Probing the secrets of probes

Review Biotechnology & Applied Microbiology

The emerging role of mass spectrometry-based proteomics in drug discovery

Felix Meissner et al.

Summary: This Review discusses the potential of proteomics and chemoproteomics approaches in drug discovery, specifically in target identification, validation, and identification of safety hazards. The advancements in biochemical methods and mass spectrometry-based proteomics have allowed for a better understanding of disease mechanisms and the development of targeted drugs.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Biochemistry & Molecular Biology

A modification-centric assessment tool for the performance of chemoproteomic probes

Ji-Xiang He et al.

Summary: Chemoproteomics is an important technology for exploring fundamental biology and discovering new small-molecule-based therapies. pChem is a computational tool that can assess the performance of chemoproteomic probes by recognizing isotopically coded probe-derived modifications, calculating masses accurately, and localizing sites precisely. The tool exports reports that score the profiling efficiency, modification homogeneity, and proteome-wide residue selectivity of the tested probe.

NATURE CHEMICAL BIOLOGY (2022)

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Article Chemistry, Multidisciplinary

Labeling Preferences of Diazirines with Protein Biomolecules

Alexander West et al.

Summary: The reactivity of alkyl and aryl diazirines with amino acids, proteins, and the cell proteome was systematically evaluated, revealing different labeling patterns. Alkyl diazirines preferentially label acidic amino acids in a pH-dependent manner, while aryl-fluorodiazirine labeling occurs mainly through a carbene intermediate. These findings help rationalize the enrichment of specific proteins by alkyl diazirine probes and the higher labeling yields of positively charged probes in cells and in vitro.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Review Biochemistry & Molecular Biology