A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

By M. Matyskiela, Gang Lu, Takumi Ito, B. Pagarigan, Chin-Chun Lu, Karen Miller, W. Fang, Nai-Yu Wang, Derek Nguyen, J. Houston and 14 more. 2016

584 citations recorded by the source corpus.

Subfields: Hematology, Molecular Biology

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Hematology

1. Benjamin L. Ebert

In Molecular Biology

1. C. Crews
2. George M. Burslem
3. Yang Xie
4. Benjamin L. Ebert
5. Tarjei S. Mikkelsen

Citations in the corpus

• Proteolysis Targeting Chimeras as Therapeutics and Tools for Biological Discovery (2020, background): “The off-target effects of CRBN-recruiting PROTACs must be very carefully assessed because the IMiD components, alone or incorporated into PROTACs, can induce degradation of zincfinger CRBN neo-substrates (Fischer et al., 2014; Ishoey et al., 2018; Krönke et al., 2014; Matyskiela et al., 2016).”
• Lessons in PROTAC design from selective degradation with a promiscuous warhead (2017, background): “In our proteomic dataset, we observed degradation of GSPT1 and ZFP91 with the active PROTAC compound 2 but not with the N-methylated negative control 4.”
• Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15 (2017, background): “In another example of how chemical structure can influence neosubstrate preference, CC-885 was identified in a screen of IMiD derivatives as catalyzing the recruitment of GSPT1, a translation termination factor essential for myeloid leukemia cell proliferation, to CUL4-CRBN (44).”
• Acute pharmacological degradation of Helios destabilizes regulatory T cells (2021, unknown): “Indeed, thalidomide analogs (also known as IMiDs, or immunomodulatory imide drugs) can induce the degradation of a variety of proteins, such as Ikaros (IKZF1) and Aiolos (IKZF3) 8,9 , casein kinase 1 α (CK1 α ) 10 , ZFP91 11 , SALL4 12,13 , and GSPT1 14 .”
• Defining the human C2H2 zinc-finger degrome targeted by thalidomide analogs through CRBN (2018, methodology): “Previous work has implicated the second C2H2 ZF domain in IKZF1 and IKZF3 (5, 7) and ZF4 of ZFP91 as the drug-inducible degrons (5, 7, 16).”