NDLI: Sulfonyl fluorides as privileged warheads in chemical biology

Content Provider	Royal Society of Chemistry (RSC)
Author	Jones, Lyn H. Narayanan, Arjun
Copyright Year	2015
Abstract	Sulfonyl fluoride electrophiles have found significant utility as reactive probes in chemical biology and molecular pharmacology. As warheads they possess the right balance of biocompatibility (including aqueous stability) and protein reactivity. Their functionality is privileged in this regard as they are known to modify not only reactive serines (resulting in their common use as protease inhibitors), but also context-specific threonine, lysine, tyrosine, cysteine and histidine residues. This review describes the application of sulfonyl fluoride probes across various areas of research and explores new approaches that could further enhance the chemical biology toolkit. We believe that sulfonyl fluoride probes will find greater utility in areas such as covalent enzyme inhibition, target identification and validation, and the mapping of enzyme binding sites, substrates and protein–protein interactions.
Starting Page	2650
Ending Page	2659
Page Count	10
File Format	HTM / HTML PDF
ISSN	20416520
Volume Number	6
Issue Number	5
Journal	Chemical Science
DOI	10.1039/c5sc00408j
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Subscribed
Subject Keyword	Tyrosine Cysteine Threonine Enzyme Protease inhibitor (pharmacology) Enzyme inhibitor Pharmacology Protein Fluoride Histidine Lysine Covalent bond Biocompatibility Sulfonyl Molecular biology
Content Type	Text
Resource Type	Article
Subject	Chemistry

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Covalent Inhibitors of Protein–Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues

Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development.

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Unexpected Activity of a Novel Kunitz-type Inhibitor

Systematic Exploration of Privileged Warheads for Covalent Kinase Drug Discovery.

Unexpected Activity of a Novel Kunitz-type Inhibitor INHIBITION OF CYSTEINE PROTEASES BUT NOT SERINE PROTEASES

s as privileged warheads in chemical biology

Sulfonyl fluorides as privileged warheads in chemical biology

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