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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 …
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
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 …
A proteome-wide atlas of lysine-reactive chemistry
Recent advances in chemical proteomics have begun to characterize the reactivity and
ligandability of lysines on a global scale. Yet, only a limited diversity of aminophilic …
ligandability of lysines on a global scale. Yet, only a limited diversity of aminophilic …
Direct map** 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 …
Detecting diagnostic features in MS/MS spectra of post-translationally modified peptides
Post-translational modifications are an area of great interest in mass spectrometry-based
proteomics, with a surge in methods to detect them in recent years. However, post …
proteomics, with a surge in methods to detect them in recent years. However, post …
CysDB: a human cysteine database based on experimental quantitative chemoproteomics
Cysteine chemoproteomics provides proteome-wide portraits of the ligandability or potential"
druggability" for thousands of cysteine residues. Consequently, these studies are facilitating …
druggability" for thousands of cysteine residues. Consequently, these studies are facilitating …
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 …
A simple method for develo** lysine targeted covalent protein reagents
R Gabizon, B Tivon, RN Reddi… - Nature …, 2023 - nature.com
Peptide-based covalent probes can target shallow protein surfaces not typically addressable
using small molecules, yet there is a need for versatile approaches to convert native peptide …
using small molecules, yet there is a need for versatile approaches to convert native peptide …
Oxidative cyclization reagents reveal tryptophan cation–π interactions
X ** covalent ligands for functional allosteric methionine sites: redox-dependent inhibition of cyclin …
Activity-based protein profiling (ABPP) is a versatile strategy for identifying and
characterizing functional protein sites and compounds for therapeutic development …
characterizing functional protein sites and compounds for therapeutic development …