Members of the RAS family of GTPases (which comprises KRAS, NRAS, and HRAS) are major oncogenes. Especially, mutations in the RAS genes are major oncogenes with a high occurrence rate…
Chronic myeloid leukemia is a myeloproliferative disorder characterized by the presence of the oncogenic fusion protein BCR-ABL1. ABL1, one of the fusion partners in the BCR-ABL1 protein, contains an allosteric…
BRD4 (Bromodomain-containing protein 4) belongs to the BET family, which also contains BRD2, BRD3, and BRDT. BRD4 has two bromodomains to recognize acetylated lysine residues. They are BD1 and BD2.…
Yesterday, I introduced AMG 232 as a potent, selective and orally available inhibitor of p53-MDM2 interaction. Additionally, we have known the significance of MDM2-p53 interaction in cancer development. Today, I’d…
The p53 tumor suppressor induces cell growth arrest and apoptosis in response to DNA damage or stress. And inactivation of the p53 pathway plays an indispensable role in tumor survival.…
The occurrence of many cancers is due to a mismatch of chromosomes. It leads to the formation of aneuploidy and incomplete genes, and hence triggering an imbalance of cell cycles…
CDK6 plays a significant role in cell cycle entrance. However, overexpression of CDK6 correlates to CDK4/6 inhibitor resistance in breast cancer cell lines and patient samples. Moreover, point mutation of…
SPIN1 (Spindlin 1) is a chromatin reader protein. It recognizes trimethylated histone H3 lysine 4 (H3K4me3) through the protein-protein interaction at the defined “aromatic cage” in Tudor domain II. The…
Phosphoglycerate dehydrogenase (PHGDH) is an essential enzyme catalyzing the synthesis of amino acid serine. PHGDH is important for maintaining the poorly differentiated, stem-like state of cancer stem-like cells (CSLCs). Typically,…
The three human RAS genes encode four RAS proteins, with two KRAS isoforms. The two KRAS isoforms arise from alternative RNA splicing KRAS4A and KRAS4B. The 3 human RAS genes…