Current status and progress made in malaria chemotherapy
Malaria is the most important parasitic disease worldwide, affecting more than 500 million people and causing close to 1 million deaths per annum. This serious fact is mainly attributable to the emergence of drug resistant strains of Plasmodium falciparum. The advances made in malaria chemotherapy b...
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todo:paper_09298673_v14_n3_p289_Linares2023-10-03T15:47:37Z Current status and progress made in malaria chemotherapy Liñares, G.E.G. Rodriguez, J.B. Chloroquine Cysteine proteases Farnesyltransferase inhibitors Piperazine derivatives Plasmodium falciparum 4 aminoquinoline derivative aminobenzenesulfonamide derivative aminophenol derivative amodiaquine antimalarial agent artemisinin artemisinin derivative artemisone chloroquine cysteine proteinase dihydroartemisinin dihydrofolate reductase falcipain inhibitor fatty acid fatty acid synthase inhibitor heme hemoglobin mefloquine mepacrine methylpiperazine derivative polyamine protein farnesyltransferase proteinase pyrimethamine pyronaridine quinine quinoline derivative sulfonamide thioacridone derivative unclassified drug unindexed drug antimalarial agent artemisinin artemisinin derivative cysteine proteinase cysteine proteinase inhibitor falcipain fatty acid glutathione glutathione transferase hemoprotein hemozoin p21(ras) farnesyl protein transferase p21(ras) farnesyl-protein transferase polyamine sesquiterpene thioredoxin transferase antimalarial activity biochemistry chemotherapy drug bioavailability drug design drug half life drug potency drug potentiation drug structure human IC 50 in vitro study in vivo study malaria control malaria falciparum neurotoxicity nonhuman parasite survival parasitosis Plasmodium falciparum review structure activity relation animal biosynthesis drug antagonism drug effect drug resistance malaria metabolism physiology Alkyl and Aryl Transferases Animals Antimalarials Artemisinins Cysteine Endopeptidases Cysteine Proteinase Inhibitors Drug Resistance Fatty Acids Glutathione Glutathione Transferase Hemeproteins Humans Malaria Plasmodium falciparum Polyamines Sesquiterpenes Structure-Activity Relationship Thioredoxin Malaria is the most important parasitic disease worldwide, affecting more than 500 million people and causing close to 1 million deaths per annum. This serious fact is mainly attributable to the emergence of drug resistant strains of Plasmodium falciparum. The advances made in malaria chemotherapy based on unique aspects of the biochemistry and physiology of the responsible agents for this disease, parasites of Plasmodium genus, are covered in this review. Increasing resistance to conventional antimalarial drugs constitutes the main drawback for the persistence of this disease. In the present article, a comprehensive analysis of selected molecular targets is depicted in terms of their potential utility as chemotherapeutic agents. Our review focuses on different and important molecular targets for drug design that include proteases that hydrolyze hemoglobin, protein farnesyltransferase, heme detoxification pathway, polyamine pathways, dihydrofolate reductase, artemisinin-based combination therapies (ACTs), etc. Therefore, rational approaches to control malaria targeting metabolic pathways of malaria parasites which are essential for parasites survival are presented. © 2007 Bentham Science Publishers Ltd. Fil:Rodriguez, J.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_09298673_v14_n3_p289_Linares |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Chloroquine Cysteine proteases Farnesyltransferase inhibitors Piperazine derivatives Plasmodium falciparum 4 aminoquinoline derivative aminobenzenesulfonamide derivative aminophenol derivative amodiaquine antimalarial agent artemisinin artemisinin derivative artemisone chloroquine cysteine proteinase dihydroartemisinin dihydrofolate reductase falcipain inhibitor fatty acid fatty acid synthase inhibitor heme hemoglobin mefloquine mepacrine methylpiperazine derivative polyamine protein farnesyltransferase proteinase pyrimethamine pyronaridine quinine quinoline derivative sulfonamide thioacridone derivative unclassified drug unindexed drug antimalarial agent artemisinin artemisinin derivative cysteine proteinase cysteine proteinase inhibitor falcipain fatty acid glutathione glutathione transferase hemoprotein hemozoin p21(ras) farnesyl protein transferase p21(ras) farnesyl-protein transferase polyamine sesquiterpene thioredoxin transferase antimalarial activity biochemistry chemotherapy drug bioavailability drug design drug half life drug potency drug potentiation drug structure human IC 50 in vitro study in vivo study malaria control malaria falciparum neurotoxicity nonhuman parasite survival parasitosis Plasmodium falciparum review structure activity relation animal biosynthesis drug antagonism drug effect drug resistance malaria metabolism physiology Alkyl and Aryl Transferases Animals Antimalarials Artemisinins Cysteine Endopeptidases Cysteine Proteinase Inhibitors Drug Resistance Fatty Acids Glutathione Glutathione Transferase Hemeproteins Humans Malaria Plasmodium falciparum Polyamines Sesquiterpenes Structure-Activity Relationship Thioredoxin |
| spellingShingle |
