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 …

An activity-based oxaziridine platform for identifying and developing 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 …

Discovery of potent and selective inhibitors against protein-derived electrophilic cofactors

X Wang, Z Lin, KA Bustin, NR McKnight… - Journal of the …, 2022 - ACS Publications
Electrophilic cofactors are widely distributed in nature and play important roles in many
physiological and disease processes, yet they have remained blind spots in traditional …

Developing an Affinity-Based Chemical Proteomics Method to In Situ Capture Amorphous Aggregated Proteome and Profile Its Heterogeneity in Stressed Cells

D Shen, Q Zhao, M Wang, B Zhong, W Jin… - Analytical …, 2023 - ACS Publications
Stress induced amorphous proteome aggregation is a hallmark for diseased cells, with the
proteomic composition intimately associated with disease pathogenicity. Due to its …

[HTML][HTML] CySP3-96 enables scalable, streamlined, and low-cost sample preparation for cysteine chemoproteomic applications

F Shikwana, BS Heydari, S Ofori, C Truong… - Molecular & Cellular …, 2024 - Elsevier
Cysteine chemoproteomic screening platforms are widely utilized for chemical probe and
drug discovery campaigns. Chemoproteomic compound screens, which use a mass …

Protein oxidation of fucose environments (POFE) reveals fucose–protein interactions

Y Xie, S Chen, MR Alvarez, Y Sheng, Q Li… - Chemical …, 2024 - pubs.rsc.org
Cell membrane glycoproteins are generally highly fucosylated and sialylated, and post-
translational modifications play important roles in the proteins' functions of signaling, binding …

Automation to Enable High-Throughput Chemical Proteomics

Z Lin, J Gongora, X Liu, Y Xie, C Zhao… - Journal of proteome …, 2023 - ACS Publications
Chemical proteomics utilizes small-molecule probes to covalently engage with their
interacting proteins. Since chemical probes are tagged to the active or binding sites of …

Flipping the switch: innovations in inducible probes for protein profiling

SM McKenna, EM Fay, JF McGouran - ACS Chemical Biology, 2021 - ACS Publications
Over the past two decades, activity-based probes have enabled a range of discoveries,
including the characterization of new enzymes and drug targets. However, their suitability in …

Protein phosphatase PP2Cα S-glutathionylation regulates cell migration

DSK Kukulage, KTG Samarasinghe, NNJM Don… - Journal of Biological …, 2024 - jbc.org
Redox signaling is a fundamental mechanism that controls all major biological processes
partly via protein cysteine oxidations, including S-glutathionylation. Despite over 2000 …