Betta Pharmaceuticals Co. Ltd. has prepared and tested probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) inhibitors reported to be useful for the treatment of cancer.
Work at Dark Blue Therapeutics Ltd. has led to the identification of proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a MLLT1- or MLLT3-targeting moiety through a linker.
Bayer Consumer Care AG has disclosed new tachykinin NK1 and NK3 receptor dual antagonists reported to be useful for the treatment of breast cancer, endometriosis, hidradenitis, hypertrichosis, osteoporosis, polycystic ovary syndrome, preeclampsia and benign prostatic hyperplasia, among others.
Aurigene Oncology Ltd. and Olema Pharmaceuticals Inc. have jointly patented acylsulfonamide histone acetyltransferase KAT6A (monocytic leukemia zinc finger protein; MOZ; MYST-3) inhibitors reported to be useful for the treatment of cancer.
In research conducted at West China Hospital of Sichuan University and Chengdu University of Traditional Chinese Medicine, coupling of the pan-FGFR inhibitor erdafitinib with a CRBN binder led to a new series of fibroblast growth factor receptor (FGFR) degraders, with compound [I] identified as the lead candidate.
Investigators at Nanjing Medical University and The University of Texas MD Anderson Cancer Center recently published data from their research that aimed to identify novel immunotherapy targets in triple-negative breast cancer (TNBC).
Metastasis is the leading cause of mortality in patients with small-cell lung cancer (SCLC), with limited therapeutic options available. SCLC is characterized by a high proliferation rate, early metastasis and poor prognosis.
Researchers from Nuvalent Inc. reported preclinical data of NVL-655, a next-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitors with IC50 of 0.9 and 1.8 nM against ALK wild-type (WT) and ALK G1202R/L1196M, respectively.
Adcencdo ApS has obtained FDA clearance of its IND application for ADCE-D01 in patients with metastatic and/or unresectable soft tissue sarcoma (STS). A first-in-human phase I/II study in patients with metastatic and/or unresectable STS will recruit in the U.S. and Europe.
Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) are involved in the regulation of transcription elongation, DNA damage response and genomic stability balance. A few inhibitors of CDK12- and CDK13-mediated transcription have shown antiproliferative effects in the preclinical setting but have not progressed to clinical testing due to excessive toxicity.
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