Poly ADP Ribose Polymerase (PARP) Inhibitors are a group of compounds used in the treatment of cancer. They are unique in their ability to specifically target cancerous cells. PARP proteins are responsible for repairing single-strand breaks in DNA, and when inhibited result in double strand breaks during the raid DNA replication that is characteristic of cancers. This collection of double...
- Staurprimde is a semi-synthetic analog of the staurosporine family of indolocarbazoles. The study conducted by Zhu, et al (2009) found Stauprimide increases efficiency of directed Embryonic Stem Cells (ESC) differentiation. Stauprimide promoted induction of Sox17 / Sox 7 cells in both mouse and human ESC, and also helped induce extensive endoderm differentiation markers in the mouse ESC. Early stauprimide treatment was found to enhance later differentiation of the cells toward hepatic and pancreatic lineages. Additionally the study shows Staurpimide binds NME2, impairing nuclear localiz
- A large new epidemiological study appears to provide further evidence that regular intake of fiber from fruits, vegetables and whole grains is associated with a reduced risk of developing breast cancer in women.
- TGF-Î² superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases. Here, we characterize a small molecule inhibitor (SB-431542) that was identified as an inhibitor of activin receptor-like kinase (ALK)5 (the TGF-Î² type I receptor).
- Improving reagent performance in immunoassays both to enhance assay sensitivity and to minimize interference are ongoing challenges in clinical diagnostics. We describe herein the syntheses of a new class of hydrophilic reagents containing sulfobetaines zwitterions and their applications.
- There is extensive evidence that necrosis plays a prominent role in a wide range of human pathological conditions, such as myocardial infarct, ischemic injury and neurodegeneration. Therefore, development of necrosis inhibitors is of high interest.
- In a study on how the ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-Î², A-83-01 was synthesized and characterized a small molecule inhibitor. It is structurally similar to previously reported ALK-5 inhibitors developed by Sawyer et al. (2003) and blocks signaling of type I serine/threonine kinase receptors for cytokines of the TGF-Î² superfamily (known as activin receptor-like kinases; ALKs).
- Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis.
- Activation of the hedgehog pathway has been implicated in the development of cancers in various organs, including brain, lung, mammary gland, prostate and skin. Basal cell carcinoma, the most common form of cancerous malignancy, has the closest association with hedgehog signaling.