Researchers from AUTOTAC Bio Inc. and affiliated organizations presented preclinical data for ATC-324, a novel autophagy-targeting chimera (AUTOTAC) designed to induce androgen receptor (AR) degradation.
MBT-C101 is a selective, potentially first-in-class potent HSP90 chaperone-mediated degrader of PI3Kα, for the treatment of breast cancer. It was developed by Magicbullet Therapeutics Inc. using the company’s Chaperone-mediated Degrader (CM-Degrader) platform.
The transcription factor IKZF2 is a marker of highly suppressive regulatory T cells (Tregs). When IKZF2 is degraded, Tregs become effector-like T cells leading to increased antitumor immune response in the tumor microenvironment.
Data from preclinical studies conducted to evaluate the activity of NKT-3964, a first-in-class, orally bioavailable CDK2-selective PROTAC degrader being developed for the potential treatment of cancer, were reported by Nikang Therapeutics Inc.
Two days after Monte Rosa Therapeutics Inc. signed a molecular glue degrader deal with Novartis AG, two other companies, Biogen Inc. and Neomorph Inc., are moving forward in the same space in a partnership worth up to $1.45 billion. Cambridge, Mass.-based Biogen and San Diego-based Neomorph will develop molecular glue degraders (MGDs) for priority targets in Alzheimer’s, rare neurological and immunological diseases, using Neomorph’s MGD platform to identify and validate novel small-molecule protein degraders.
Shanghai Helioson Pharmaceutical Co. Ltd. has identified molecular glue degraders acting as DNA-binding protein Ikaros (IKZF1) and/or zinc finger protein Aiolos (IKZF3) degradation inducers reported to be useful for the treatment of cancer, autoimmune disease and inflammatory disorders.
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.
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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