Relevant bibliographies by topics / DHFR inhibition

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  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'DHFR inhibition'

Author: Grafiati
Published: 7 June 2025
Last updated: 2 August 2025

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Journal articles on the topic "DHFR inhibition"

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Maskell, Jeffrey P., Armine M. Sefton, and Lucinda M. C. Hall. "Multiple Mutations Modulate the Function of Dihydrofolate Reductase in Trimethoprim-ResistantStreptococcus pneumoniae." Antimicrobial Agents and Chemotherapy 45, no. 4 (2001): 1104–8. http://dx.doi.org/10.1128/aac.45.4.1104-1108.2001.

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ABSTRACT Trimethoprim resistance in Streptococcus pneumoniaecan be conferred by a single amino acid substitution (I100-L) in dihydrofolate reductase (DHFR), but resistant clinical isolates usually carry multiple DHFR mutations. DHFR genes from five trimethoprim-resistant isolates from the United Kingdom were compared to susceptible isolates and used to transform a susceptible control strain (CP1015). All trimethoprim-resistant isolates and transformants contained the I100-L mutation. The properties of DHFRs from transformants with different combinations of mutations were compared. In a transfo
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Mayur, Bagane*1 Rutuparna Karkare2 Rajesh Jorgewad3 Saee Thakur4 Medha Petkar5 Amruta Patil6 Sneha Kagale7. "Revealing the Molecular Interactions: Investigating the Docking Studies of (N-(4-Carboxy-4-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]-benzoylamino}-butyl)-phthalamic acid) with Dihydrofolate Reductase." International Journal in Pharmaceutical Sciences 2, no. 4 (2024): 321–30. https://doi.org/10.5281/zenodo.10932469.

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Dihydrofolate reductase (DHFR) is a vital enzyme in folate metabolism, and its inhibition is a well-established strategy for antibacterial and anticancer therapies. Here, we investigated the inhibitory mechanism of N-(4-Carboxy-4-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]-benzoylamino}-butyl)-phthalamicacid(BDBM50011320), a small molecule identified through in silico docking to possess high affinity for human DHFR. In vitro enzymatic assays confirmed a sub-nanomolar Ki value for BDBM50011320, indicating potent inhibition of DHFR activity. To elucidate the binding mode and inhibitory mechanis
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Queener, S. F., V. Cody, J. Pace, P. Torkelson, and A. Gangjee. "Trimethoprim Resistance of Dihydrofolate Reductase Variants from Clinical Isolates of Pneumocystis jirovecii." Antimicrobial Agents and Chemotherapy 57, no. 10 (2013): 4990–98. http://dx.doi.org/10.1128/aac.01161-13.

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ABSTRACTPneumocystis jiroveciiis an opportunistic pathogen that causes serious pneumonia in immunosuppressed patients. Standard therapy and prophylaxis include trimethoprim (TMP)-sulfamethoxazole; trimethoprim in this combination targets dihydrofolate reductase (DHFR). Fourteen clinically observed variants ofP. jiroveciiDHFR were produced recombinantly to allow exploration of the causes of clinically observed failure of therapy and prophylaxis that includes trimethoprim. Six DHFR variants (S31F, F36C, L65P, A67V, V79I, and I158V) showed resistance to inhibition by trimethoprim, withKivalues fo
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Boese, Austin, Isabelle Young, Jihoon Kang, Courteney Malin, Jung Seok Hwang, and Sumin Kang. "Abstract 2334: Inhibition of DHFR modulates anti-tumor immunity." Cancer Research 82, no. 12_Supplement (2022): 2334. http://dx.doi.org/10.1158/1538-7445.am2022-2334.

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Abstract Lung cancer is the second most common type of cancer in both men and women and has the highest mortality rate. Non-small cell lung cancer (NSCLC) makes up most cases. Immune checkpoint inhibitors have significantly improved the clinical management of some NSCLC cases, yet many lung cancer patients still fail to respond to conventional immunotherapy. Therefore, more research is needed to characterize cellular pathways contribute to immune checkpoint inhibitor (ICI) resistance in NSCLC patients. Dysregulated cellular metabolism is a common feature of many cancer types, and metabolites a
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Bhoj, Priyanka S., Sandeep P. Bahekar, Shambhavi Chowdhary, et al. "Michael Adduct of Sulfonamide Chalcone Targets Folate Metabolism in Brugia Malayi Parasite." Biomedicines 11, no. 3 (2023): 723. http://dx.doi.org/10.3390/biomedicines11030723.

