⮝ Full datasets listing
PXD059370
PXD059370 is an original dataset announced via ProteomeXchange.
Dataset Summary
| Title | in silico Screening based KLHL41 Ligand Discovery for Muscle Cell Specific Protein Degradation |
| Description | Proteolysis-targeting chimeras (PROTACs) have emerged as an innovative therapeutic strategy for targeted protein degradation (TPD) by leveraging the cellular ubiquitin-proteasome system (UPS). Despite the recent advancement of PROTAC development, they remain predominantly dependent on two specific E3 ligases, CRBN and VHL, which are ubiquitously expressed in all types of cells. Recently, discovery of tissue specific E3 ligase ligands has been spotlighted for tissue specific protein degradation to avoid the off-target tissue effect. In this context, we discovered a ligand of KLHL41, a muscle-specific E3 ligase, through in silico screening using 4 different commercial programs. We further used the KLHL41 ligand for the development of a muscle specific BRD4 targeting PROTAC, KBD-1, with micromolar activity. To improve the protein degradation efficiency of KBD-1, we adopted an electrophile to the KLHL41 ligand and synthesized the BRD4 targeting covalent PROTAC, c-KBD-1, which achieved a sub-nanomolar DC50. We demonstrated that BRD4 degradation of c-KBD-1 is KLHL41-dependent and muscle cell specific. Our KLHL41 ligand was also used for androgen receptor (AR) targeting PROTAC, which showed excellent AR degradation in muscle cells. |
| HostingRepository | MassIVE |
| AnnounceDate | 2026-03-24 |
| AnnouncementXML | Submission_2026-03-24_17:41:41.860.xml |
| DigitalObjectIdentifier | |
| ReviewLevel | Non peer-reviewed dataset |
| DatasetOrigin | Original dataset |
| RepositorySupport | Unsupported dataset by repository |
| PrimarySubmitter | Soyoung Yoon |
| SpeciesList | scientific name: Homo sapiens; common name: human; NCBI TaxID: 9606; |
| ModificationList | No PTMs are included in the dataset |
| Instrument | Orbitrap Exploris 480 |
Dataset History
| Revision | Datetime | Status | ChangeLog Entry |
|---|---|---|---|
| 0 | 2025-01-01 22:35:45 | ID requested | |
| ⏵ 1 | 2026-03-24 17:41:42 | announced |
Publication List
| no publication |
Keyword List
| submitter keyword: PROTAC, DatasetType:Proteomics |
Contact List
| Jongmin Park | |
|---|---|
| contact affiliation | Kangwon National University |
| contact email | jpark@kangwon.ac.kr |
| lab head | |
| Hankum Park | |
| contact affiliation | Seoul National University |
| contact email | hanpark@snu.ac.kr |
| lab head | |
| Juyong Lee | |
| contact affiliation | Seoul National University |
| contact email | nicole23@snu.ac.kr |
| lab head | |
| Soyoung Yoon | |
| contact affiliation | Seoul National University |
| contact email | dbsthdud111@snu.ac.kr |
| dataset submitter | |
Full Dataset Link List
| MassIVE dataset URI |
| 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://massive-ftp.ucsd.edu/v10/MSV000096752/ |
