Newsletter

Clinical potential for off-target based drug repositioning

11/20/24

Examples of off-target based drug repositioning Crizotinib represents a powerful example of the transformative potential of off-target based drug repositioning. Originally developed as a potent inhibitor of MET, it ultimately received approval for treatment of ALK fusion-positive non-small cell lung cancer (NSCLC) in its capacity as an inhibitor of the...

Development of targeted FGFR2 therapies in cholangiocarcinoma (Overcoming adverse effects and acquired drug resistance)

6/ 4/24

Cholangiocarcinoma (CCA) is the second most common primary hepatic malignancy after hepatocellular carcinoma, representing ~2% of all cancer-related deaths worldwide yearly¹⁾. Surgery is a potential curative option for CCA. However, frequent post-surgical relapse appears, and furthermore, many tumors are unresectable since most patients (~70%) are diagnosed at late stages due...

Cancer treatments using inhibitors of CDK, a cell cycle regulator

2/22/24

Therapeutic potential of CDK2 inhibitors targeting HR+/HER2- breast cancer with CDK4/6 inhibitor resistance and CCNE1-amplified cancer Since the discovery of key regulators of the cell cycle by Dr. Hartwell et al. who were awarded the Nobel Prize in Physiology or Medicine in 2001, research focused on the molecular mechanism of...

Comparative biochemical kinase profiling of VEGFR2 inhibitors

8/10/23

Vascular endothelial growth factor receptor 2 (VEGFR2) is a key regulator of tumor angiogenesis, the formation of new blood vessels from existing vasculature. VEGFR2 has been an attractive target for anti-cancer therapy. However, clinical application of available VEGFR2 inhibitors has been challenged by limited efficacy and a wide range of...

ALK drug resistant mutations: Challenges for the treatment of lung cancer

2/22/23

ALK gene rearrangements are associated with NSCLC Abnormal anaplastic lymphoma kinase (ALK) fusion genes are present in approximately 5% of patients with non-small cell lung cancer (NSCLC)¹⁾. In ALK fusion proteins, the kinase domain of ALK is fused to the oligomerization domain of partner proteins²⁾ (Fig.1). Although normal ALK protein...