Tag: MCF-7

Elacestrant is an Orally Available SERD (Estrogen Receptor Degrader )

Estrogen receptor (ER) is a ligand-induced intracellular transcription factor that mediates the biological effects of estrogen at the level of most gene regulation. The biological effect of estrogen is mediated by ER, which is a member of nuclear receptor family. Specifically, these receptors act as ligand-activated transcription factors. There...

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...