Chemical Proteomics–Guided Discovery of Covalent Ligands for ...

Annual Review of Cancer Biology Volume 8, 2024 Chemical Proteomics–Guided Discovery of Covalent Ligands for Cancer Proteins

Chemoproteomics-Enabled Discovery of Covalent RNF114-Based ...

Here, using chemoproteomics-enabled covalent ligand screening approaches, we have discovered a more synthetically tractable covalent ligand EN219 that targets ...

Mass Spectrometry & Proteomics for Covalent Lead Discovery

Recent advances in high-throughput technology have made it possible for researchers to screen thousands of ligands against a protein of interest ...

Chemoproteomic-Driven Discovery of Covalent PROTACs

Chemical proteomics is a powerful strategy for large-scale profiling and systematic analysis of small molecule–protein interactions across the ...

Chemical Proteomics–Guided Discovery of Covalent Ligands for ...

We speculate on the attributes of chemical proteomics and covalent chemistry that have enabled targeting of previously inaccessible cancer-relevant pathways and ...

Discovery of chemical probes that perturb protein complexes using ...

Lazear et al. ... suggest that covalent ligands may provide an advantage for chemically targeting the historically challenging protein classes, ...

Chemical Proteomic Characterization of a Covalent KRASG12C ...

In order to better understand the mechanism of action of small molecule drugs, it is important to identify the cellular protein targets of the ligand, as well ...

ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery ...

Incorporating an electrophile warhead into DNA-encoded compounds recently permitted the discovery of covalent ligands that selectively react ...

Proteomic discovery of chemical probes that perturb protein ...

Efforts to expand the druggable proteome have begun to introduce complementary approaches for ligand discovery that leverage binding assays with ...

Quantitative proteomics and applications in covalent ligand discovery

In the realm of covalent drug discovery, chemoproteomics has become an integral component, as it enables the mapping of chemical modifications ...

Identification of Covalent Ligands – from Single Targets to Whole ...

There has been a surge of interest and efforts in the discovery of covalent ligands for diverse proteins as tool compounds or therapeutic ...

Advances in covalent drug discovery - Nature

Chemoproteomics platforms have emerged to complement covalent ligand screening and assist in ligand discovery, selectivity profiling and target ...

Covalent ligand discovery for chemical probes to challenging targets

Covalent ligand discovery for chemical probes to challenging targets – 16 February 2021. 2.8K views 3 years ago

Covalent Ligand Research Articles - R Discovery

We speculate on the attributes of chemical proteomics and covalent chemistry that have enabled targeting of previously inaccessible cancer-relevant pathways and ...

Fragment-based covalent ligand discovery - Vividion Therapeutics

its utility to both the discovery of novel covalent ligands and their cognate protein targets. ... proteome.59. RSC Chemical Biology. Review. Open ...

Prof. Lu Zhou's group reported a new method for high-throughput ...

This work was published online in the Journal of the American Chemical Society entitled as ABPP-CoDEL: Activity-Based Proteome Profiling-Guided ...

Proteome‐Wide Fragment‐Based Ligand and Target Discovery

Conventional chemical probe discovery is typically pursued via the high-throughput screening (HTS) of large chemical libraries (∼106 compounds) ...

Proteome-wide covalent ligand discovery in native biological systems

Fragment-based approaches in drug discovery and chemical biology. Biochemistry 51, 4990–5003 (2012). 4. Erlanson, D. A. et al. Site-directed ...

Covalent hits and where to find them - SLAS Discovery

Covalent hits for drug discovery campaigns are neither fantastic beasts nor mythical creatures, they can be routinely identified through electrophile-first ...

Fragment-based covalent ligand discovery - RSC Publishing

Fragment-based drug discovery, which has traditionally been used in a target-centric fashion, is now being deployed on a proteome-wide scale ...