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 …
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 …
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 …
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 …
drug discovery campaigns. Chemoproteomic compound screens, which use a mass …
Redirecting the pioneering function of FOXA1 with covalent small molecules
Pioneer transcription factors (TFs) bind to and open closed chromatin, facilitating
engagement by other regulatory factors involved in gene activation or repression. Chemical …
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 …
adenantha, a traditional Chinese medicinal plant with potent anti-cancer and anti …
Simple, Enantiocontrolled Azetidine Library Synthesis via Strain Release Functionalization of 1-Azabicyclobutanes
A simple, modular, programmable approach to access complex stereopure azetidines
through strain-release functionalization is disclosed. The synthetic methods developed …
through strain-release functionalization is disclosed. The synthetic methods developed …
Coordinated inheritance of extrachromosomal DNAs in cancer cells
The chromosomal theory of inheritance dictates that genes on the same chromosome
segregate together while genes on different chromosomes assort independently …
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 …
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 …
different structural conformations and differentially interact with other biomolecules …