PXD073488 is an
original dataset announced via ProteomeXchange.
Dataset Summary
| Title | Kinome-profiling enabled discovery of a LATS1/2 inhibitor with wound healing potential |
| Description | System-level mapping of kinase inhibitors polypharmacology can uncover opportunities for drug repurposing and identify starting points for medicinal chemistry campaigns aimed at novel targets. Here, we describe a large-scale profiling of 257 kinase inhibitors that revealed domains of promiscuity, pockets of selectivity and a broad region of uninhibited targets. Focusing on a subcluster enriched for AGC group kinases and using the AKT inhibitor AT-7867 (an antiproliferative agent) as a starting point, we employed scaffold hopping and property-based optimization to discover NCGC-6782, a LATS1/2 inhibitor with robust pro-proliferative activity. In cells, NCGC-6782 inhibited LATS1/2 activity, promoted rapid YAP nuclear translocation and transactivation of YAP-target genes. Kinome-wide profilings demonstrated good in vitro selectivity and exquisite chemoproteomic and kinetic selectivity. Transcriptomics and proteomics following NCGC-6782 revealed upregulation of YAP-dependent genes (4h) followed by activation of cell-cycle programs (24h). Consistently, NCGC-6782 accelerated proliferative regeneration in both cell-based and in vivo wound healing models |
| HostingRepository | PRIDE |
| AnnounceDate | 2026-07-15 |
| AnnouncementXML | Submission_2026-07-15_11:19:20.829.xml |
| DigitalObjectIdentifier | |
| ReviewLevel | Peer-reviewed dataset |
| DatasetOrigin | Original dataset |
| RepositorySupport | Unsupported dataset by repository |
| PrimarySubmitter | Dingyin Tao |
| SpeciesList | scientific name: Homo sapiens (Human); NCBI TaxID: NEWT:9606; |
| ModificationList | monohydroxylated residue; iodoacetamide derivatized residue |
| Instrument | Orbitrap Fusion Lumos |
Dataset History
| Revision | Datetime | Status | ChangeLog Entry |
|---|
| 0 | 2026-01-23 16:13:25 | ID requested | |
| ⏵ 1 | 2026-07-15 11:19:21 | announced | |
Publication List
| Tharakan R, Qu Y, Ceribelli M, Morris PJ, Fang Y, Thomas CJ, LeClair CA, Tao D, Data-Independent Acquisition Enhancement of a Competitive Activity-Based Protein Profiling Platform for Kinase Inhibitor Screening. J Mass Spectrom, 61(3):e70038(2026) [pubmed] |
| 10.1002/jms.70038; |
Keyword List
| submitter keyword: Human, proteomics, kinase selectivity profiling, kinase inhibitor |
Contact List
| Dingyin Tao |
|---|
| contact affiliation | National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, USA. |
| contact email | dingyin.tao@nih.gov |
| lab head | |
| Dingyin Tao |
|---|
| contact affiliation | National Institutes of Health (NIH)
National Center for Advancing Translational Sciences (NCATS) |
| contact email | dingyin.tao@nih.gov |
| dataset submitter | |
Full Dataset Link List
Dataset FTP location
NOTE: Most web browsers have now discontinued native support for FTP access within the browser window. But you can usually install another FTP app (we recommend FileZilla) and configure your browser to launch the external application when you click on this FTP link. Or otherwise, launch an app that supports FTP (like FileZilla) and use this address: ftp://ftp.pride.ebi.ac.uk/pride/data/archive/2026/07/PXD073488 |
| PRIDE project URI |
Repository Record List
[ + ]
[ - ]
- PRIDE
- PXD073488
- Label: PRIDE project
- Name: Kinome-profiling enabled discovery of a LATS1/2 inhibitor with wound healing potential
