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 …

Applications of covalent chemistry in targeted protein degradation

D Lu, X Yu, H Lin, R Cheng, EY Monroy, X Qi… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

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 …

[HTML][HTML] Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D

Q Zheng, Z Zhang, KZ Guiley, KM Shokat - Nature Chemical Biology, 2024 - nature.com
K-Ras is the most commonly mutated oncogene in human cancer. The recently approved
non-small cell lung cancer drugs sotorasib and adagrasib covalently capture an acquired …

[HTML][HTML] Sulfur (VI) fluorides as tools in biomolecular and medicinal chemistry

SN Carneiro, SR Khasnavis, J Lee, TW Butler… - Organic & …, 2023 - pubs.rsc.org
Recent advances in the synthesis of sulfur (VI)-fluorides has enabled incredible growth in
their application in biomolecular chemistry. This review aims to serve as a primer …

Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions

Y Gao, B Jiang, H Kim, MJ Berberich… - Journal of Medicinal …, 2023 - ACS Publications
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …

Profiling sulfur (VI) fluorides as reactive functionalities for chemical biology tools and expansion of the ligandable proteome

KE Gilbert, A Vuorinen, A Aatkar, P Pogány… - ACS chemical …, 2023 - ACS Publications
Here, we report a comprehensive profiling of sulfur (VI) fluorides (SVI-Fs) as reactive groups
for chemical biology applications. SVI-Fs are reactive functionalities that modify lysine …

[HTML][HTML] Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Covalent drugs targeting histidine–an unexploited opportunity?

J Che, LH Jones - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Covalent drugs and chemical probes often possess pharmacological advantages over
reversible binding ligands, such as enhanced potency and pharmacodynamic duration. The …