Results 21 to 30 of about 23,665 (170)

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

Anticancer Activities of Seven Peronemins (A2, A3, B1, B2, B3, C1, and D1) from Peronema canescens Jack: A Prediction Studies

Chempublish Journal, 2023
Cancer is one of the leading causes of human death. In 2019, it was reported that cancer was the second (22%) cause of death due to non-communicable diseases in the world's population.
Muhammad Fikriansyah, Nelson, Madyawati Latief, Indra Lasmana Tarigan   +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

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

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

CREAT: A CRISPR‐Based Genome Trimming Strategy for Systematic Identification of Dispensable Regions and Rapid Genome Reduction

Advanced Science, EarlyView.
Current genome‐reduction methods work in a trial‐and‐error fashion, constituting a long‐standing bottleneck in the research. We developed CREAT (CRISPR‐based genome trimming with a multi‐homology‐arm template), a CRISPR‐based genetic approach that enables systematically classifying essential versus non‐essential genomic regions and subsequently ...
Guanhua Yuan, Zhe Gao, Yingxuan Qi, Yang Zhang, Xuhui Tian, Pengpeng Zhao, Xu Feng, Qunxin She   +7 more
wiley   +1 more source

Inosine‐Triphosphate‐Pyrophosphatase Activity as a Potential Predictor of Methotrexate Remission in Juvenile Idiopathic Arthritis

Arthritis &Rheumatology, EarlyView.
Objective Methotrexate (MTX) is the first‐line therapy for juvenile idiopathic arthritis (JIA), but up to 40% of patients do not respond to it. Low inosine triphosphate pyrophosphatase (ITPA) activity has been associated with reduced clinical remission. We investigated the role and underlying mechanisms of ITPA in vitro. Methods ITPA enzymatic activity
Sofia Sindici Forgiarini, Marianna Lucafò, Debora Curci, Davide Selvestrel, Valentina Moressa, Sofia Pagarin, Barbara Bellich, Martina Franzin, Alberto Tommasini, Mara L. Becker, Laura B. Ramsey, Susan D. Thompson, Carl D. Langefeld, Federica Corba, Edoardo Marrani, Gabriele Simonini, Gabriele Stocco, Giuliana Decorti, Andrea Taddio, Serena Pastore   +19 more
wiley   +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

Harnessing ferroptosis from multilayer defense networks to nanoplatforms for specific cancer therapy

BMEMat, EarlyView.
Nanomaterials target metabolically‐regulated ferroptosis for cancer therapy. Iron‐based or alternative nanoplatforms integrate ferroptosis with chemotherapy, immunotherapy, or radiotherapy. They enable stimulus‐responsive therapies (photothermal, photodynamic, sonodynamic) activated by near‐infrared, light, or ultrasound, achieving potent synergistic ...
Xinyue Xu, Xuejian Wang, Wenyan Jiang, Wan Hairul Anuar Kamaruddin, Chunyan Fang, Pengfei Zhang   +5 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