Web14852 Ensembl ENSG00000103342 ENSMUSG00000062203 UniProt P15170 Q8R050 RefSeq (mRNA) NM_002094 NM_001130006 NM_001130007 NM_001130008 … WebBTX-1188, a first-in-class dual degrader of GSPT1 and IKZF1/3, for treatment of acute myeloid leukemia (AML) and solid tumors. (ASCO 2024) - "This approach is expected to improve clinical outcomes and reduce toxicities associated with pure GSPT1 degradation (CC-90009), thus expanding the therapeutic window of BTX-1188. Functionally, BTX …
BTX-1188 Demonstrates Safety Benefits, Enters Phase 1 Trials
WebAug 31, 2024 · Cereblon (CRBN) is an E3 ligase adapter protein that can be reprogrammed by imide-class compounds such as thalidomide, lenalidomide, and pomalidomide to induce the degradation of neo-substrate proteins. In order to identify additional small molecule CRBN modulators, we implemented a focused combinatorial library approach where we … 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 … lw rabbit\u0027s-foot
Biotheryx to Present Preclinical Data for Its Dual Protein Degrader …
WebBTX-1188 is the first ever rationally designed dual-targeting molecular glue degrader of GSPT1 and IKZF1/3 that we are developing for the treatment of acute myeloid leukemia and solid tumors. We believe that the combination of degrading GSPT1, a promising oncology target, and IKZF1/3, clinically validated immunomodulatory targets, enables ... WebGSPT1 (G1 To S Phase Transition 1) Developing PROTACs and molecular glues for pediatric leukemias (ACS-Sp 2024) The design of a Molecular Glue Library (MGL) containing over 5,000 small molecules, its screening against a large panel of cancer cell lines, and discovery of highly potent and selective GSPT1 and CK1a degraders will also … WebCC-885 Can Induce GSPT1 Degradation Nature 2016, 535, 252 (Celgene) – GSPT1 is a translation termination factor (mediates stop codon recognition and protein release from the ribosome) – CC-885 has anti-proliferative activity in patient AML cells (sub-nanomolar) – found to degrade GSPT1 via UPS; decreased cellular fitness upon degradation lwr arm