Document Detail


Targeting DHFR in parasitic protozoa.
MedLine Citation:
PMID:  15718161     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Parasitic apicomplexans are responsible for some of the most severe worldwide health problems, including malaria, toxoplasmosis and cryptosporidiosis. These parasites are characterized by a bifunctional enzyme, dihydrofolate reductase-thymidylate synthase (DHFR-TS), which has a crucial role in pyrimidine biosynthesis. Inhibitors of DHFR have been successful in the treatment of toxoplasmosis and malaria. However, there is currently no effective therapy for cryptosporidiosis, and despite early successes against malaria, resistance to DHFR inhibitors in malaria parasites has now become a global problem. Novel DHFR inhibitors, designed using the recently revealed crystal structures of the enzymes from two parasitic protozoa, are in development.
Authors:
Amy C Anderson
Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Drug discovery today     Volume:  10     ISSN:  1359-6446     ISO Abbreviation:  Drug Discov. Today     Publication Date:  2005 Jan 
Date Detail:
Created Date:  2005-02-18     Completed Date:  2005-09-01     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9604391     Medline TA:  Drug Discov Today     Country:  England    
Other Details:
Languages:  eng     Pagination:  121-8     Citation Subset:  IM    
Affiliation:
Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA. Amy.C.Anderson@Dartmouth.edu
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MeSH Terms
Descriptor/Qualifier:
Animals
Antiprotozoal Agents / pharmacology*,  therapeutic use
Clinical Trials as Topic
Eukaryota / drug effects*,  enzymology,  physiology
Folic Acid Antagonists / pharmacology*,  therapeutic use
Humans
Protozoan Infections / drug therapy*,  enzymology
Tetrahydrofolate Dehydrogenase / chemistry,  metabolism*
Chemical
Reg. No./Substance:
0/Antiprotozoal Agents; 0/Folic Acid Antagonists; EC 1.5.1.3/Tetrahydrofolate Dehydrogenase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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