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RO5454291
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
RO5454291 (also referred to as Glixx or CPD25) is a small molecule inhibitor of the cyclin-dependent kinase 5 (CDK5) and p25 protein-protein interaction (PPI). Originally identified from a Roche internal library, RO5454291 prevents the hyperactivation of CDK5 by disrupting its interaction with the activator p25. In preclinical models of chronic kidney disease (CKD), such as unilateral ureter obstruction (UUO) and aristolochic acid nephropathy (AAN), treatment with RO5454291 has been shown to prevent proximal tubule cell (PTC) dedifferentiation, reduce profibrotic cytokine secretion, and ameliorate interstitial fibrosis.
- Other names
- GLXGlixx
02
Targets
CDK5 (Cyclin-dependent kinase 5)TPPP1 (Tubulin polymerization-promoting protein 1)
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