Comprehensive Chemoproteomics: HMGCS1 Inhibitor Profiles and Target Engagement Ratios

A chemoproteomics dataset from figshare, last updated May 13, 2026, provides insights into covalent inhibitors targeting HMG-CoA synthase 1 (HMGCS1) in cancer metabolism. The dataset, created by Liang Sun, includes on- and off-target profiles generated through orthogonal chemoproteomic methods, including scavenging proteomics to analyze de-enriched fractions. It contains data supporting the development of CNP7, a selective cyanopyrrolidine inhibitor, and includes a 2.29 Å cryo-EM structure of the inhibitor-enzyme complex.

Use Cases

• Validate target selectivity of covalent inhibitors based on chemoproteomic profiling data.
• Compare target engagement ratios across the proteome based on the scavenging proteomics approach.
• Investigate cell line-specific anticancer activity patterns distinct from statins, as mentioned in the description.
• Analyze protein deprenylation effects following HMGCS1 inhibition based on the described 4-hour treatment data.

Strengths

• Includes a 2.29 Å cryo-EM structure revealing inhibitor binding within HMGCS1's hydrophobic pocket.
• Integrates orthogonal chemoproteomic methods, providing both on- and off-target profiles.
• Dataset size is 4.4 MB, indicating a focused and likely manageable data volume.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Description metadata is limited; actual data quality requires manual inspection after download.

Provenance

Source

figshare

Collection Method

Chemoproteomic profiling integrating enrichment and scavenging proteomics.

Freshness

Last updated 2026-05-13 18:05:00; freshness should be verified.