Applications of covalent chemistry in targeted protein degradation
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …
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
Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …
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
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 …
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 …
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
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …
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 …
for chemical biology applications. SVI-Fs are reactive functionalities that modify lysine …
[HTML][HTML] Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
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 …
decades, with a variety of new targeted covalent drugs having been approved in recent …
Covalent drugs targeting histidine–an unexploited opportunity?
Covalent drugs and chemical probes often possess pharmacological advantages over
reversible binding ligands, such as enhanced potency and pharmacodynamic duration. The …
reversible binding ligands, such as enhanced potency and pharmacodynamic duration. The …