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).
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.
KAT6 is a histone lysine acetyl transferase involved in the epigenetic regulation of oncogenes and it is often dysregulated in cancer, including breast cancer. Inhibiting KAT6 blocks the transcription of genes such as ESR1 and CCND1 and the use of KAT6 inhibitors together with endocrine therapy and CDK4/6 inhibitor therapy may enhance the effectiveness in cancer.
The inhibition of hematopoietic progenitor kinase 1 (HPK1), predominantly expressed in immune cells, has proven effective in reducing tumor growth across cancer immune response modulation.
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