Covalent aptamers: agents with promising therapeutic and diagnostic potential. [PDF]
Albright S +3 more
europepmc +1 more source
Neuartige Methoden zur benzylischen Funktionalisierung von Phthalan-Cr(CO)3-Komplexen und deren Anwendung in der stereoselektiven Synthese von cis- und trans-1,3-disubstituierten Dihydroisobenzofuranen [PDF]
Zemolka, Saskia
core
Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways
Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck +1 more
wiley +1 more source
DNA-Protein Cross-Link Formation and Cellular Toxicity by Chimeric Bis-Electrophiles. [PDF]
Yu H, Jiang X, Greenberg MM.
europepmc +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Electrochemically cooperative halogen-cation delivery enables modular electrophilic haloesterification of both activated and unactivated alkenes. [PDF]
Xu HH +5 more
europepmc +1 more source
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Heterobenzyl Chlorides as Linchpins for C-H Arylation via Sequential C-H Chlorination/Cross-Electrophile Coupling. [PDF]
Floreancig JT +6 more
europepmc +1 more source
Abstract Background and Purpose Allergic contact dermatitis (ACD) is a frequent inflammatory skin disease with limited therapeutic options. While neuronal Transient Receptor Potential Ankyrin 1 (TRPA1) has been implicated in ACD, the role of keratinocyte TRPA1 remains unclear.
Areej Jaber +8 more
wiley +1 more source
Unveiling the reaction mechanism and the regioselectivity of Diels-Alder cycloadditions between 2-methoxy-3-thiophenylbutadiene and methyl vinyl ketone using topological tools. [PDF]
Chellegui M +4 more
europepmc +1 more source

