Newsletter

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...

DGKα and DGKζ are key targets for cancer immunotherapy

9/ 1/22

DGKα and DGKζ are downregulators of TCR-mediated activity One of the most recent innovations in cancer therapy is harnessing and awakening a patient’s own immune system to target their tumor burden. These revolutionary methods include the expensive CAR-T cell therapies, but also include direct targeting of immune pathways with small...

The potential of PIKfyve inhibitor as a treatment of amyotrophic lateral sclerosis (ALS)

7/ 6/22

Amyotrophic lateral sclerosis (ALS) ALS is a fatal neurodegenerative disease characterized by the selective and progressive degeneration of motor neurons in the brain, brainstem and spinal cord. Motor neuron deterioration leads to muscle weakness and results in death of the patient due to respiratory failure, typically within 3 to 5...

The importance of understanding the activity of compounds on RAF dimerization in BRAF inhibitor drug discovery

3/ 2/22

RAF protein kinases (ARAF, BRAF and CRAF) are key components of the RAS-RAF-MEK-ERK signaling cascade. An upstream signal such as from a receptor tyrosine kinase allows RAS to convert to the active GTP-bound form. The GTP-bound RAS binds RAF proteins, inducing RAF dimerization which then activates the downstream MEK-ERK signaling¹⁾...