New Reversible Covalent Warheads: Proteome-Wide Map of Ligandable N-Terminal Cysteines

Jixian Zhang's dataset, shared via figshare in April 2026, provides a proteome-wide map of ligandable native N-terminal cysteine (NCys) residues. The data likely contains results from a library of electrophilic probes, including cyanobenzothiazole (CBT), used to systematically identify modifiable sites in proteins like GFPT1 and CSTB. The 952.8 KB XLSX file includes findings on the use of CBT for generating reversible covalent degraders targeting proteins such as BRD4, EGFR, and HER2.

Use Cases

• Identifying novel ligandable protein targets based on the proteome-wide map of N-terminal cysteines.
• Designing reversible covalent degraders based on the cyanobenzothiazole (CBT) warhead platform.
• Benchmarking degradation efficiency (DC50, Dmax) for challenging targets like EGFR mutants.
• Studying ternary complex formation and ubiquitination mechanisms based on DCAF16 modification data.

Strengths

• Includes specific quantitative results, such as a degrader DC50 of 16.7 nM and Dmax of 98%.
• Demonstrates application against challenging, clinically relevant targets like EGFR L858R/T790M/C797S and HER2.
• Provides the first proteome-wide map of ligandable NCys residues, a foundational resource.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment for large-scale analysis.
• Data is stored in a single 952.8 KB XLSX file, indicating a limited scope for raw experimental data.

Provenance

Source

Jixian Zhang

Collection Method

Constructed from a library of electrophilic probes to systematically map ligandable native NCys residues.

Time Range

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Freshness

Last updated 2026-04-28 03:05:35; freshness should be verified.

Geography

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