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DHFR (dihydrofolate reductase) [PDF]

Atlas of Genetics and Cytogenetics in Oncology and Haematology, 2018
Dihydrofolate reductase (DHFR) is a member of the reductase enzyme family, which is ubiquitously expressed in all organisms. Levels of this enzyme peak at the G1/S cell cycle boundary. Autoregulation, through DHFR-RNA interactions, has also been reported.
Krajinovic, Maja, Abaji, Rachid, Sharif-Askari, Bahram   +2 more
openaire   +2 more sources

Self-organizing Neural Networks for Modeling Robust 3D and 4D QSAR: Application to Dihydrofolate Reductase Inhibitors

Molecules, 2004
We have used SOM and grid 3D and 4D QSAR schemes for modeling the activity of a series of dihydrofolate reductase inhibitors. Careful analysis of the performance and external predictivities proves that this method can provide an efficient inhibition ...
Tomasz Magdziarz, Rafal Gieleciak, Andrzej Bak, Jaroslaw Polanski   +3 more
doaj   +1 more source

Identification of Novel Potential Inhibitors of Pteridine Reductase 1 in Trypanosoma brucei via Computational Structure-Based Approaches and in Vitro Inhibition Assays

Molecules, 2019
Pteridine reductase 1 (PTR1) is a trypanosomatid multifunctional enzyme that provides a mechanism for escape of dihydrofolate reductase (DHFR) inhibition. This is because PTR1 can reduce pterins and folates.
Magambo Phillip Kimuda, Dustin Laming, Heinrich C. Hoppe, Özlem Tastan Bishop   +3 more
doaj   +1 more source

Design, synthesis, and biological evaluation of novel N 4 -substituted sulfonamides: acetamides derivatives as dihydrofolate reductase (DHFR) inhibitors

BMC Chemistry, 2019
Background Sulfonamide derivatives are of great attention due to their wide spectrum of biological activities. Sulfonamides conjugated with acetamide fragments exhibit antimicrobial and anticancer activities. The inhibition dihydrofolate reductase (DHFR)
Essam M. Hussein, Munirah M. Al-Rooqi, Shimaa M. Abd El-Galil, Saleh A. Ahmed   +3 more
doaj   +1 more source

Cinnamomum zeylanicum Extract and its Bioactive Component Cinnamaldehyde Show Anti-Tumor Effects via Inhibition of Multiple Cellular Pathways

Frontiers in Pharmacology, 2022
Cinnamomum zeylanicum is a tropical plant with traditional medicinal significance that possesses antimicrobial, antifungal, anti-parasitic, and anti-tumor properties.
Sadhna Aggarwal, Kanchan Bhadana, Baldeep Singh, Meenakshi Rawat, Taj Mohammad, Lamya Ahmed Al-Keridis, Nawaf Alshammari, Md. Imtaiyaz Hassan, Satya N. Das   +8 more
doaj   +1 more source

A Two-Enzyme Adaptive Unit within Bacterial Folate Metabolism

Cell Reports, 2019
Summary: Enzyme function and evolution are influenced by the larger context of a metabolic pathway. Deleterious mutations or perturbations in one enzyme can often be compensated by mutations to others.
Andrew F. Schober, Andrew D. Mathis, Christine Ingle, Junyoung O. Park, Li Chen, Joshua D. Rabinowitz, Ivan Junier, Olivier Rivoire, Kimberly A. Reynolds   +8 more
doaj   +1 more source

Prediction of Inhibition Activity of Dihydrofolate Reductase Inhibitors With Multivariate Adaptive Regression Splines

IEEE Access, 2023
Dihydrofolate reductase (DHFR) enzyme is a crucial component of cell growth and proliferation in the human body, making it an important target for treating cancer diseases.
Zanib Qayyum, Tahir Mehmood, Laila A. Al-Essa   +2 more
doaj   +1 more source

A silent sulfonamide-resistant microbial world: The curious case of missing DHPS in candidate phyla radiation

Journal of Global Antimicrobial Resistance
Candidate phyla radiation (CPR) microbes exhibit minimal genomes, episymbiotic/parasitic lifestyles, and metabolic dependencies on host cells. In this study, we look for the presence of dihydropteroate synthase (DHPS) and dihydrofolate reductase, key ...
Riyad Razzouk, Adel Azour, Jean-Marc Rolain, Fadi Bittar   +3 more
doaj   +1 more source

Combined gene deletion of dihydrofolate reductase-thymidylate synthase and pteridine reductase in Leishmania infantum.

PLoS Neglected Tropical Diseases, 2021
Our understanding of folate metabolism in Leishmania has greatly benefited from studies of resistance to the inhibitor methotrexate (MTX). Folates are reduced in Leishmania by the bifunctional dihydrofolate reductase thymidylate synthase (DHFR-TS) and by
Arijit Bhattacharya, Philippe Leprohon, Marc Ouellette   +2 more
doaj   +1 more source

Tales of Dihydrofolate Binding to R67 Dihydrofolate Reductase

Biochemistry, 2015
Homotetrameric R67 dihydrofolate reductase possesses 222 symmetry and a single active site pore. This situation results in a promiscuous binding site that accommodates either the substrate, dihydrofolate (DHF), or the cofactor, NADPH. NADPH interacts more directly with the protein as it is larger than the substrate.
Duff, Michael R., Chopra, Shaileja, Strader, Michael Brad, Agarwal, Pratul K., Howell, Elizabeth E.   +4 more
openaire   +2 more sources