Category: Small Cell Lung Cancer

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...

CC-90011 is a Selective and Orally Active Inhibitor of LSD1

Lysine-specific histone demethylase 1 (LSD1) (also known as KDM1) is a member of a broad family of monoamine oxidases and is encoded by the KDM1A gene. However, LSD1 requires the flavin adenine dinucleotide (FAD) as a cofactor to catalyze demethylase activity. For example, LSD1 catalyzes demethylation at H3K4me1/2 and...

Trilaciclib is an Orally Active CDK4 and CDK6 Inhibitor

The cell cycle is a highly conserved process. Additionally, this process must maintain genomic integrity and replicative capacity for proper cell maintenance and proliferation. The cell cycle consists of four distinct phases: G1 or Gap1 phase, G2 or Gap2 phase, and M phase. As we all know, the G1...

MCP110 is an Inhibitor of Ras/Raf-1 Interaction

Ras is a small GTPase and interacts with the protein Raf to create activated Ras-Raf complex that activates the downstream effectors in the ERK pathway. Malfunctioning Ras-Raf switches cause cancer. Ras-Raf interaction has taken a center stage in cancer research. Ras is a peripheral membrane protein that acts as...

JNJ-64619178 is a Selective PRMT5 Inhibitor with Potent Activity In Lung Cancer

Protein arginine methylation, a common post-translational modification, involves in numerous cellular processes including transcription, DNA repair, mRNA splicing and signal transduction. Protein arginine methyltransferases (PRMTs) catalyze arginine methylation on both chromatin-bound and cytoplasmic proteins. Currently, there are nine protein arginine methyltransferases (PRMTs) encoded in mammalian genomes. Each PRMT isoform...