PXD057094-1
PXD057094 is an original dataset announced via ProteomeXchange.
Dataset Summary
| Title | Evaluation of linkers and cereblon-directing warheads for the development of orally bioavailable PROTACs |
| Description | PROTACs usually occupy physicochemical space outside the one defined by classical drug-like molecules, which often presents considerable challenges in their optimization and development for oral administration. We have previously reported phenyl glutarimide (PG)-based BET PROTAC SJ995973, with improved overall in vitro degradation and antiproliferative activities compared to its direct thalidomide-based analogue dBET1, but similarly poor in vivo pharmacokinetic profile. Here we describe optimization efforts that led to the discovery of an orally bioavailable PG-PROTAC SJ44236, and results of a comprehensive in vitro/vivo comparative study with direct analogues containing alternative CRBN warheads. |
| HostingRepository | MassIVE |
| AnnounceDate | 2025-01-30 |
| AnnouncementXML | Submission_2025-01-30_12:20:21.176.xml |
| DigitalObjectIdentifier | |
| ReviewLevel | Non peer-reviewed dataset |
| DatasetOrigin | Original dataset |
| RepositorySupport | Unsupported dataset by repository |
| PrimarySubmitter | Martin Steger |
| SpeciesList | scientific name: Homo sapiens; common name: human; NCBI TaxID: 9606; |
| ModificationList | GG |
| Instrument | Bruker Daltonics instrument model |
Dataset History
| Revision | Datetime | Status | ChangeLog Entry |
|---|---|---|---|
| 0 | 2024-10-23 01:33:16 | ID requested | |
| ⏵ 1 | 2025-01-30 12:20:21 | announced |
Publication List
| no publication |
Keyword List
| submitter keyword: Targeted protein degradation, PROTACs, DatasetType:Proteomics |
Contact List
| Zoran Rankovic | |
|---|---|
| contact affiliation | The Institute of Cancer Research |
| contact email | zoran.rankovic@icr.ac.uk |
| lab head | |
| Martin Steger | |
| contact affiliation | NEOsphere Biotechnologies GmbH |
| contact email | martin.steger@neospherebiotech.com |
| 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.ucsd.edu/v07/MSV000096172/ |
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