Results 11 to 20 of about 23,186 (181)

A novel bicyclic 2,4-diaminopyrimidine inhibitor of Streptococcus suis dihydrofolate reductase [PDF]

PeerJ, 2021
Streptococcus suis is a Gram-positive bacterial pathogen of pigs and an emerging zoonotic pathogen. It has become increasingly resistant to multiple classes of antibiotics.
Warangkhana Songsungthong, Sunisa Prasopporn, Louise Bohan, Potjanee Srimanote, Ubolsree Leartsakulpanich, Suganya Yongkiettrakul   +5 more
doaj   +2 more sources

Covalent Protein Inhibitors via Tyrosine and Tryptophan Conjugation with Cyclic Imine Mannich Electrophiles

Angewandte Chemie, EarlyView.
Targeted covalent inhibitors (TCI) containing cyclic imine warheads react with tyrosine and tryptophan residues via the Mannich reaction. These cyclic imine warheads show comparable reaction kinetics to cysteine‐reactive electrophiles commonly used in TCIs.
Sijie Wang, Lei Wang, Marco Hadisurya, Siavash Shahbazi Nia, W. Andy Tao, Emily C. Dykhuizen, Casey J. Krusemark   +6 more
wiley   +2 more sources

MOLECULAR SURVEILLANCE OF Plasmodium vivax AND Plasmodium falciparum DHFR MUTATIONS IN ISOLATES FROM SOUTHERN IRAN

Revista do Instituto de Medicina Tropical de São Paulo, 2016
In Iran, both Plasmodium vivax and P. falciparum malaria have been detected, but P. vivax is the predominant species. Point mutations in dihydrofolate reductase (dhfr) gene in both Plasmodia are the major mechanisms of pyrimethamine resistance.
Khojasteh SHARIFI-SARASIABI, Ali HAGHIGHI, Bahram KAZEMI, Niloofar TAGHIPOUR, Ehsan Nazemalhosseini MOJARAD, Latif GACHKAR   +5 more
doaj   +1 more source

A calibration curve for immobilized dihydrofolate reductase activity assay

Data in Brief, 2015
An assay was developed for measuring the active-site concentration, activity, and thereby the catalytic turnover rate (kcat) of an immobilized dihydrofolate reductase model system (Singh et al., (2015), Anal. Biochem).
Priyanka Singh, Holly Morris, Alexei V. Tivanski, Amnon Kohen   +3 more
doaj   +1 more source

Synthesis, Molecular Docking Study, and Biological Evaluation of New 4-(2,5-Dimethyl-1H-pyrrol-1-yl)-N’-(2-(substituted)acetyl)benzohydrazides as Dual Enoyl ACP Reductase and DHFR Enzyme Inhibitors

Antibiotics, 2023
In this study, a new series of 4-(2,5-dimethyl-1H-pyrrol-1-yl)-N’-(2-(substituted)acetyl) benzohydrazides (5a–n) were prepared and new heterocycles underwent thorough characterization and evaluation for antibacterial activity; some of them underwent ...
Mater H. Mahnashi, Pooja Koganole, Prem Kumar S. R., Sami S. Ashgar, Ibrahim Ahmed Shaikh, Shrinivas D. Joshi, Ali S. Alqahtani   +6 more
doaj   +1 more source

Trimethoprim: An Old Antibacterial Drug as a Template to Search for New Targets. Synthesis, Biological Activity and Molecular Modeling Study of Novel Trimethoprim Analogs

Molecules, 2019
A new series of trimethoprim (TMP) analogs containing amide bonds (1−6) have been synthesized. Molecular docking, as well as dihydrofolate reductase (DHFR) inhibition assay were used to confirm their affinity to bind dihydrofolate reductase enzyme.
Agnieszka Wróbel, Dawid Maliszewski, Maciej Baradyn, Danuta Drozdowska   +3 more
doaj   +1 more source

Tetrahydrobiopterin Uptake in Supplemental Administration: Elevation of Tissue Tetrahydrobiopterin in Mice Following Uptake of the Exogenously Oxidized Product 7,8-Dihydrobiopterin and Subsequent Reduction by an Anti-folate-Sensitive Process

Journal of Pharmacological Sciences, 2004
In order to increase the tissue level of tetrahydrobiopterin (BH4), supplementation with 6R-tetrahydrobiopterin (6RBH4) has been widely employed. In this work, the effectiveness of 6RBH4 was compared with 7,8-dihydrobiopterin (7,8BH2) and sepiapterin by ...
Keiko Sawabe, Kazunori Osuke Wakasugi, Hiroyuki Hasegawa   +2 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

Frequency of Drug Resistance Gene Amplification in Clinical Leishmania Strains

International Journal of Microbiology, 2010
Experimental studies about Leishmania resistance to metal and antifolates have pointed out that gene amplification is one of the main mechanisms of drug detoxification.
C. Mary, F. Faraut, M. Deniau, J. Dereure, K. Aoun, S. Ranque, R. Piarroux   +6 more
doaj   +1 more source

Cell-Cycle-Dependent Pharmacology of Methotrexate in HL-60

Journal of Pharmacological Sciences, 2005
The role of the susceptibility of cells and the pharmacokinetics of MTX on the time-dependent change of methotrexate (MTX) pharmacologic action in HL-60 (human leukemia cell) was investigated from the viewpoints of the rhythm of DNA synthesis.
Atsushi Yamauchi, Takanobu Ichimiya, Kouichi Inoue, Yukie Taguchi, Naoya Matsunaga, Satoru Koyanagi, Tatsuo Fukagawa, Hironori Aramaki, Shun Higuchi, Shigehiro Ohdo   +9 more
doaj   +1 more source