Compound class:
Synthetic organic
Comment: NX-2127 is an orally bioavailable protein degrader molecule. It reduces levels of both Bruton's tyrosine kinase (BTK) and the IKZF transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) through targeted ubiquitination and proteasomal degradation. NX-2127 acts as a dual PROTAC (through recruitment of cereblon) and molecular glue (degradation of the neosubstrate transcription factors). It is predicted that this approach can achieve clinical efficacy, even in the presence of BTK mutations that confer resistance to clinically used kinase inhibitor drugs.
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Immunopharmacology Comments |
NX-2127 a clinical lead with predicted utility as a treatment for B cell malignancies. Targeted degradation of BTK is an alternative approach to direct inhibition of kinase activity. |