Results 61 to 70 of about 22,971 (281)
Affinity labeling has been employed as a powerful tool for target protein identification, yet outcomes are often unpredictable due to the inherent protein‐dependent reactivity of electrophilic labels.
Shione Kamoshita, Kaori Sakurai
doaj +1 more source
Photoredox/Nickel Dual Catalysis for C(sp2)-C(sp3) Cross Electrophile Coupling Reaction Using Phenols and Alcohols as the Latent Electrophile Sources [PDF]
Introducing alkyl groups, particularly through innovative C(sp2)-C(sp3) bond-forming methods utilizing abundant feedstocks, holds promise for expanding chemical diversity, especially in drug discovery programs.
Biplab, Maji +4 more
core +2 more sources
Electrophile Scanning Reveals Reactivity Hotspots for the Design of Covalent Peptide Binders [PDF]
Protein–protein interactions (PPIs) are intriguing targets in drug discovery and development. Peptides are well suited to target PPIs, which typically present with large surface areas lacking distinct features and deep binding pockets. To improve binding
Jeffrey Y. K., Wong +11 more
core +2 more sources
A 3D Multitask Graph Neural Network Framework for Ames Mutagenicity Prediction
Our proposed multitask graph neural network model has a high predictive accuracy for Ames mutagenicity. By operating directly on molecular graph representations instead of traditional molecular descriptors, and predicting strain‐specific results, the model outperforms most existing benchmarks.
Abigail E. Teitgen +3 more
wiley +1 more source
Double Reduction of Ph3B to a Dianionic Borane With a Powerful SrI Intermediate
Although dianionic boranes follow the octet rule and are isoelectronic to carbanions or amines, the high electron density combined with the electropositive nature of the B center make them highly unstable species. In this study, we present synthesis and full characterization of a complex in which Ph3B2− is sandwiched between two Sr2+ ions and describe ...
Michael Morasch +4 more
wiley +2 more sources
Electrophile-Dependent Reactivity of Lithiated N-Benzylpyrene-1-Carboxamide
In this paper, we describe the lithiation of N-benzylpyrene-1-carboxamide with RLi-TMEDA. We found that the reaction outcome strongly depends on the electrophile used in the quenching step.
Magdalena Ciechańska +4 more
doaj +1 more source
Carbohydrate-Directed Labeling Probes for UV-Independent Chemoproteomic Profiling of Carbohydrate-Protein Interactions. [PDF]
Modular carbohydrate‐directed labeling probes (CDLPs) convert weak carbohydrate–protein interactions into durable covalent tags in live cells without the need for multivalency or UV irradiation. Ligand binding triggers proximity‐enabled, glycan‐releasing acyl transfer to install a click handle for protein tagging and chemoproteomic profiling.
Russolillo MC +7 more
europepmc +2 more sources
Three-Component Friedel–Crafts Alkenylation of Arenes and Heteroarenes with Ynamides and Iodine(III) Electrophile [PDF]
The three-component Friedel–Crafts type functionalization of an arene using an alkyne and an electrophile can offer a strategy for rapidly increasing the molecular complexity of aromatic compounds.
Jun, Kikuchi +3 more
core +2 more sources
Oncogenic MYC is a transcription factor that is difficult to inhibit. However, precise positioning of an acrylamide electrophile in MAX to covalently bond to the unique Cys438 in MYC, enabled shortening and optimizing of MAX‐derived, helix‐constrained peptides with high‐affinity and selectivity.
Aline Dantas de Araujo +7 more
wiley +2 more sources
The enzymatic oxidation of arachidonic acid is proposed to yield trihydroxytetraene species (termed lipoxins) that resolve inflammation via ligand activation of the formyl peptide receptor, FPR2.
Adolf Koudelka +11 more
doaj +1 more source