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A series of Michael adducts of malononitrile and sulfonamide chalcones were synthesized, characterized, and evaluated for their antifilarial activity. Out of 14 compounds, N-(4-(4,4-dicyano-3-p-tolylbutanoyl)phenyl)benzenesulfonamide showed favorable drug-likeness properties with marked antifilarial effects at micro-molar dosages. Apoptosis in Brugia malayi microfilariae was confirmed by EB/AO staining, MTT assay, and cytoplasmic cytochrome c ELISA. Since chalcone and folate synthesis pathways share the same substrate, we hypothesize a structural analogy-based inhibition of folate metabolism b
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Mahnashi, Mater H., B. H. Prabhanjana, Sudarshan Seetammanavar, et al. "Synthesis and in silico studies of some new Schiff bases as antimicrobial and antitubercular agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 141. https://doi.org/10.59467/ijhc.2025.35.141.

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Ten pyridine carbohydrazide Schiff bases (3a-3e) and (5a-5e) were synthesized by refluxing pyridine carbohydrazides 1 and 4 with different ketones in the presence of ethanol and a few drops of glacial acetic acid. The synthesized compounds were biologically screened for antitubercular and antibacterial activity studies. The fit of these compounds within the active sites of the dihydrofolate reductase (DHFR) and enoyl ACP reductase was evaluated using molecular modeling techniques. The findings of the anticipated ADMET investigation showed that the compounds with the given names have drug-like
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Aragaw, Wassihun Wedajo, Brendon M. Lee, Xuan Yang, et al. "Potency boost of a Mycobacterium tuberculosis dihydrofolate reductase inhibitor by multienzyme F420H2-dependent reduction." Proceedings of the National Academy of Sciences 118, no. 25 (2021): e2025172118. http://dx.doi.org/10.1073/pnas.2025172118.

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Triaza-coumarin (TA-C) is a Mycobacterium tuberculosis (Mtb) dihydrofolate reductase (DHFR) inhibitor with an IC50 (half maximal inhibitory concentration) of ∼1 µM against the enzyme. Despite this moderate target inhibition, TA-C shows exquisite antimycobacterial activity (MIC50, concentration inhibiting growth by 50% = 10 to 20 nM). Here, we investigated the mechanism underlying this potency disconnect. To confirm that TA-C targets DHFR and investigate its unusual potency pattern, we focused on resistance mechanisms. In Mtb, resistance to DHFR inhibitors is frequently associated with mutation
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Aboge, Gabriel O., Honglin Jia, Mohamad A. Terkawi, et al. "Cloning, Expression, and Characterization of Babesia gibsoni Dihydrofolate Reductase-Thymidylate Synthase: Inhibitory Effect of Antifolates on Its Catalytic Activity and Parasite Proliferation." Antimicrobial Agents and Chemotherapy 52, no. 11 (2008): 4072–80. http://dx.doi.org/10.1128/aac.00384-08.

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ABSTRACT Dihydrofolate reductase-thymidylate synthase (DHFR-TS) is a well-validated antifolate drug target in certain pathogenic apicomplexans, but not in the genus Babesia, including Babesia gibsoni. Therefore, we isolated, cloned, and expressed the wild-type B. gibsoni dhfr-ts gene in Escherichia coli and evaluated the inhibitory effect of antifolates on its enzyme activity, as well as on in vitro parasite growth. The full-length gene consists of a 1,548-bp open reading frame encoding a 58.8-kDa translated peptide containing DHFR and TS domains linked together in a single polypeptide chain.
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Avunoori, Sravanthi, Nayef Abdulaziz Aldabaan, Ibrahim Ahmed Shaikh, et al. "Synthesis and in silico studies of some new pyrrolylbenzamide derivatives as antitubercular and antimicrobial agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 353. http://dx.doi.org/10.59467/ijhc.2024.34.353.

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Eighteen new pyrrolylbenzamide derivatives (6a-6r) were synthesized by reacting N-(2,5-dimethyl- 1H-pyrrol-1-yl)-4-(2-hydrazineyl-2-oxoethoxy)benzamide (4) with substituted benzoic acids (5a-5r) in the presence of 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate, diisopropyl ethylamine and dimethyl formamide. The produced compounds were subjected to molecular docking studies against the dihydrofolate reductase (DHFR) and InhA mycobacterial enzymes. The compounds were biologically screened for antimycobacterial, and antibacterial activities along with InhA and DHFR enzym
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Batra, Apsara, and V. Girija Sastry. "Extraction of ursolic acid from Ocimum sanctum and synthesis of its novel derivatives: effects on extracellular homocysteine, dihydrofolate reductase activity and proliferation of HepG2 human hepatoma cells." Pteridines 24, no. 3 (2013): 191–99. http://dx.doi.org/10.1515/pterid-2013-0023.

