Focus New

Filipin III for Cholesterol Research

Filipin III is a microbial natural product isolated from Streptomyces filipinensis. It is an important fluorescent probe for cellular cholesterol detection. In addition, because it binds to cholesterol it is used to disrupt lipid rafts in cells (T Hayashi for a recent example). Cholesterol plays important roles in membrane trafficking, lipid metabolism, and diseases such …

Filipin III for Cholesterol Research Read More »

Sinefungin in Antiviral Research

Two recent papers employed Sinefungin in determination of the structure of two different viral methyltransferases. Sinefungin is a Streptomyces natural product analog of S-adenosylmethionine acting as a MTase inhibitor. In an Antiviral Research paper by DS Ferrero and coworkers, the Usutu virus MTase domain was cocrystalized with Sinefungin. In another paper by Kottur and coworkers …

Sinefungin in Antiviral Research Read More »

Obesity research news

Carlos Guijas and coworkers at Scripps recently found that the leukotriene antagonist and antiasthmatic agent zafirlukast was able to differentiate adipocyte precursors into functional brown adipocytes. A drug-initiated metabolomics study then identified N-myristoylglycine as the endogenous signaling lipid which mediated the response. Experiments with N-myristoylglycine alone mimicked the effect of zafirlukast.

Romidepsin attenuates growth of rare sarcomas

Yuki Yoshimatsu and coworkers have shown that they could establish patient-derived cancer cell lines for myxofibrosarcoma and pleomorphic sarcoma. After screening these cell lines with a number of cancer drugs they found that romidepsin, a novel microbial product HDAC inhibitor demonstrated considerable antiproliferative effect on these cells.

Inducing Autophagy Against Mycobacterial Infection

Activation of autophagy is a novel mode of therapeutic intervention and offers the possibility of developing new “host-directed” therapeutics against mycobacterial infection. For example, Kim et al. found that thiostrepton, a complex microbial product, offers a dual MOA by first targeting the bacterial ribosome and second, by induction of ER stress-mediated autophagy to promote the …

Inducing Autophagy Against Mycobacterial Infection Read More »

HDAC3 Inhibition Stimulates Myelination

Robert Prior and coworkers report in a recent issue of Molecular Neurobiology that inhibition of HDAC3 with RGFP966, a highly selective HDAC3 inhibitor, stimulates myelination in a CMT mouse model. CMT (Charcot-Marie-Tooth disease) is the most common inherited peripheral neuropathy and is characterized by dysmyelination of peripheral nerves.