Prelude Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety. They are described as potentially useful for the treatment of cancer.
Jiangsu Hansoh Pharmaceutical Group Co. Ltd. and Shanghai Hansoh Biomedical Co. Ltd. have identified pyrimidine-containing polycyclic compounds acting as GTPase KRAS (G12D mutant) inhibitors reported to be useful for the treatment of cancer.
Cambridge Enterprise Ltd. has synthesized casein kinase II isoform α (CK2α) inhibitors reported to be useful for the treatment of cancer, viral infection, diabetes, ischemia, neurodegeneration, circadian rhythm disorders, vascular disorders and inflammatory disorders.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has disclosed molecular glue degraders comprising cereblon (CRBN) ligands acting as DNA-binding protein Ikaros (IKZF1) or zinc finger protein Aiolos (IKZF3) degradation inducers reported to be useful for the treatment of cancer, autoimmune diseases, diabetes, infections, septic shock and more.
Shasqi Inc. recently reported the discovery of novel candidates using their proprietary Click Activated Protodrugs Against Cancer (CAPAC) platform, which aims to selectively activate high doses of cancer drugs directly at the tumor site. To achieve this, CAPAC consists of two separate components: a tumor-targeted activator and an inactivated payload.
DNA-encoded library (DEL) technology is a promising new tool for identifying ligands for challenging protein targets, allowing for the preparation and screening of large chemical libraries with significantly reduced time, costs and material requirements when compared to HIT-finding strategy.
Metabolic dysfunction-associated steatotic liver disease (MASLD), previously known as nonalcoholic fatty liver disease, shows different occurrence between sexes, being less prevalent in premenopausal women than in men or postmenopausal women.
Pfizer Inc. has presented preclinical data on its first-in-class, selective cyclin-dependent kinase 4 (CDK4) inhibitor compound, PF-07220060, that has shown 20-fold and 4-fold increased selectivity for CDK4 vs. CDK6 compared to palbociclib and abemaciclib/ribociclib, respectively.
It has been previously demonstrated that B7-H3 and EGFR are co-expressed in multiple solid tumors. At the ongoing AACR meeting in San Diego, researchers from Innovent Biologics Inc. presented preclinical data for their bispecific antibody (bsAb), IBI-334, against B7-H3 and EGFR.
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