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AbstractThe objective of the present study was to extract ursolic acid (UA) from Ocimum sanctum, to synthesize its bioactive derivatives, evaluate the anti-cancer effect of its derivatives and to establish the possible mechanism of action. In the present report, we extracted UA from whole plant of O. sanctum, synthesized its novel derivatives and investigated their effect on homocysteine metabolism and dihydrofolate reductase (DHFR) activity of HepG2 cells. UA and its derivatives UA-1, UA-2 and UA-3 down-regulated DHFR activity and increased extracellular homocysteine. UA-2 showed significant
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Dissertations / Theses on the topic "DHFR inhibition"

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Volpato, Jordan. "Mutagénèse semi-aléatoire au site actif de la DHFR humaine : création et caractérisation de variantes hautement résistantes au MTX." Thèse, 2008. http://hdl.handle.net/1866/2895.

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La dihydrofolate réductase humaine (DHFRh) est une enzyme essentielle à la prolifération cellulaire. Elle réduit le dihydrofolate en tétrahydrofolate, un co-facteur impliqué dans la biosynthèse des purines et du thymidylate. La DHFRh est une cible de choix pour des agents de chimiothérapie comme le méthotrexate (MTX), inhibant spécifiquement l’enzyme ce qui mène à un arrêt de la prolifération et ultimement à la mort cellulaire. Le MTX est utilisé pour le traitement de plusieurs maladies prolifératives, incluant le cancer. La grande utilisation du MTX dans le milieu clinique a mené au développe
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Book chapters on the topic "DHFR inhibition"

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Jaiswal, Shalini. "Imidazothiazole." In Advances in Bioinformatics and Biomedical Engineering. IGI Global, 2024. http://dx.doi.org/10.4018/979-8-3693-7520-4.ch003.

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Recent research on cancer therapy has revealed that the emergence of malignant cells is caused by several enzyme alterations. such include kinase inhibitors of ErB4 (HER4), B-Raf kinase, and indoleamine 2,3-dioxygenase 1 (IDO1). Researchers discovered that drugs based on imidazothiazoles, and their analogues exhibit more robust anticancer action by inhibiting these enzymatic receptors. In recent times, imidazothiazole scaffold is broadly explored for its anticancer activity, which acts through various mechanisms such as EGFR, B-RAF, DHFR kinase inhibition and tubulin polymerization inhibition
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Bolocan, Natalia, and Gheorghe Duca. "Computational research of dihydroxyfumaric acid and its derivatives with antioxidant activity." In Redox Processes with Electron and Proton Transfer. Moldova State University, 2023. http://dx.doi.org/10.59295/prtep2023_07.

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The present chapter describes the application of computational methods in the research of the isomerization/tautomerization processes of dihydroxyfumaric acid (DHF), for the calculation of global and local reactivity indices of new derivatives of DHF, for the demonstration of the validity of the KID procedure in gas, water and methanol. In the present research, the predictive analysis was performed for the first time by calculation methods of the properties of absorption, distribution, metabolism, excretion and toxicity of the investigated derivatives, which demonstrated ерушк пкгпдшлутуыы. Bi
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Conference papers on the topic "DHFR inhibition"

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Zettlmeiβl, G., H. Ragg, and H. Karges. "EXPRESSION OF BIOLOGICALLY ACTIVE HUMAN ANTITHROMBIN III IN CHINESE HAMSTER OVARY CELLS." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643683.

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Expression of human antithrombin III (AT III) at high levels has been achieved in Chinese hamster ovary (CH0) cells by cotransfection and subsequent coamplification of the transfected sequences. Expression vectors containing the AT III cDNA gene and a dihydrofolate reductase (DHFR) cDNA gene were transfected into CH0 DHFR-deficient cells. About 20% of the DHFR+ transformants secreted recombinant human AT III into the medium. Stepwise selection of the AT III producing DHFR+ -transformants in increasing concentrations of methotrexate generated cells which had amplified the AT III géne. We determ
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Duartey, K. O., A. K. Quainoo, and C. K. Darko. "Evaluation Studies of KCl and Amino Acid Mixtures for Clay Stabilization and Rheological Enhancement of Water-Based Fracturing Fluids." In SPE Nigeria Annual International Conference and Exhibition. SPE, 2023. http://dx.doi.org/10.2118/217118-ms.

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Summary Conventional stabilizers such as inorganic salts in water-based fluids are restricted for use in gas and oil shales drilling and hydraulic fracturing for drilling due to environmental, economic and performance concerns. For example, 2% use of KCl, a commonly used inorganic salt, contains an excess of 9500ppm chloride. This is considered high and toxic. Apart from environmental problems, KCl inhibiting solutions tend to negatively affect the rheology of the water-based fluids, posing a dilemma for industry operators. The clay and rheological stabilizing effects of KCl and amino acid mix
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Alfon, Jose, Jordi Espadaler, Jose A. García-Martínez, Jose Miguel Lizcano, and Carles Domènech. "Abstract 922: ABTL0812: A new drug class with oral antitumor action inhibiting mTOR activity and DHFR expression." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-922.

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