WebNov 13, 2024 · The cereblon E3 ligase modulator (CELMoD) CC-885 co-opts the CUL4-DDB1-CRBN-RBX1 (CRL4 CRBN) E3 ubiquitin ligase complex to trigger the ubiquitination and proteasomal degradation of the translation termination factor G1 to S phase transition 1 (GSPT1), resulting in robust growth inhibition in AML cell lines and primary patient blasts … WebAs a result, we identified 34f (TD-522), which exhibits strong anti-proliferative effects in both KG-1 (EC 50 = 0.5 nM) and TMD-8 (EC 50 = 5.2 nM) cell lines. Compound 34f …
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WebDec 23, 2024 · with either vehicle or the appropriate molecular glue degraders to select for candidate drug resistance-conferring mutations (Fig 1a, Fig S1a). For GSPT1 CRISPR-suppressor scanning, the GSPT1 degraders CC-885 and ZXH-1-16133 were dosed in gradual escalation due to their acute cytotoxicity, starting at the approximate GI 50 • Ozawa K, Murakami Y, Eki T, Yokoyama K, Soeda E, Hoshino S, Ui M, Hanaoka F (Mar 1992). "Mapping of the human GSPT1 gene, a human homolog of the yeast GST1 gene, to chromosomal band 16p13.1". Somatic Cell and Molecular Genetics. 18 (2): 189–94. doi:10.1007/BF01233164. PMID 1574740. S2CID 12796634. • Kikuchi Y, Shimatake H, Kikuchi A (Apr 1988). "A yeast gene required for the G1-to-S transition encodes a protein containing an A-kinas… grohe bau soft close toilet seat
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WebG1 to S phase transition 1 protein (GSPT1) is a translation termination factor that plays a central role in messenger RNA (mRNA) translation and regulation of the G1/S checkpoint … WebPolyclonal Antibody for studying GSPT1 iso3. Cited in 12 publications. Validated for Western Blotting. Highly specific and rigorously validated in … WebFeb 4, 2024 · A number of clinically validated drugs have been developed by repurposing the CUL4-DDB1-CRBN-RBX1 (CRL4CRBN) E3 ubiquitin ligase complex with molecular glue degraders to eliminate disease-driving proteins. Here, we present the identification of a first-in-class GSPT1-selective cereblon E3 ligase mod … filenotfoundexception import