Compound class:
Synthetic organic
Comment: T3 is a PROTAC degrader that simultaneously targets alpha-synuclein (α-Syn) and tau proteins [1]. It was developed for potential to reduce pathological α-Syn and tau aggregations for application as a neurodegenerative disease therapy. The target protein warhead binds both α-Syn and tau, and the cereblon E3 ubiquitin ligase is engaged by a pomalidomide moiety.
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Bioactivity Comments |
T3 binding affinity (Kd) for α-Syn is 470 nM [1]. The DC50 for T3-induced α-Syn degradation is 1.57 μM, and for tau degradation the DC50 is 4 μM. T3 crosses the blood-brain barrier in vivo, and promotes the clearance of α-Syn and tau from the brains of MPTP-induced Parkinson's disease model mice. T3 binding affinity (Kd) for α-Syn is 470 nM. |
Selectivity at ligand targets | ||||||||||||||||||||||||||||||||||
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