The emerging inverse electron demand Diels–Alder (IEDDA) reaction stands out from other
bioorthogonal reactions by virtue of its unmatchable kinetics, excellent orthogonality and …

Despite advances in genetic and proteomic techniques, a complete portrait of the proteome
and its complement of dynamic interactions and modifications remains a lofty, and as of yet …

Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …

The Bromo-and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …

Small molecules can serve as leads for new therapeutics as well as powerful tools to
investigate biological processes. Understanding the interactions of these molecules …

Protein-protein interactions (PPIs) trigger a wide range of biological signaling pathways that
are crucial for biomedical research and drug discovery. Various techniques have been used …

Natural products and synthetic small molecules can be used to perturb, dissect and
manipulate biological processes, thereby providing the basis for drug development. Over the …

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 …

Over half of new therapeutic approaches fail in clinical trials due to a lack of target validation.
As such, the development of new methods to improve and accelerate the identification of …

The bioorthogonality of tetrazole photoclick chemistry has been reassessed. Upon
photolysis of a tetrazole, the highly reactive nitrile imine formed undergoes rapid …