Category: Colorectal 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...

Birinapant (TL32711), a Bivalent Smac Mimetic, is an Antagonist for XIAP and cIAP1

XIAP is a protein that prevents apoptosis. XIAP is a member of apoptosis protein family (IAP) inhibitors. Specifically, IAP blocks cell death in vitro and in vivo by inhibiting different caspases. The caspase inhibitory activity of XIAP is negatively regulated by at least two XIAP interacting proteins XAF1 and...

PTC-209 is a Specific BMI-1 Inhibitor and Impairs the Tumor Microenvironment

Glioblastoma multiforme (GBM) is the most common and aggressive brain tumor and refractory to existing therapies. BMI-1 is part of the polycomb repressive complex 1 (PRC1). There is a statistically significant correlation between the high frequency of BMI-1-positive tumor cells and poor prognosis of patients according to the data...

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...

SHP394 is an Orally Active and Selective Inhibitor of SHP2

SH2 containing protein tyrosine phosphatase-2 (SHP2) is an oncogenic phosphatase. SHP2 facilitates growth and survival signaling downstream of numerous receptor inputs. In addition, higher levels of SHP2 phosphorylation associate with decreased survival of breast cancer patients. Especially, SHP394 is an orally active and selective inhibitor of SHP2. Pharmacological inhibition...

Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor

ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...

Elimusertib is an Orally Available and Selective ATR Inhibitor

TM serine/threonine kinase (ATM) is a serine/threonine-protein kinase and can be recruited and activated by DNA double-strand breaks. Specifically, ATM phosphorylates several key proteins. These proteins initiate the activation of DNA damage checkpoints, leading to cell cycle arrest, DNA repair, or apoptosis. Besides, ATM belongs to the superfamily of...