Dihydrofolate reductase

Part 2 book "Trypanosomatid diseases, molecular routes to drug discovery" includes content: Proteases of trypanosoma brucei, peptidases in autophagy are therapeutic targets for leishmaniasis, screening approaches towards trypanothione reductase, inhibition of trypanothione synthetase as a therapeutic concept, targeting the trypanosomatidic enzymes pteridine reductase and dihydrofolate reductase.... and other contents.

269p oursky05 20-09-2023 2 1   Download

Dihydrofolate reductase (DHFR) is an important target for antimetabolite class of antimicrobials because it participates in purine synthesis. 2-mercaptobenzimidazole (2MBI) has similar structural features as purine nucleotides.

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Sulfonamide derivatives are of great attention due to their wide spectrum of biological activities. Sulfonamides conjugated with acetamide fragments exhibit antimicrobial and anticancer activities.

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Dihydrofolate reductase (DHFR) is an important enzyme for de novo synthesis of nucleotides in Plasmodium falciparum and it is essential for cell proliferation. DHFR is a well known antimalarial target for drugs like cycloguanil and pyrimethamine which target its inhibition for their pharmacological actions.

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Expression vector engineering technology is one of the most convenient and timely method for cell line development to meet the rising demand of novel production cell line with high productivity.

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Dihydrofolate reductase (EC 1.5.1.3) is a key enzyme in the folate biosyn-thetic pathway. Information regarding key residues in the dihydrofolate-binding site ofMycobacterium aviumdihydrofolate reductase is lacking. On the basis of previous information, Asp31 and Leu32 were selected as resi-dues that are potentially important in interactions with dihydrofolate and antifolates (e.g. trimethoprim), respectively.

13p galaxyss3 19-03-2013 50 3   Download

Post-translational glycosylation is one of the most abundant forms of cova-lent protein modification in eukaryotic cells. It plays an important role in determining the properties of proteins, and stabilizes many proteins against thermal denaturation. Protein glycosylation may establish a surface micro-environment that resembles that of unglycosylated proteins in concentrated solutions of sugars and other polyols.

9p mobifone23 21-01-2013 42 3   Download

Tên chung quốc tế: Trimethoprim. Mã ATC: J01E A01. Loại thuốc: Kháng khuẩn. Dạng thuốc và hàm lượng: Viên nén 100 mg; 200 mg trimethoprim. Trimethoprim tiêm (dưới dạng lactat) 20 mg/ml. Dược lý và cơ chế tác dụng Trimethoprim có tác dụng kìm khuẩn, ức chế enzym dihydrofolate reductase của vi khuẩn. Trimethoprim chống lại tác nhân gây nhiễm khuẩn đường tiết niệu như E. coli, Proteus, Klebsiella, Enterobacter, Staphylococcus saprophyticus, Streptococcus faecalis và chống lại nhiều vi khuẩn dạng coli. ...

8p dududam 18-05-2011 79 11   Download

Trimethoprim Trimethoprim is a diaminopyrimidine, a structural analogue of the pteridine moiety of folic acid. Trimethoprim is a competitive inhibitor of dihydrofolate reductase; this enzyme is responsible for reduction of dihydrofolic acid to tetrahydrofolic acid—the essential final component in the folic acid synthesis pathway. Like that of the sulfonamides, the activity of trimethoprim is compromised in the presence of exogenous thymine or thymidine. Inhibition of Nucleic Acid Synthesis or Activity Numerous antibacterial compounds have disparate effects on nucleic acids.

7p colgate_colgate 21-12-2010 60 2   Download

Pemetrexed is a novel folate-directed antimetabolite. It is "multitargeted" in that it inhibits the activity of several enzymes, including thymidylate synthetase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase, thereby affecting the synthesis of both purine and pyrimidine nucleic acid precursors. To avoid significant toxicity to the normal tissues, patients receiving pemetrexed should also receive low-dose folate and vitamin B12 supplementation.

5p konheokonmummim 03-12-2010 65 3   Download