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Inhibition of 5 alpha-reductase and aromatase by the ellagitannins oenothein A and oenothein B from Epilobium species.
TLDR
Quantitation of oenothein B in 10 different species of Epilobium has shown that amounts of up to 14% in the crude plant extracts are possible, and activity-guided fractionation has led to the identification of two macrocyclic ellagitannins, oanothein A and oenethein B, as the main constituents responsible for the inhibition of the two enzymes.
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Allosteric activation of the protein kinase PDK1 with low molecular weight compounds
TLDR
Specific, low molecular weight compounds are developed, which target the HM/PIF‐pocket and have the ability to allosterically activate phosphoinositide‐dependent protein kinase 1 (PDK1) by modulating the phosphorylation‐dependent conformational transition.
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17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development
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Antibiotic-free nanotherapeutics: ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors.
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A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
TLDR
The goal to find new potent inhibitors of aromatase was reached with the xanthone derivatives 22d,e and 22g-i, which exceeded the potency of the known reference drug fadrozole and also showed high selectivity with respect to P450 17.
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Discovery of antagonists of PqsR, a key player in 2-alkyl-4-quinolone-dependent quorum sensing in Pseudomonas aeruginosa.
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The IGF2 mRNA binding protein p62/IGF2BP2-2 induces fatty acid elongation as a critical feature of steatosis[S]
TLDR
P62 represents an inducer of hepatic C18 fatty acid production via a SREBF1-dependent induction of ELOVL6, and decreased palmitoyl-CoA levels, as found in p62 transgenic livers, can explain the lipogenic action of ELovL6.
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Rule–based regulatory and metabolic model for Quorum sensing in P. aeruginosa
TLDR
A modified network topology is suggested in which PqsE and PqsR acts as receptors and an autoinducer as ligand that up–regulate pyocyanin in a concerted manner is suggested.
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Novel Strategies for the Treatment of Pseudomonas aeruginosa Infections.
TLDR
It can be expected that combination therapies, also containing antivirulence agents, will pave the way toward novel treatment options against P. aeruginosa, and antivirulent drugs are expected to yield a significantly reduced rate of resistance development.
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Effects of novel 17α-hydroxylase/C17, 20-lyase (P450 17, CYP 17) inhibitors on androgen biosynthesis in vitro and in vivo
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