Results 51 to 60 of about 6,190 (152)

Kinase Inhibitor Selectivity Profiling Using Differential Scanning Fluorimetry

, 2011
Fast, robust, and inexpensive screening methods are the heart of drug discovery processes. Moreover, it is useful to have access to several established assay formats, for validation purposes. If a targeted protein is an enzyme, the logical and widely used approach is the direct measurement of the effect of the added ligands on its activity.
Fedorov, O, Niesen, F, Knapp, S
openaire   +2 more sources

Directed evolution of enzymes at the crossroads of tradition and innovation

FEBS Open Bio, EarlyView.
An iterative cycle of data‐driven enzyme optimization comprising four stages: genetic diversification of a template enzyme, expression of protein variants, high‐throughput evaluation, and machine‐learning‐guided redesign of the next variant library.
Maria Tomkova, Andrej Mirossay, Erik Sedlak   +2 more
wiley   +1 more source

Persulfide Dioxygenase From Acidithiobacillus caldus: Variable Roles of Cysteine Residues and Hydrogen Bond Networks of the Active Site

Frontiers in Microbiology, 2018
Persulfide dioxygenases (PDOs) are abundant in Bacteria and also crucial for H2S detoxification in mitochondria. One of the two pdo-genes of the acidophilic bacterium Acidithiobacillus caldus was expressed in Escherichia coli.
Patrick Rühl, Patrick Haas, Dominik Seipel, Jan Becker, Arnulf Kletzin   +4 more
doaj   +1 more source

A Phase‐Resolved Geometric Deep Learning Framework Maps Structural Determinants of Disease‐Associated Protein Aggregation and Guides Suppressor Design

Advanced Science, EarlyView.
SKALE 2.0 maps disease‐associated protein aggregation as a phase‐resolved structural process, linking mutation‐induced geometric perturbations to nucleation, elongation, and suppressor design. Across neurodegenerative proteins, the framework reveals cryptic aggregation vulnerabilities, separates phase‐concordant and phase‐switching mutations, and ...
Jia Shen Sio, Wei Xuan Wilson Loo, Yan Shan Loo, Wen Xin Tan, Hui Xuan Lim, Huitao Liu, Chen Seng Ng   +6 more
wiley   +1 more source

Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
In various malaria-endemic regions, the appearance of resistance has precluded the use of pyrimidine-based antifolate drugs. Here, a three-step fragment screening was used to identify new non-pyrimidine Plasmodium falciparum dihydrofolate reductase ...
Marie Hoarau, Jarunee Vanichtanankul, Nitipol Srimongkolpithak, Danoo Vitsupakorn, Yongyuth Yuthavong, Sumalee Kamchonwongpaisan   +5 more
doaj   +1 more source

Automation and Active Learning for the Multi‐Objective Optimization of Antibody Formulations

Advanced Science, EarlyView.
Successful antibody formulation necessitates balancing factors such as thermal stability, colloidal stability, and viscosity across a vast excipient design space. This work integrates robotic liquid handling, high‐throughput biophysical characterization, and multi‐objective Bayesian optimization in an iterative closed‐loop Design‐Build‐Test‐Learn cycle.
D. Christopher Radford, Matthew Tamasi, Elena Di Mare, Adam J. Gormley   +3 more
wiley   +1 more source

Excess of guide RNA reduces knockin efficiency and drastically increases on-target large deletions

iScience, 2023
Summary: CRISPR-Cas9 cleavage efficacy and accuracy are the main challenges gene editing faces, and they are particularly affected by the optimal formation of the ribonucleoprotein (RNP) complex.
Vanessa Chenouard, Isabelle Leray, Laurent Tesson, Severine Remy, Alasdair Allan, Daniel Archer, Adam Caulder, Agnès Fortun, Karine Bernardeau, Yacine Cherifi, Lydia Teboul, Laurent David, Ignacio Anegon   +12 more
doaj   +1 more source

Membrane‐Active Peptide Protects Against Inflammation by Targeting NLRP3 Activation at the Trans‐Golgi Network

Advanced Science, EarlyView.
The membrane‐active peptide Pep19‐2.5 reduces harmful inflammation by blocking activation of the NLRP3 inflammasome at trans‐Golgi network membranes. By targeting key membrane interactions, Pep19‐2.5 suppresses inflammatory IL‐1β production and alleviates allergic airway inflammation in mice, leading to reduced immune cell infiltration and improved ...
Jonas Engelhardt, Nico Kirsch, Aileen Kerfin, Lars P. Lunding, Dominic Ferber, Hannes Buthmann, Ilka Schreier, Carlotta Bosio, Ann‐Kathrin Dobbelstein, Anna Klawonn, Rebecca C. Coll, Lena Bauernhofer, Sandro Keller, Matthias Geyer, Michael Wegmann, Andra B. Schromm, Günther Weindl   +16 more
wiley   +1 more source

Sulfated polysaccharides interact with fibroblast growth factors and protect from denaturation

FEBS Open Bio, 2019
Fibroblast growth factors (FGFs) regulate embryonic development and homeostasis, including tissue and organ repair and specific aspects of metabolism.
Changye Sun, Mengxin Liu, Panwen Sun, Mingming Yang, Edwin A. Yates, Zhikun Guo, David G. Fernig   +6 more
doaj   +1 more source

Synthesis of Novel Halogenated Heterocycles Based on o-Phenylenediamine and Their Interactions with the Catalytic Subunit of Protein Kinase CK2

Molecules, 2021
Protein kinase CK2 is a highly pleiotropic protein kinase capable of phosphorylating hundreds of protein substrates. It is involved in numerous cellular functions, including cell viability, apoptosis, cell proliferation and survival, angiogenesis, or ER ...
Maria Winiewska-Szajewska, Agnieszka Monika Maciejewska, Elżbieta Speina, Jarosław Poznański, Daniel Paprocki   +4 more
doaj   +1 more source