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 …

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 …

A proteome-wide atlas of lysine-reactive chemistry

ME Abbasov, ME Kavanagh, TA Ichu, MR Lazear… - Nature …, 2021 - nature.com
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 …

Direct map** 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 …

Detecting diagnostic features in MS/MS spectra of post-translationally modified peptides

DJ Geiszler, DA Polasky, F Yu, AI Nesvizhskii - Nature Communications, 2023 - nature.com
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 …

CysDB: a human cysteine database based on experimental quantitative chemoproteomics

LM Boatner, MF Palafox, DK Schweppe… - Cell Chemical …, 2023 - cell.com
Cysteine chemoproteomics provides proteome-wide portraits of the ligandability or potential"
druggability" for thousands of cysteine residues. Consequently, these studies are facilitating …

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 …

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 …

Oxidative cyclization reagents reveal tryptophan cation–π interactions

X ** covalent ligands for functional allosteric methionine sites: redox-dependent inhibition of cyclin …
A Gonzalez-Valero, AG Reeves… - Journal of the …, 2022 - ACS Publications
Activity-based protein profiling (ABPP) is a versatile strategy for identifying and
characterizing functional protein sites and compounds for therapeutic development …