Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Sulfonyl fluorides as targets and substrates in the development of new synthetic methods

TSB Lou, MC Willis - Nature Reviews Chemistry, 2022 - nature.com
The advent of sulfur (vi)-fluoride exchange (SuFEx) processes as transformations with click-
like reactivity has invigorated research into electrophilic species featuring a sulfur–fluorine …

Direct mapping of ligandable tyrosines and lysines in cells with chiral sulfonyl fluoride probes

Y Chen, GB Craven, RA Kamber, A Cuesta… - Nature Chemistry, 2023 - nature.com
Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …

Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

The growing applications of SuFEx click chemistry

AS Barrow, CJ Smedley, Q Zheng, S Li… - Chemical Society …, 2019 - pubs.rsc.org
SuFEx (Sulfur Fluoride Exchange) is a modular, next generation family of click reactions,
geared towards the rapid and reliable assembly of functional molecules. This review …

Sulfur fluoride exchange

JA Homer, L Xu, N Kayambu, Q Zheng… - Nature Reviews …, 2023 - nature.com
Click chemistry is a conceptual strategy to rapidly synthesize and discover functional
molecules. Sulfur fluoride exchange (SuFEx) is a click reaction that has revolutionized …

Developing bioorthogonal probes to span a spectrum of reactivities

SS Nguyen, JA Prescher - Nature Reviews Chemistry, 2020 - nature.com
Bioorthogonal chemistries enable researchers to interrogate biomolecules in living systems.
These reactions are highly selective and biocompatible, and can be performed in many …

Sulfonyl fluorides as privileged warheads in chemical biology

A Narayanan, LH Jones - Chemical science, 2015 - pubs.rsc.org
Sulfonyl fluoride electrophiles have found significant utility as reactive probes in chemical
biology and molecular pharmacology. As warheads they possess the right balance of …

Chemical protein modification through cysteine

SB Gunnoo, A Madder - ChemBioChem, 2016 - Wiley Online Library
The modification of proteins with non‐protein entities is important for a wealth of
applications, and methods for chemically modifying proteins attract considerable attention …

Broad-spectrum kinase profiling in live cells with lysine-targeted sulfonyl fluoride probes

Q Zhao, X Ouyang, X Wan, KS Gajiwala… - Journal of the …, 2017 - ACS Publications
Protein kinases comprise a large family of structurally related enzymes. A major goal in
kinase-inhibitor development is to selectively engage the desired kinase while avoiding …