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 …
Chemical Diversity of Reagents that Modify RNA 2'-OH in Water: a Review
Electrophilic water-soluble compounds have proven versatile in reacting selectively with 2′-
OH groups in RNA, enabling structure mapping, probing, caging, labeling, crosslinking, and …
OH groups in RNA, enabling structure mapping, probing, caging, labeling, crosslinking, and …
Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1
G Alboreggia, P Udompholkul, C Baggio… - Journal of Medicinal …, 2024 - ACS Publications
Several novel and effective cysteine targeting (Cys) covalent drugs are in clinical use.
However, the target area containing a druggable Cys residue is limited. Therefore, methods …
However, the target area containing a druggable Cys residue is limited. Therefore, methods …
Imidazoles are Tunable Nucleofuges for Developing Tyrosine‐Reactive Electrophiles
Abstract Imidazole‐1‐sulfonyl and‐sulfonate (imidazylate) are widely used in synthetic
chemistry as nucleofuges for diazotransfer, nucleophilic substitution, and cross‐coupling …
chemistry as nucleofuges for diazotransfer, nucleophilic substitution, and cross‐coupling …