Tumor cell survival is dependent on phosphate homeostasis, which requires high amounts of energy. Researchers have demonstrated that the silencing of xenotropic and polytropic retrovirus receptor 1 (XPR1) led to reduced tumor growth in an ovarian cancer cell line xenograft, and similar vulnerability was found in lung 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.
Genetic alterations in FAT1, YAP1 or WWTR1 genes are commonly seen in head and neck squamous cell carcinoma (HNSCC) patients. Targeting Hippo and MAPK pathways in combination has proven effective in preclinical models of HNSCC.
The next-generation farnesyl transferase inhibitor KO-2806 is currently in phase I clinical development at Kura Oncology Inc. for the treatment of patients with solid tumors, including non-small-cell lung cancer (NSCLC) and colorectal cancer (CRC).
Duality Biologics Ltd. presented preclinical data on DB-1419, a potentially first-in-class bispecific antibody-drug conjugate (ADC) consisting of a humanized antibody targeting B7-H3 and PD-L1 conjugated to a DNA topoisomerase I inhibitor under development for the treatment of cancer.
Gain-of-function mutations and overexpression of the EZH2 gene lead to H3K27Me3 accumulation, which in turn initiates tumorigenesis and tumor progression, thus making it a promising target for therapy.
Activin receptor-like kinase 5 (ALK5) is a member of the transforming growth factor-β (TGF-β) family associated with tumor development and progression that impacts cancer immune response within the tumor microenvironment.
Nonselective poly(ADP-ribose) polymerase (PARP) inhibitors have shown antitumoral activity, but they are tied to hematotoxicity, most probably due to PARP2 inhibition. Instead, selective PARP inhibitors retain antitumoral activity without risking PARP2-related toxicity.
Researchers from Zymeworks Inc. recently reported preclinical data for ZW-220, an antibody-drug conjugate (ADC) consisting of humanized IgG1 monoclonal antibody targeting sodium-dependent phosphate transport protein 2B (SLC34A2, NaPi2b) conjugated to a topoisomerase I inhibitor, being developed for the treatment of cancer.
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