Results 21 to 30 of about 217,358 (308)

Identification of novel Mycobacterium tuberculosis dihydrofolate reductase inhibitors through rational drug design

open access: yesInternational Journal of Mycobacteriology, 2016
Objectives/Background: Dihydrofolate reductase (DHFR) is one of the validated drug targets in Mycobacterium tuberculosis (Mtb) infection. DHFR inhibitors have been used to treat various life-threatening diseases such as cancer, malaria, and several ...
Mymoona Akhter
doaj   +1 more source

A designed phenylalanyl-tRNA synthetase variant allows efficient in vivo incorporation of aryl ketone functionality into proteins [PDF]

open access: yes, 2002
Incorporation of non-natural amino acids into proteins in vivo expands the scope of protein synthesis and design. p-Acetylphenylalanine was incorporated into recombinant dihydrofolate reductase (DHFR) in Escherichia coli via a computationally designed ...
Carrico, Isaac S.   +4 more
core   +2 more sources

Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.

open access: yesJournal of Medicinal Chemistry, 2019
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).
Allen T. Hopper   +8 more
semanticscholar   +1 more source

Mining electron density for functionally relevant protein polysterism in crystal structures. [PDF]

open access: yes, 2010
This review focuses on conceptual and methodological advances in our understanding and characterization of the conformational heterogeneity of proteins.
Fraser, James S, Jackson, Colin J
core   +3 more sources

A trimethoprim derivative impedes antibiotic resistance evolution

open access: yesNature Communications, 2021
The efficacy of the antibiotic trimethoprim, which inhibits bacterial dihydrofolate reductase (DHFR), is limited by the rapid emergence of resistant bacteria. Here, Manna et al.
Madhu Sudan Manna   +15 more
doaj   +1 more source

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

open access: yesPeerJ, 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   +5 more
doaj   +2 more sources

A-to-I RNA Editing Up-regulates Human Dihydrofolate Reductase in Breast Cancer*

open access: yesJournal of Biological Chemistry, 2017
Dihydrofolate reductase (DHFR) plays a key role in folate metabolism and is a target molecule of methotrexate. An increase in the cellular expression level of DHFR is one of the mechanisms of tumor resistance to methotrexate.
Masataka Nakano   +3 more
semanticscholar   +1 more source

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

open access: yesRevista 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   +5 more
doaj   +1 more source

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

open access: yesAngewandte 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   +6 more
wiley   +2 more sources

Plasmodium dihydrofolate reductase is a second enzyme target for the antimalarial action of triclosan

open access: yesScientific Reports, 2018
Malaria, caused by parasites of the genus Plasmodium, leads to over half a million deaths per year, 90% of which are caused by Plasmodium falciparum. P. vivax usually causes milder forms of malaria; however, P.
E. Bilsland   +12 more
semanticscholar   +1 more source

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