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...
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...
Olafertinib is a Third-Generation EGFR TKI
Non-small-cell lung carcinoma (NSCLC) is any type of epithelial lung cancer other than small-cell lung carcinoma (SCLC). NSCLC patients with activating EGFR mutations initially respond to first-generation EGFR inhibitors. Epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein with an extracellular epidermal growth factor binding domain and an intracellular...
UZH1a is a Selective METTL3 Inhibitor
METTL3/14 plays a critical role in disorders associated with abnormal self-renewal, aberrant proliferation, and blocking differentiation of hematopoietic cells. Both METTL3 and METTL14 are upregulated in all subtypes of AML, despite the heterogeneity of this blood cell cancer in terms of chromosomal rearrangement and gene mutations. AML and B-cell...
DBPR112 is an Orally Active EGFR (both WT and Mutant) Inhibitor
Epidermal growth factor receptor (EGFR), a transmembrane protein, is a receptor of EGF family members of extracellular protein ligands. Specifically, EGFR expresses at elevated levels in different forms of cancer and is usually positively relevant to cancer progression and adverse prognosis. Different mutant forms of this protein also contribute...
YUM70, a Selective GRP78 Inhibitor, Induces ER Stress-Induced Apoptosis
GRP78 (Glucose-regulated protein, 78 kDa) is a key regulator of endoplasmic reticulum (ER) stress signaling. In this study, researchers describe the discovery of a series of GRP78 inhibitors. YUM70 is an ER stress inducer and kills cells by activating the apoptosis pathway. Especially, YUM70 treatment induces ER stress and...
TPP-1 is a Potent Inhibitor of the PD-1/PD-L1 Interaction
PD-L1 is expressed in many types of cancers. And its high expression in tumor cells or presence in TME can be indicative of tumor-infiltrating lymphocytes (TILs). Blockade of PD-1/PD-L1 can strengthen the function of effector T cells. Blockade of PD-1/PD-L1 can strengthen the function of effector T cells. Additionally,...