Results 41 to 50 of about 1,155,277 (319)

Application of biomimetic HPLC to estimate lipophilicity, protein and phospholipid binding of potential peptide therapeutics

ADMET and DMPK, 2018
Peptide therapeutics are new modalities offering several challenges to drug discovery. They are generally less stable and permeable in vivo. The characterization of their lipophilicity cannot be carried out using the traditional in silico or wet octanol ...
Klara Livia Valko, Gabriela Ivanova-Berndt, Paul Beswick, Mark Kindey, Dorothy Ko   +4 more
doaj   +1 more source

Influence of Selected Factors on Antioxidant Properties of Chlorogenic Acid and Kaempferol as Well as Their Binary Mixtures

Applied Sciences, 2023
Plants are a rich source of substances with antioxidant properties, including high amounts of polyphenolic compounds, as well as other substances that do not necessarily have antioxidant properties.
Małgorzata Olszowy-Tomczyk, Dorota Wianowska   +1 more
doaj   +1 more source

Serial amplification of tau filaments using Alzheimer's brain homogenates and C322A or C322S recombinant tau

FEBS Letters, EarlyView.
We investigated the seeded assembly of 0N3R tau and two variants, C322A and C322S, designed to model the mutation landscape at residue 322, using Alzheimer's disease brain homogenates in a real‐time quaking‐induced conversion (RT‐QuIC) assay. The C322A variant formed filaments that partially resembled the paired helical filament (PHF) structure ...
Alessia Santambrogio, Sofia Lövestam, Michael A. Metrick II, Thomas Löhr, Peifeng Xu, Nicholas C. T. Gallagher, Bernardino Ghetti, Byron Caughey, Sjors H. W. Scheres, Michele Vendruscolo   +9 more
wiley   +1 more source

Single cis‐elements in brassinosteroid‐induced upregulated genes are insufficient to recruit both redox states of the BIL1/BZR1 DNA‐binding domain

FEBS Letters, EarlyView.
Phytohormone brassinosteroid‐induced gene regulation by the transcription factor BIL1/BZR1 involves redox‐dependent DNA‐binding alternation and interaction with the transcription factor PIF4. The reduced BIL1/BZR1 dimer binds preferred cis‐elements, while oxidation alters its oligomerization state and disrupts DNA‐binding ability.
Shohei Nosaki, Masae Ohtsuka, Takeshi Nakano, Masaru Tanokura, Takuya Miyakawa   +4 more
wiley   +1 more source

Structural dynamics of the plant hormone receptor ETR1 in a native‐like membrane environment

FEBS Letters, EarlyView.
The present study unveils the structural and signaling dynamics of ETR1, a key plant ethylene receptor. Using an optimized nanodisc system and solution NMR, we captured full‐length ETR1 in a native‐like membrane environment. Our findings reveal dynamic domain uncoupling and Cu(I)‐induced rigidification, providing the first evidence of metal‐triggered ...
Moritz Lemke, Nils Alexander Lakomek, Georg Groth   +2 more
wiley   +1 more source

Mechanistic basis for inhibition of the extended‐spectrum β‐lactamase GES‐1 by enmetazobactam and tazobactam

FEBS Letters, EarlyView.
Antimicrobial resistance (AMR) is of huge importance, resulting in over 1 million deaths each year. Here, we describe how a new drug, enmetazobactam, designed to help fight resistant bacterial diseases, inhibits a key enzyme (GES‐1) responsible for AMR. Our data show it is a more potent inhibitor than the related tazobactam, with high‐level computation
Michael Beer, Philip Hinchliffe, Marko Hanževački, Christopher R. Bethel, Catherine L. Tooke, Marc W. Van der Kamp, Krisztina M. Papp‐Wallace, Robert A. Bonomo, Stuart Shapiro, Adrian J. Mulholland, James Spencer   +10 more
wiley   +1 more source

Determination of pesticide residues in urine by chromatography-mass spectrometry: methods and applications

Frontiers in Public Health
IntroductionPollution has emerged as a significant threat to humanity, necessitating a thorough evaluation of its impacts. As a result, various methods for human biomonitoring have been proposed as vital tools for assessing, managing, and mitigating ...
Willian Garcia Birolli, Willian Garcia Birolli, Fernando Mauro Lanças, Álvaro José dos Santos Neto, Henrique C. S. Silveira   +4 more
doaj   +1 more source

Erratum to the paper: In vitro membrane binding and protein binding (IAM MB/PB technology) to estimate in vivo distribution: applications in early drug discovery

ADMET and DMPK, 2018
The authors of the original paper published with the same title: ADMET & DMPK 5(1) (2017) 14-38; doi: 10.5599/admet.5.1.373, apologize for the error in the plot on Figure 5. The erratum gives a correct plot.
Klara Livia Valko, Simon Teague, Charles Pudgeon   +2 more
doaj   +1 more source

C9orf72 ALS‐causing mutations lead to mislocalization and aggregation of nucleoporin Nup107 into stress granules

FEBS Letters, EarlyView.
Mutations in the C9orf72 gene represent the most common genetic cause of amyotrophic lateral sclerosis (ALS), a fatal neurodegenerative disease. Using patient‐derived neurons and C. elegans models, we find that the nucleoporin Nup107 is dysregulated in C9orf72‐associated ALS. Conversely, reducing Nup107 levels mitigates disease‐related changes.
Saygın Bilican, Yara Nabawi, William Hongyu Zhang, Dunja Petrovic, Markus Wehrmann, Sara Muñoz‐García, Seda Koyuncu, David Vilchez   +7 more
wiley   +1 more source

Chromatographic technique to support ADMET&DMPK in early drug discovery

ADMET and DMPK, 2018
The drug discovery process usually involves the discovery of a potent new chemical entity which has shown some activity on a target that is believed to be relevant in a certain type of disease.
Klara Livia Valko
doaj   +1 more source