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News & Views |
Virulence caught green-handed
Many of us eat mushrooms, but few of us have probably ever thought about — let alone witnessed — the epic battle of kingdoms that can occur between this delicacy and its bacterial pathogens. Now, imaging mass spectrometry has enabled the identification of a bacterium's potent antifungal weapon of choice.
- Laura M. Sanchez
- & Pieter C. Dorrestein
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News & Views |
Forcing an enemy into the open
A series of highly active, simplified analogues of the natural product bryostatin have been prepared. They offer an improved approach for the activation of latent HIV that could, in combination with current state-of-the-art antiretroviral therapy, offer hope for eventual eradication of the infection.
- Christian Melander
- & David M. Margolis
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Article |
Designed, synthetically accessible bryostatin analogues potently induce activation of latent HIV reservoirs in vitro
Simplified bryostatin analogues are shown to potently induce latent HIV expression in vitro. These analogues display comparable or better potency when compared with bryostatin. Moreover, they are up to 1,000-fold more potent in inducing latent HIV expression than prostratin, the current lead preclinical candidate.
- Brian A. DeChristopher
- , Brian A. Loy
- & Paul A. Wender
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News & Views |
A light touch to a deadly problem
Flow chemistry has grown in stature as a technique with the potential to deliver synthetic complexity with assembly-line-like efficiency. Application of flow technology to the front-line antimalarial drug artemisinin promises to revolutionalize treatment.
- Kevin Booker-Milburn
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Blogroll |
Blogroll: Arnie and artemisinin
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Article |
The transcription factor FOXM1 is a cellular target of the natural product thiostrepton
The natural product thiostrepton is known to have anticancer properties but its mechanism of action is not known. Here, it is shown that thiostrepton binds to the protein FOXM1, preventing its interaction with several gene promoters and inhibits their expression. This illustrates the druggability of transcription factors, and provides a molecular basis for targeting FOXM1.
- Nagaratna S. Hegde
- , Deborah A. Sanders
- & Shankar Balasubramanian
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Article |
Synthesis of 3-O-sulfonated heparan sulfate octasaccharides that inhibit the herpes simplex virus type 1 host–cell interaction
Oligosaccharides displayed at cell surfaces have important biological functions — such as controlling the entry of viruses — but a full understanding of this behaviour requires the synthesis of such compounds, which remains challenging. Here, two synthetic octasaccharides were shown to have remarkably similar inhibition of herpes simplex virus type 1 infection of cell cultures to the natural oligosaccharide identified in enzymatic studies.
- Yu-Peng Hu
- , Shu-Yi Lin
- & Shang-Cheng Hung
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News & Views |
Towards artificial terpene cyclases
The plant-derived sesquiterpene englerin A is a potent inhibitor of several renal cancer cell lines. Two recent total syntheses have utilized cationic gold(I)-complexes to coax readily available open-chain precursors into englerin's challenging oxotricyclic core with enzyme-like precision.
- Matthieu Willot
- & Mathias Christmann
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