Design and synthesis of minimalist terminal alkyne‐containing diazirine photo‐crosslinkers and their incorporation into kinase inhibitors for cell‐and tissue‐based …
Photoaffinity labeling (PAL) is a powerful technique in chemical biology and chemical
proteomics, and has been successfully demonstrated on a variety of non-covalent molecular …
proteomics, and has been successfully demonstrated on a variety of non-covalent molecular …
Recent applications of diazirines in chemical proteomics
MW Halloran, JP Lumb - Chemistry–A European Journal, 2019 - Wiley Online Library
The elucidation of substrate–protein interactions is an important component of the drug
development process. Due to the complexity of native cellular environments, elucidating …
development process. Due to the complexity of native cellular environments, elucidating …
A Suite of “Minimalist” Photo‐Crosslinkers for Live‐Cell Imaging and Chemical Proteomics: Case Study with BRD4 Inhibitors
Affinity‐based probes (AfBPs) provide a powerful tool for large‐scale chemoproteomic
studies of drug–target interactions. The development of high‐quality probes capable of …
studies of drug–target interactions. The development of high‐quality probes capable of …
Design and evaluation of a cyclobutane Diazirine Alkyne tag for photoaffinity labeling in cells
AV West, Y Amako, CM Woo - Journal of the American Chemical …, 2022 - ACS Publications
Alkyl diazirines are frequently used in photoaffinity labeling to map small molecule–protein
interactions in target identification studies. However, the alkyl diazirines can preferentially …
interactions in target identification studies. However, the alkyl diazirines can preferentially …
Fishing for drug targets: a focus on diazirine photoaffinity probe synthesis
JR Hill, AAB Robertson - Journal of medicinal chemistry, 2018 - ACS Publications
Target identification is a high-priority, albeit challenging, aspect of drug discovery. Diazirine-
based photoaffinity probes (PAPs) can facilitate the process by covalently capturing transient …
based photoaffinity probes (PAPs) can facilitate the process by covalently capturing transient …
A whole proteome inventory of background photocrosslinker binding
P Kleiner, W Heydenreuter, M Stahl… - Angewandte Chemie …, 2017 - Wiley Online Library
Affinity‐based protein profiling (AfBPP) is a widely applied method for the target
identification of bioactive molecules. Probes containing photocrosslinkers, such as …
identification of bioactive molecules. Probes containing photocrosslinkers, such as …
Labeling preferences of diazirines with protein biomolecules
AV West, G Muncipinto, HY Wu, AC Huang… - Journal of the …, 2021 - ACS Publications
Diazirines are widely used in photoaffinity labeling (PAL) to trap noncovalent interactions
with biomolecules. However, design and interpretation of PAL experiments is challenging …
with biomolecules. However, design and interpretation of PAL experiments is challenging …
Target identification by diazirine photo‐cross‐linking and click chemistry
AL MacKinnon, J Taunton - Current protocols in chemical …, 2009 - Wiley Online Library
Target identification is often the rate‐determining step in deciphering the mechanism of
action of biologically active small molecules. Photo‐affinity labeling (PAL) represents a …
action of biologically active small molecules. Photo‐affinity labeling (PAL) represents a …
Evaluation of fully-functionalized diazirine tags for chemical proteomic applications
The use of photo-affinity reagents for the mapping of noncovalent small molecule–protein
interactions has become widespread. Recently, several 'fully-functionalized'(FF) chemical …
interactions has become widespread. Recently, several 'fully-functionalized'(FF) chemical …
2-Aryl-5-carboxytetrazole as a new photoaffinity label for drug target identification
A Herner, J Marjanovic, TM Lewandowski… - Journal of the …, 2016 - ACS Publications
Photoaffinity labels are powerful tools for dissecting ligand–protein interactions, and they
have a broad utility in medicinal chemistry and drug discovery. Traditional photoaffinity …
have a broad utility in medicinal chemistry and drug discovery. Traditional photoaffinity …
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