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PROTAC XPO1 degrader-1
- Development stage
- Preclinical
- Lead developer
- Kaken Pharmaceutical
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
PROTAC XPO1 degrader-1 is a small-molecule proteolysis-targeting chimera (PROTAC) designed to induce the degradation of the Exportin 1 (XPO1) protein. XPO1, also known as Chromosome Region Maintenance 1 (CRM1), is a nuclear export protein often overexpressed in cancer cells, leading to the abnormal export of tumor suppressor proteins. By targeting XPO1 for degradation, PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest in the G1 phase. This compound is currently in preclinical research for its potential therapeutic application in hematological malignancies, particularly acute myeloid leukemia (AML).
- Other names
- XPO1 PROTACXPO-1 PROTACXPO 1 PROTAC
02
Targets
XPO1 (Exportin-1)
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