Category: Breast Cancer

FLTX1, a Fluorescent Tamoxifen Derivative, Specifically Labels Intracellular Binding Sites (ER)

Tamoxifen is a nonsteroidal agent and competitively binds to estrogen receptors (ER). This compound itself is a prodrug and it has a relatively little affinity for ER. However, tamoxifen can transform into active metabolites 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen (endoxifen). Besides, these metabolites exhibit 30–100 times more affinity with the estrogen...

Conglobatin, an Orally Active Hsp90 Inhibitor, Disrupts Hsp90-Cdc37 Complex Formation

Heat shock protein (Hsp) 90 is a chaperone protein. In addition to protecting cells by correcting misfolded proteins, Hsp90 also plays a key role in regulating the stability, maturation, and activation of a wide range of client substrates, including kinases, hormone receptors, and transcription factors. Most Hsp90 client proteins,...

ENMD-1198, an Orally Active Tubulin-Binding Agent, Reduces HIF-1α and STAT3 Activity

Hepatocellular carcinoma (HCC) is the fifth most cancer worldwide, with a continuously increasing incidence. HCC represents a hyper vascularized tumor and its progression is closely related to angiogenesis. Hepatocellular carcinoma overexpresses the vascular endothelial growth factor (VEGF). The transcription factor HIF-1α also plays a central role in HCC progression...

AES-135 is a Potent HDAC Inhibitor

Pancreatic cancer is cancer that’s found anywhere in the pancreas. Histone deacetylases (HDACs) regulate the post-translational modification of histones and consequent gene expression. HDACs act as transcriptional repressors and overexpress in several types of cancer, including pancreatic cancer. HDAC inhibitors are effective in killing pancreatic cancer cells. In this...

PF-06843195 is a Selective PI3Kα Inhibitor

Phosphoinositide 3-kinases (PI3Ks) can catalyze the synthesis of the phosphatidylinositol (PI) second messengers, including PI(3)P (PIP), PI(3,4)P2 (PIP2), and PI(3,4,5)P3 (PIP3). The PI3K lipid kinase family contains three classes based on sequence homology. Class, I PI3Ks are further divided into class IA (PI3Kα, PI3Kβ, and PI3Kδ) and class IB...

KS15 is an Inhibitor of the Cryptochromes and CLOCK:BMAL1 Heterodimer Interaction

Cryptochrome (CRY), a circadian transcription factor, is a risk factor for the initiation of breast cancer. Cryptochrome inhibitor (KS15) has anti-tumor activity to human breast cancer cells. In this study, researchers evaluated the anti-proliferative and pro-apoptotic activity of KS15 in human breast cancer cells. KS15 decreases the speed of...

Triciferol is Both a VDR Agonist and HDAC Antagonist

The biologically active metabolite of vitamin D3, 1α,25-dihydroxyvitamin D3 (1,25D), is a primary regulator of calcium homeostasis. 1,25D also controls cell differentiation and proliferation through binding to the nuclear vitamin D receptor (VDR). It regulates histone acetylation, chromatin remodeling, and recruitment of RNA polymerase II and ancillary factors required...