Targeted protein degradation has gained attention in recent years due to its potential to hit proteins that are difficult to engage with conventional small molecules. Pin1 is an enzyme associated with tumor formation overexpressed in pancreatic cancer cells or cancer-associated fibroblasts in particular.
Work at Foghorn Therapeutics Inc. has led to the design of proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agent coupled to CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker acting as CBP degradation inducers.
Hainan Simcere Pharmaceutical Co. Ltd. has patented new membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (PKMYT1) inhibitors reported to be useful for the treatment of breast cancer.
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.
Trogenix Ltd. has emerged from stealth with a focus on treating cancer through viral immunotherapy. The company was founded as a spinout from the University of Edinburgh last year.
Cancer Targeted Technology LLC has been awarded the phase I portion ($400,000) of a fast track phase I/II ($2.4 million) Small Business Innovation Research (SBIR) grant by the National Cancer Institute (NCI) to develop CTT-2274 to treat metastatic prostate cancer.
Researchers from Elpiscience Biopharmaceuticals Inc. discussed the discovery and preclinical characterization of a novel NKG2A antibody-IL-2 mutant fusion protein – ES-015.129 – being developed as cancer immunotherapy.
Researchers from Exelixis Inc. described the preclinical characterization of XB-002, an antibody-drug conjugate consisting of a monoclonal antibody recognizing a tissue factor (TF) epitope that does not interfere with factor VII binding.
MDX-2001 (Modex Therapeutics Inc.) was engineered as a potentially first-in-class tetraspecific lymphocyte activator and survival enhancement receptor (LASER) recognizing CD3 and CD28 on human T cells and c-MET and TROP2 on tumor cells.