Light‐Wavelength‐Based Quantitative Control of Dihydrofolate Reductase Activity by Using a Photochromic Isostere of an Inhibitor
Sign Up to like & getrecommendations! Published in 2019 at "ChemBioChem"
DOI: 10.1002/cbic.201800816
Abstract: Photopharmacology has attracted research attention as a new tool for achieving optical control of biomolecules, following the methods of caged compounds and optogenetics. We have developed an efficient photopharmacological inhibitor—azoMTX—for Escherichia coli dihydrofolate reductase (eDHFR)… read more here.
Keywords: inhibitor; dihydrofolate reductase; control; activity ... See more keywords
Molecular Docking Studies, Synthesis and Biological Evaluation of Substituted Pyrimidine‐2,4‐diamines as Inhibitors of Plasmodium falciparum Dihydrofolate Reductase
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200418
Abstract: A series of 5‐[(phenethylamino)methyl]pyrimidine‐2,4‐diamines were assessed in silico as potential inhibitors of Plasmodium falciparum dihydrofolate reductase (PfDHFR), synthesised and tested for inhibitory activity against PfDHFR in vitro. The compounds displayed promising inhibitory activity against both wild‐type… read more here.
Keywords: plasmodium falciparum; falciparum dihydrofolate; inhibitors plasmodium; pyrimidine diamines ... See more keywords
Distal Regions Regulate Dihydrofolate Reductase-Ligand Interactions.
Sign Up to like & getrecommendations! Published in 2021 at "Methods in molecular biology"
DOI: 10.1007/978-1-0716-1154-8_12
Abstract: Protein motions play a fundamental role in enzyme catalysis and ligand binding. The relationship between protein motion and function has been extensively investigated in the model enzyme dihydrofolate reductase (DHFR). DHFR is an essential enzyme… read more here.
Keywords: protein; dihydrofolate reductase; ligand interactions; ligand binding ... See more keywords
High rate of antimicrobial resistance and multiple mutations in dihydrofolate reductase gene among Streptococcus pneumoniae isolated from HIV-infected adults in a community setting in Tanzania.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of global antimicrobial resistance"
DOI: 10.1016/j.jgar.2020.06.026
Abstract: OBJECTIVES This study characterizes the molecular mechanisms of trimethoprim resistance and antibiotics resistance of Streptococcus pneumoniae isolates from HIV-infected adults in Dar es Salaam, Tanzania. METHODS A total of 1877 nasopharyngeal swabs were collected and… read more here.
Keywords: dihydrofolate reductase; streptococcus pneumoniae; resistance; mutations dihydrofolate ... See more keywords
Characterization of Plasmodium knowlesi dihydrofolate reductase-thymidylate synthase and sensitivity to antifolates.
Sign Up to like & getrecommendations! Published in 2018 at "Parasitology international"
DOI: 10.1016/j.parint.2018.08.004
Abstract: Malaria caused by an infection of Plasmodium knowlesi can result in high parasitemia and deaths. Therefore, effective and prompt treatment is necessary to reduce morbidity and mortality. The study aims to characterize P. knowlesi dihydrofolate… read more here.
Keywords: sensitivity antifolates; reductase thymidylate; dihydrofolate reductase; knowlesi dihydrofolate ... See more keywords
Small Angle Neutron Scattering Studies of R67 Dihydrofolate Reductase, a Tetrameric Protein with Intrinsically Disordered N-Termini
Sign Up to like & getrecommendations! Published in 2017 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b00822
Abstract: R67 dihydrofolate reductase (DHFR) is a homotetramer with a single active site pore and no sequence or structural homology with chromosomal DHFRs. The R67 enzyme provides resistance to trimethoprim, an active site-directed inhibitor of Escherichia… read more here.
Keywords: protein; dhfr; dihydrofolate reductase; r67 dihydrofolate ... See more keywords
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01754
Abstract: A safer treatment for toxoplasmosis would be achieved by improving the selectivity and potency of dihydrofolate reductase (DHFR) inhibitors, such as pyrimethamine (1), for Toxoplasma gondii DHFR ( TgDHFR) relative to human DHFR ( hDHFR).… read more here.
Keywords: treatment toxoplasmosis; dihydrofolate reductase; toxoplasma gondii; selectivity ... See more keywords
Single-Molecule Sampling of Dihydrofolate Reductase Shows Kinetic Pauses and an Endosteric Effect Linked to Catalysis
Sign Up to like & getrecommendations! Published in 2022 at "ACS Catalysis"
DOI: 10.1021/acscatal.1c04388
Abstract: The ability to sample multiple reactions on the same single enzyme is important to link rare intermediates with catalysis and to unravel the role of conformational changes. Despite decades of efforts, however, the single-molecule characterization… read more here.
Keywords: catalysis; dihydrofolate reductase; single molecule; endosteric effect ... See more keywords
Structural Insight into Effective Inhibitors' Binding to Toxoplasma gondii Dihydrofolate Reductase Thymidylate Synthase.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.1c00627
Abstract: Pyrimethamine (Pyr), a known dihydrofolate reductase (DHFR) inhibitor, has long been used to treat toxoplasmosis caused by Toxoplasma gondii (Tg) infection. However, Pyr is effective only at high doses with associated toxicity to patients, calling… read more here.
Keywords: thymidylate synthase; gondii; toxoplasma gondii; dhfr ... See more keywords
Arylazopyrazole-Based Photoswitchable Inhibitors Selective for Escherichia coli Dihydrofolate Reductase.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00749
Abstract: Selective inhibitors of Escherichia coli dihydrofolate reductase (eDHFR) are crucial chemical biology tools that have widespread clinical applications. We developed a set of eDHFR-selective photoswitchable inhibitors by derivatizing the structure of our previously reported methotrexate… read more here.
Keywords: coli dihydrofolate; escherichia coli; photoswitchable inhibitors; biology ... See more keywords
Synthesis, Antitumor Activity, and In Silico Drug Design of New Thieno[2,3-d]Pyrimidine-4-One Derivatives as Nonclassical Lipophilic Dihydrofolate Reductase Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c06078
Abstract: Synthesis of a new series of 20 compounds bearing the thieno[2,3-d]pyrimidine-4-one scaffold was achieved. The inhibitory activity of these compounds was performed over 60 cell lines of human tumor at single and five dose concentrations.… read more here.
Keywords: antitumor; thieno pyrimidine; pyrimidine one; activity ... See more keywords