CNP7 Inhibitor Chemoproteomics Data for HMGCS1 Target Validation

A 2.29 Å cryo-EM structure reveals how the covalent inhibitor CNP7 engages the catalytic cysteine of HMGCS1. This dataset, shared by Liang Sun on figshare, contains chemoproteomic profiles comparing scavenging and enrichment proteomics methods to assess on- and off-target binding of inhibitors targeting the mevalonate pathway in cancer. It was last updated in May 2026.

Use Cases

• Validate target engagement and selectivity of covalent inhibitors based on chemoproteomic profiling methods described.
• Compare scavenging versus enrichment proteomics approaches for distinguishing high- and low-occupancy binders.
• Investigate cell line-specific anticancer activity patterns based on pathway node-specific vulnerabilities mentioned.
• Analyze global protein deprenylation effects following HMGCS1 inhibition.
• Benchmark new covalent inhibitor candidates against the selectivity profile of CNP7.

Strengths

• Includes orthogonal chemoproteomic methods (scavenging and enrichment proteomics) for unbiased profiling.
• Provides a target engagement framework validated by a 2.29 Å cryo-EM structure.
• Dataset is shared under a CC-BY-NC-4.0 license, permitting non-commercial reuse with attribution.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Data may reflect experimental bias inherent to the specific cell lines and methods used.

Provenance

Source

Liang Sun via figshare.

Collection Method

Integrated chemoproteomic methods (scavenging and enrichment proteomics) applied to covalent inhibitor development.

Freshness

Last updated 2026-05-13 18:04:52; freshness should be verified.