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February 28, 2011 - Volume 89, Number 9
- p. 48
Science & Technology Concentrates
More Science & Technology Concentrates
- Sequestered Antibiotics
- Shuttling drugs away from their intended targets can sometimes transform them into good antimicrobials.
- A Revised Picture Of Deep-Earth Sulfur
- Under extreme conditions, sulfur may exist as S3-, rather than the presumed sulfide and sulfate species.
- Picking Prion Infectivity Apart
- New research suggests that infectious protein misfolding and Prion diseases’ neurological toxicity are independent processes.
- Iron(V) Nitride Mimics Nitrogenase Activity
- Chemists have isolated a rare Fe≡N complex and show that it readily produces ammonia.
- Catalytic Methanol Coupling Achieved
- An iridium complex catalyzes the direct C–H functionalization of methanol, a first for the single-carbon compound.
- Fish Poop Establishes A Geologic Record
- Scientists find that the aquatic vertebrates generate a large portion of the carbonate mud that deposits on the ocean floor.
- Palladium-Allyl Bridges Snatch CO2
- Unusual double-bridging complexes reveal their ability to insert CO2 and form carboxylates.
- Peptide Induces Hair Regrowth In Mice
- Astressin B helps genetically altered mice to regain skin pigmentation and regrow nearly all their hair.
Topics Covered
J. Am. Chem. Soc.
Peptide-conjugated methotrexate (green) accumulates in the cytoplasm of bacteria (top) and the mitochondria (red) of human cells (bottom).
Shuttling drugs away from their intended targets can transform compounds that might otherwise be too toxic for people into good antimicrobials, according to researchers at the University of Toronto. Shana O. Kelley and Mark P. Pereira attached a mitochondria-targeting peptide to the cancer drug methotrexate and demonstrated the drug’s antimicrobial abilities (J. Am. Chem. Soc., DOI: 10.1021/ja110246u). The researchers show that the conjugate accumulates in mitochondria in human cells, where it can’t reach its enzyme target, but in the cytoplasm in bacteria. In cell culture, the conjugate killed a broad range of bacteria, including methicillin-resistant Staphylococcus aureus, a microbe resistant to most drugs. Kelley’s group is starting to study animals to see whether the drug retains its activity and reduced toxicity. The approach could be general for other drugs, provided they have a convenient “synthetic handle to tinker with,” Kelley says. The demonstration with methotrexate “opens the door to using similar strategies to revisit or repurpose old molecules that may have been discarded at early stages of antibiotic development,” says infectious disease expert Gerard D. Wright of McMaster University, in Hamilton, Ontario.
- Chemical & Engineering News
- ISSN 0009-2347
- Copyright © 2011 American Chemical Society
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