Category: Breast Cancer

AGN194204 is an Orally Active and Selective RXR Agonist

Rexinoids are selective ligands for the retinoid X receptors (RXRα, RXRβ, and RXRγ). Specifically, rexinoids are multifunctional drugs that are useful for both the prevention and treatment of lung and breast cancer in preclinical animal models. Besides, retinoid X receptors heterodimerize with other receptors in the nuclear receptor superfamily. They modulate the activities of numerous steroid-like...

6RK73 is a Covalent Irreversible and Specific UCHL1 Inhibitor

Approximately 90% of breast cancer-related deaths are due to metastasis. During the metastasis process, epithelial-mesenchymal transition (EMT) plays an important role. The secreted cytokine transforming growth factor-β (TGFβ) can induce it. Breast cancer has multiple subtypes with distinct metastatic potential based on genetic and clinical features. The most aggressive...

BCI-215 is a Tumor Cell-Selective DUSP-MKP Inhibitor

Mitogen-activated protein kinase phosphatases (MKPs) belongs to the dual-specificity phosphatase (DUSP) family. DUSP-MKPs dephosphorylate and inactivate the MAPKs extracellular signal-regulated kinase (ERK), JNK/SAPK, and p38 on tyrosine and threonine residues. As a result, they result in regulating the duration and amplitude of mitogenic and survival signaling. There exists a ...

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...

CWP232228 is a Highly Potent and Selective Wnt/β-catenin Inhibitor

Conventional chemotherapy and radiation induce more and more breast cancer stem cells (BCSC) resistance. In recent years, increasing studies have suggested that the dysregulation of Wnt/β-catenin signaling occurs in breast cancer. A study from Gyu-Beom Jang, the researchers showed that the level of Wnt/β-catenin signaling in BCSC is relatively...

D-I03 is a Selective RAD52 Inhibitor

DNA repair is very important for the maintenance of genome integrity in all organisms. Different exogenous agents or genotoxic products of metabolism cause multiple DNA repair systems evolved to eliminate a broad variety of DNA lesions. In normal cells, the specificities of different DNA repair mechanisms overlap to assure...