Results 21 to 30 of about 23,657 (193)

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

A novel antifolate suppresses growth of FPGS-deficient cells and overcomes methotrexate resistance

Life Science Alliance, 2023
Mechanistic characterization of a novel, lipophilic antifolate that suppresses growth of FPGS-deficient cells that are linked to methotrexate resistance and relapse in cancer patients.
Felix van der Krift, Dick W Zijlmans, Rhythm Shukla, Ali Javed, Panagiotis I Koukos, Laura LE Schwarz, Elpetra PM Timmermans-Sprang, Peter EM Maas, Digvijay Gahtory, Maurits van den Nieuwboer, Jan A Mol, Ger J Strous, Alexandre MJJ Bonvin, Mario van der Stelt, Edwin JA Veldhuizen, Markus Weingarth, Michiel Vermeulen, Judith Klumperman, Madelon M Maurice   +18 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

Affinity chromatography of dihydrofolate reductase [PDF]

Biochemical Journal, 1971
1. Dihydrofolate reductase was purified from Lactobacillus casei MTX/R, and studied on affinity columns containing folic acid and methotrexate. Two forms of the enzyme were interconverted by incubation with substrates. 2. Affinity columns were prepared from agarose activated with cyanogen bromide and coupled with 1,6-diaminohexane.
P C, Newbold, N G, Harding
openaire   +2 more sources

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

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

Large‐scale bidirectional arrayed genetic screens identify OXR1 and EMC4 as modifiers of αSynuclein aggregation

FEBS Open Bio, EarlyView.
Activation of the mitochondrial protein OXR1 increases pSyn129 αSynuclein aggregation by lowering ATP levels and altering mitochondrial membrane potential, particularly in response to MSA‐derived fibrils. In contrast, ablation of the ER protein EMC4 enhances autophagic flux and lysosomal clearance, broadly reducing α‐synuclein aggregates.
Sandesh Neupane, Lea Nikolić, Lorenzo Maraio, Thomas Goiran, Nathan Karpilovsky, Stefano Sellitto, Vangelis Bouris, Jiang‐An Yin, Ronald Melki, Edward A Fon, Adriano Aguzzi, Elena De Cecco   +11 more
wiley   +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

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