Reconstituted Complex

An interaction is detected between purified proteins in vitro.

Publication

Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation.

Lv L, Chen P, Cao L, Li Y, Zeng Z, Cui Y, Wu Q, Li J, Wang JH, Dong MQ, Qi X, Han T

Molecular-glue degraders mediate interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a new molecular glue HQ461 discovered by high-throughput screening. Using loss-of-function and gain-of-function genetic screening in human cancer cells followed by biochemical reconstitution, we show that HQ461 acts by promoting an interaction between CDK12 and DDB1-CUL4-RBX1 E3 ubiquitin ligase, ... [more]

Elife Dec. 17, 2019; 9(); [Pubmed: 32804079]

Throughput

  • Low Throughput

Additional Notes

  • The reaction contained E1, UBCH5a [E2], and CUL4A-RBX1-DDB1 ligase [E3].

Curated By

  • BioGRID