Lipophilic prodrugs of FR900098 are antimicrobial against Francisella novicida in vivo and in vitro and show GlpT independent efficacy. [PDF]
Bacteria, plants, and algae produce isoprenoids through the methylerythritol phosphate (MEP) pathway, an attractive pathway for antimicrobial drug development as it is present in prokaryotes and some lower eukaryotes but absent from human cells.
Elizabeth S McKenney +8 more
doaj +1 more source
MEP Pathway: First-Synthesized IspH-Directed Prodrugs with Potent Antimycobacterial Activity. [PDF]
We report the first synthesis of IspH-directed prodrugs targeting the terminal enzyme of the 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway, (E)-4-hydroxy-3-methylbut-2-enyl diphosphate reductase (IspH or LytB). A series of alkyne and pyridine monophosphate cycloSaligenyl (cycloSal) prodrugs were prepared to enhance membrane permeability by masking ...
Allamand A +5 more
europepmc +3 more sources
Inhibition of DXR in the MEP pathway with lipophilic <i>N</i>-alkoxyaryl FR900098 analogs. [PDF]
Isoprene biosynthesis is a point of vulnerability for many pathogens. Building on prior work, we report a novel set of potent compounds that display selectivity for P. falciparum over M. tuberculosis, and act on-target intracellularly.
Bague D +10 more
europepmc +3 more sources
Kinetic characterization and phosphoregulation of the Francisella tularensis 1-deoxy-D-xylulose 5-phosphate reductoisomerase (MEP synthase). [PDF]
Deliberate and natural outbreaks of infectious disease underscore the necessity of effective vaccines and antimicrobial/antiviral therapeutics. The prevalence of antibiotic resistant strains and the ease by which antibiotic resistant bacteria can be ...
Safdar Jawaid +7 more
doaj +1 more source
The MEP-pathway genes are polyphyletic origin and evolutionary conserved [PDF]
Abstract BackgroundIsoprenoids are amongst the most ancient and essential class of metabolites produced in all organisms, either via mevalonate (MVA)-and/or methylerythritol dicyclophosphate (MEP)-pathways. The MEP-pathway is present in all plastid-bearing organisms and most eubacteria.
Liping Zeng, Katayoon Dehesh
openaire +1 more source
International audienceTrifluoromethyl analogues of methylerythritol phosphate (MEP) and 2-C-methyl-erythritol 2,4-cyclodiphosphate (MEcPP), natural substrates of key enzymes from the MEP pathway, were prepared starting from d-glucose as the chiral ...
Chaignon, Philippe +7 more
core +2 more sources
Different roles of the mevalonate and methylerythritol phosphate pathways in cell growth and tanshinone production of Salvia miltiorrhiza hairy roots. [PDF]
Salvia miltiorrhiza has been widely used in the treatment of coronary heart disease. Tanshinones, a group of diterpenoids are the main active ingredients in S. miltiorrhiza.
Dongfeng Yang +7 more
doaj +1 more source
Astaxanthin is a powerful antioxidant and is used extensively as an animal feed additive and nutraceutical product. Here, we report the use of the β-carotene hydroxylase (CBFD1) and the β-carotene ketolase (HBFD1) from Adonis aestivalis, a flowering ...
Jared H. Roth, Valerie C. A. Ward
doaj +1 more source
The plastidial MEP pathway: unified nomenclature and resources
In plants, the plastid-localized 2-C-methyl-d-erythritol 4-phosphate (MEP) pathway provides the precursors for the synthesis of isoprenoid hormones, monoterpenes, carotenoids and the side chain of chlorophylls, tocopherols and prenylquinones. As a result of the fast progress in the elucidation and characterization of the pathway (mainly by genetic ...
Phillips, Michael +3 more
openaire +3 more sources
Identification of target genes of the bZIP transcription factor OsTGAP1, whose overexpression causes elicitor-induced hyperaccumulation of diterpenoid phytoalexins in rice cells. [PDF]
Phytoalexins are specialised antimicrobial metabolites that are produced by plants in response to pathogen attack. Momilactones and phytocassanes are the major diterpenoid phytoalexins in rice and are synthesised from geranylgeranyl diphosphate, which is
Koji Miyamoto +8 more
doaj +1 more source

