Category: Colorectal Cancer

PR-619 is a Broad-Range DUB Inhibitor

Ubiquitination is a post-translational modification where the polypeptide ubiquitin is attached to lysine residues of substrate proteins. This process is reversible, and ubiquitin removal is orchestrated by a large family of deubiquitinating enzymes (DUBs). DUBs fall into six subfamilies based on sequence and domain similarity. Ubiquitination and deubiquitination together...

PF 477736 is a Selective and ATP-Competitive Inhibitor of Chk1

Cancer is a multiplicity of diseases characterized by a range of molecular defects leading to unregulated, aberrant cell growth. Checkpoints are present in all phases of the cell cycle. Checkpoints act as gatekeepers maintaining the integrity of the genome. Researchers use anti-tumor agents to treat cancer by imparting damage...

E7820 is an α2 Integrin Inhibitor with Anti-Tumor Activity

Vascular endothelial growth factor (VEGF) is a prime contributor to tumor angiogenesis. Most tumor cells produce high levels of VEGF and VEGF receptors associated with tumor endothelial cells. E7820 is an aromatic sulfonamide derivative and an Angiogenesis inhibitor. E7820 inhibits in vitro proliferation and tube formation of human umbilical...

MSAB is a Selective Inhibitor of Wnt/β-Catenin Signaling

Wnt/β-catenin signaling regulates key cellular functions including proliferation, differentiation, migration, apoptosis, and stem cell renewal. The β-catenin is a core component of the cadherin protein complex, whose stabilization is essential for the activation of Wnt/β-catenin signaling. In this study, researchers screen for small molecule compounds that act against Wnt/β-catenin...

TAI-1 is an Orally Active and Highly Potent Hec1 Inhibitor

Hec1 (Ndc80) is one of the outer kinetochore proteins and forms heterotetramers with proteins NUF2, SPC25, and SPC24. Specifically, drugs that interfere with mitosis are part of the most successful chemotherapeutic compounds for cancer in clinical practice. Hec1, a component of mitochondria, is overexpressed in a variety of human...

LY3214996 an Orally Active ERK1/2 Inhibitor with Potential Antineoplastic Activity

The Ras/Raf/MEK/ERK signaling cascade integrates extracellular clues from cell surface receptors to gene expression and regulation of multiple cellular proteins. Extracellular-signal-regulated kinases (ERKs) serve as key central nodes within this pathway. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

S130, Targeting ATG4B, Inhibits Autophagy and Activates Apoptosis in Colorectal Colon Cancer

Autophagy is an evolutionarily conserved and stress-responsive catabolic process. Particularly, cellular components and damaged organelles are sequestered within autophagosomes for lysosomal degradation. Autophagy is a multi-step process. Autophagosome biogenesis requires 2 ubiquitin-like conjugation systems: the Atg12-Atg5 and the Atg8–phosphatidylethanolamine (PE) systems. Importantly, the cysteine protease ATG4B is a key...