Photoaffinity labelling strategies for mapping the small molecule–protein interactome
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 …
to and modulating proteins. Consequently, understanding how small molecules interact with …
Chemical profiling of DNA G-quadruplex-interacting proteins in live cells
DNA–protein interactions regulate critical biological processes. Identifying proteins that bind
to specific, functional genomic loci is essential to understand the underlying regulatory …
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
Photoaffinity labeling is a powerful technique to interrogate drug‐protein interactions in
native cellular environments. Photo‐cross‐linkers are instrumental for this technique …
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 …
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 …
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 …
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 …
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 …
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 …
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
Background Radioiodide (131I) is commonly used to treat thyroid cancer and hyperthyroidis.
131I released during nuclear accidents, have resulted in increased incidence of thyroid …
131I released during nuclear accidents, have resulted in increased incidence of thyroid …