Photoaffinity labelling strategies for mapping the small molecule–protein interactome

NR Burton, P Kim, KM Backus - Organic & biomolecular chemistry, 2021 - pubs.rsc.org
Nearly all FDA approved drugs and bioactive small molecules exert their effects by binding
to and modulating proteins. Consequently, understanding how small molecules interact with …

Chemical profiling of DNA G-quadruplex-interacting proteins in live cells

X Zhang, J Spiegel, S Martínez Cuesta, S Adhikari… - Nature Chemistry, 2021 - nature.com
DNA–protein interactions regulate critical biological processes. Identifying proteins that bind
to specific, functional genomic loci is essential to understand the underlying regulatory …

Developing Isoxazole as a Native Photo‐Cross‐Linker for Photoaffinity Labeling and Chemoproteomics

K Cheng, J Qi, X Ren, J Zhang, H Li… - Angewandte Chemie …, 2022 - Wiley Online Library
Photoaffinity labeling is a powerful technique to interrogate drug‐protein interactions in
native cellular environments. Photo‐cross‐linkers are instrumental for this technique …

Chemical proteomics accelerates the target discovery of natural products

SJ He, J Li, JC Zhou, ZY Yang, X Liu, YW Ge - Biochemical Pharmacology, 2024 - Elsevier
More than half of the global novel drugs are directly or indirectly derived from natural
products (NPs) because of their better selectivity towards proteins. Traditional medicines …

Ynamide electrophile for the profiling of ligandable carboxyl residues in live cells and the development of new covalent inhibitors

S Li, P Zhang, F Xu, S Hu, J Liu, Y Tan… - Journal of Medicinal …, 2022 - ACS Publications
Covalent inhibitors with an electrophilic warhead have received considerable attention due
to their remarkable pharmacological properties. However, the electrophilic warhead in …

Discovery of encequidar, first-in-class intestine specific P-glycoprotein inhibitor

MP Smolinski, S Urgaonkar, L Pitzonka… - Journal of Medicinal …, 2021 - ACS Publications
Many chemotherapeutics, such as paclitaxel, are administered intravenously as they suffer
from poor oral bioavailability, partly because of efflux mechanism of P-glycoprotein in the …

Protein-labeling fluorescent probe for folate receptor α

PW Fang, YC Lin, SY Fan, A Panja, SQ Xu… - Analytical …, 2023 - ACS Publications
GPI-anchored folate receptor α (FRα) is an attractive anticancer drug target and diagnosis
marker in fundamental biology and medical research due to its significant expression on …

Novel electrophilic warhead targeting a triple-negative breast cancer driver in live cells revealed by “inverse drug discovery”

Y Fan, H Si, Z Zhang, L Zhong, H Sun… - Journal of Medicinal …, 2021 - ACS Publications
The “inverse drug discovery” strategy is a potent means of exploring the cellular targets of
latent electrophiles not typically used in medicinal chemistry. Cyclopropenone, a powerful …

Light-Controlled Traceless Protein Labeling via Decaging Thio-o-naphthoquinone Methide Chemistry

H Yu, S Wang, J Huang, Y Fu, M Wagner, T Weil… - Organic …, 2022 - ACS Publications
We report the molecular design of a novel multifunctional reagent and its application for light-
controlled selective protein labeling. This molecule integrates functions of protein–ligand …

Long-term transcriptomic and proteomic effects in Sprague Dawley rat thyroid and plasma after internal low dose 131I exposure

M Larsson, N Rudqvist, J Spetz, E Shubbar, TZ Parris… - Plos one, 2020 - journals.plos.org
Background Radioiodide (131I) is commonly used to treat thyroid cancer and hyperthyroidis.
131I released during nuclear accidents, have resulted in increased incidence of thyroid …