Chloroquine Cysteine proteases Farnesyltransferase inhibitors Piperazine derivatives Plasmodium falciparum 4 aminoquinoline derivative aminobenzenesulfonamide derivative aminophenol derivative amodiaquine antimalarial agent artemisinin artemisinin derivative artemisone chloroquine cysteine proteinase dihydroartemisinin dihydrofolate reductase falcipain inhibitor fatty acid fatty acid synthase inhibitor heme hemoglobin mefloquine mepacrine methylpiperazine derivative polyamine protein farnesyltransferase proteinase pyrimethamine pyronaridine quinine quinoline derivative sulfonamide thioacridone derivative unclassified drug unindexed drug antimalarial agent artemisinin artemisinin derivative cysteine proteinase cysteine proteinase inhibitor falcipain fatty acid glutathione glutathione transferase hemoprotein hemozoin p21(ras) farnesyl protein transferase p21(ras) farnesyl-protein transferase polyamine sesquiterpene thioredoxin transferase antimalarial activity biochemistry chemotherapy drug bioavailability drug design drug half life drug potency drug potentiation drug structure human IC 50 in vitro study in vivo study malaria control malaria falciparum neurotoxicity nonhuman parasite survival parasitosis Plasmodium falciparum review structure activity relation animal biosynthesis drug antagonism drug effect drug resistance malaria metabolism physiology Alkyl and Aryl Transferases Animals Antimalarials Artemisinins Cysteine Endopeptidases Cysteine Proteinase Inhibitors Drug Resistance Fatty Acids Glutathione Glutathione Transferase Hemeproteins Humans Malaria Plasmodium falciparum Polyamines Sesquiterpenes Structure-Activity Relationship Thioredoxin Liñares, G.E.G. Rodriguez, J.B. Current status and progress made in malaria chemotherapy |
| topic_facet |
Chloroquine Cysteine proteases Farnesyltransferase inhibitors Piperazine derivatives Plasmodium falciparum 4 aminoquinoline derivative aminobenzenesulfonamide derivative aminophenol derivative amodiaquine antimalarial agent artemisinin artemisinin derivative artemisone chloroquine cysteine proteinase dihydroartemisinin dihydrofolate reductase falcipain inhibitor fatty acid fatty acid synthase inhibitor heme hemoglobin mefloquine mepacrine methylpiperazine derivative polyamine protein farnesyltransferase proteinase pyrimethamine pyronaridine quinine quinoline derivative sulfonamide thioacridone derivative unclassified drug unindexed drug antimalarial agent artemisinin artemisinin derivative cysteine proteinase cysteine proteinase inhibitor falcipain fatty acid glutathione glutathione transferase hemoprotein hemozoin p21(ras) farnesyl protein transferase p21(ras) farnesyl-protein transferase polyamine sesquiterpene thioredoxin transferase antimalarial activity biochemistry chemotherapy drug bioavailability drug design drug half life drug potency drug potentiation drug structure human IC 50 in vitro study in vivo study malaria control malaria falciparum neurotoxicity nonhuman parasite survival parasitosis Plasmodium falciparum review structure activity relation animal biosynthesis drug antagonism drug effect drug resistance malaria metabolism physiology Alkyl and Aryl Transferases Animals Antimalarials Artemisinins Cysteine Endopeptidases Cysteine Proteinase Inhibitors Drug Resistance Fatty Acids Glutathione Glutathione Transferase Hemeproteins Humans Malaria Plasmodium falciparum Polyamines Sesquiterpenes Structure-Activity Relationship Thioredoxin |
| description |
Malaria is the most important parasitic disease worldwide, affecting more than 500 million people and causing close to 1 million deaths per annum. This serious fact is mainly attributable to the emergence of drug resistant strains of Plasmodium falciparum. The advances made in malaria chemotherapy based on unique aspects of the biochemistry and physiology of the responsible agents for this disease, parasites of Plasmodium genus, are covered in this review. Increasing resistance to conventional antimalarial drugs constitutes the main drawback for the persistence of this disease. In the present article, a comprehensive analysis of selected molecular targets is depicted in terms of their potential utility as chemotherapeutic agents. Our review focuses on different and important molecular targets for drug design that include proteases that hydrolyze hemoglobin, protein farnesyltransferase, heme detoxification pathway, polyamine pathways, dihydrofolate reductase, artemisinin-based combination therapies (ACTs), etc. Therefore, rational approaches to control malaria targeting metabolic pathways of malaria parasites which are essential for parasites survival are presented. © 2007 Bentham Science Publishers Ltd. |
| format |
JOUR |
| author |
Liñares, G.E.G. Rodriguez, J.B. |
| author_facet |
Liñares, G.E.G. Rodriguez, J.B. |
| author_sort |
Liñares, G.E.G. |
| title |
Current status and progress made in malaria chemotherapy |
| title_short |
Current status and progress made in malaria chemotherapy |
| title_full |
Current status and progress made in malaria chemotherapy |
| title_fullStr |
Current status and progress made in malaria chemotherapy |
| title_full_unstemmed |
Current status and progress made in malaria chemotherapy |
| title_sort |
current status and progress made in malaria chemotherapy |
| url |
http://hdl.handle.net/20.500.12110/paper_09298673_v14_n3_p289_Linares |
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AT linaresgeg currentstatusandprogressmadeinmalariachemotherapy AT rodriguezjb currentstatusandprogressmadeinmalariachemotherapy |
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