple life-cycle stages of
Plasmodium falciparum
and good pharmacokinetic and safety properties, with potential for single-dose treatment, chemoprotection and prevention of transmission.
A new antimalarial agent
With artemisinin resistance spreading, there is an urgent need to develop new therapeutics to target
Plasmodium falciparum
, the causative agent of malaria. Here Ian Gilbert and colleagues report the discovery of a compound (DDD107498) with antimalarial activity against multiple life-cycle stages of the parasite and good pharmacokinetic and safety properties. It is non-mutagenic and has potential for both single-dose treatment and once-weekly chemoprotection. DDD107498 acts through inhibition of cytosolic protein synthesis, with translation elongation factor eEF2 as its target.
Publisher
Nature Publishing Group UK,Nature Publishing Group
Subject
/ 59/5
/ Animals
/ Antimalarials - administration & dosage
/ Antimalarials - adverse effects
/ Antimalarials - pharmacokinetics
/ Antimalarials - pharmacology
/ Female
/ Gene Expression Regulation - drug effects
/ Humanities and Social Sciences
/ Kinases
/ Life Cycle Stages - drug effects
/ Malaria
/ Male
/ Peptide Elongation Factor 2 - antagonists & inhibitors
/ Peptide Elongation Factor 2 - metabolism
/ Plasmodium - growth & development
/ Plasmodium berghei - drug effects
/ Plasmodium berghei - physiology
/ Plasmodium falciparum - drug effects
/ Plasmodium falciparum - metabolism
/ Plasmodium vivax - drug effects
/ Plasmodium vivax - metabolism
/ Protein Biosynthesis - drug effects
/ Quinolines - administration & dosage
/ Quinolines - pharmacokinetics
/ Science
