Category: Colorectal Cancer

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...

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...