Ligand discovery by activity-based protein profiling

MJ Niphakis, BF Cravatt - Cell Chemical Biology, 2024 - cell.com
Genomic technologies have led to massive gains in our understanding of human gene
function and disease relevance. Chemical biologists are a primary beneficiary of this …

Covalent Proximity Inducers

N London - Chemical Reviews, 2024 - ACS Publications
Molecules that are able to induce proximity between two proteins are finding ever increasing
applications in chemical biology and drug discovery. The ability to introduce an electrophile …

Covalent degrader of the oncogenic transcription factor β-catenin

FA Gowans, N Forte, J Hatcher… - Journal of the …, 2024 - ACS Publications
β-catenin (CTNNB1) is an oncogenic transcription factor that is important in cell–cell
adhesion and transcription of cell proliferation and survival genes that drive the …

[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 …

Redirecting the pioneering function of FOXA1 with covalent small molecules

SJ Won, Y Zhang, CJ Reinhardt, LM Hargis… - Molecular Cell, 2024 - cell.com
Pioneer transcription factors (TFs) bind to and open closed chromatin, facilitating
engagement by other regulatory factors involved in gene activation or repression. Chemical …

Adenanthin exhibits anti-inflammatory effects by covalently targeting the p65 subunit in the NF-κB signaling pathway

L Tong, ML Zha, J Hu, HY Li, L Kuai, B Li… - European Journal of …, 2024 - Elsevier
Adenanthin is a structurally unique ent-kaurane diterpenoid isolated from Rabdosia
adenantha, a traditional Chinese medicinal plant with potent anti-cancer and anti …

Simple, Enantiocontrolled Azetidine Library Synthesis via Strain Release Functionalization of 1-Azabicyclobutanes

M Bielecki, M Nassir, HA Sharma, NJ Truax, N Raheja… - 2024 - chemrxiv.org
A simple, modular, programmable approach to access complex stereopure azetidines
through strain-release functionalization is disclosed. The synthetic methods developed …

Coordinated inheritance of extrachromosomal DNAs in cancer cells

KL Hung, MG Jones, ITL Wong, EJ Curtis, JT Lange… - Nature, 2024 - nature.com
The chromosomal theory of inheritance dictates that genes on the same chromosome
segregate together while genes on different chromosomes assort independently …

[PDF][PDF] –RNA polymerase II stalling in cancer therapy: chemistry and biology of transcription and repair associated drug sensitivity vs. resistance

L Slappendel, CMN Aloisi… - … for Targeted Cancer …, 2024 - research-collection.ethz.ch
Many chemotherapeutics target metabolic processes associated with DNA replication and
transcription to induce cell death. While traditional chemotherapeutics that inhibit DNA …

Covalent modification of protein by chemical probe in living cells for structural and interaction studies

Z Zheng, Y Cheng, P Li, CS Heng Tan - ChemBioChem - Wiley Online Library
Cellular activities are predominantly carried out by proteins that can dynamically adopt
different structural conformations and differentially interact with other biomolecules …