专利号:WO-2023187827-A1 优先权日:2022-03-30 标题:A pharmaceutical composition comprising an inhibitor of glutamine synthetase enzyme to combat artemisinin resistance in malaria 发明人:ARUN NAGARAJ VISWANATHAN; PADMANABAN GOVINDARAJAN; GHOSH SOURAV; KUNDU RAJIB; CHANDANA MANJUNATHA; ANAND ADITYA 权利人:INST OF LIFE SCIENCES 摘要:The present disclosure relates to a pharmaceutical composition to combat artemisinin resistance in malaria with the identification of Plasmodium falciparum (Pf) glutamine synthetase (GS) as a drug target. Pf Gs is important for maintaining asparagine levels in the parasite and promote protein synthesis. Since ART-resistant parasites undergo fitness loss in amino acid/nutrient- limiting conditions and GS levels are upregulated during ART exposure, targeting Pf GS and asparagine requirement can be harnessed to prevent ART resistance. The present disclosure also provides a method of suppressing the growth of Plasmodium falciparum and a method of treating malaria using GS inhibitors.
参考标题:A Methylidene Group In The Phosphonic Acid Analogue Of Phenylalanine Reverses The Enantiopreference Of Binding To Phenylalanine Ammonia-Lyases 作者:Zsófia Bata,Renzhe Qian,Alexander Roller,Jeannie Horak,László Csaba Bencze,Csaba Paizs,Friedrich Hammerschmidt,Beáta G. Vértessy,László Poppe |发布日期:2017.6.19 摘要:Formed Prosthetic 3,5-Dihydro-4-Methylidene-5H-Imidazol-5-One (Mio) Group. Mio Enzymes Catalyze The Stereoselective Synthesis Of α- Or β-Amino Acid Enantiomers, Making These Chemical Processes Environmentally Friendly And Affordable. Characterization Of Novel Inhibitors Enables Structural Understanding Of Enzyme Mechanism And Recognizes Promising Herbicide Candidates As Well. The Present Study Found That
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