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New drugs


john

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Two new drugs. One says it is for breast cancer, but the target, HER2, also known as erbb2 is found in lung cancer.

Anticancer Drugs

Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab.

Cho, H.-S. et al. Nature 421, 756–760 (2003)

Overexpression of the receptor tyrosine kinase HER2 is found in 20–30% of breast cancer cases, and trastuzumab (Herceptin; Genentech) — a monoclonal antibody against HER2 — has been approved for the treatment of such patients. The authors report the crystal structure of human HER2 complexed with the Herceptin antigen-binding fragment, which reveals a region of the receptor that could be a promising target for the development of drugs with improved therapeutic properties.

Selective killing of cancer cells by -lapachone: direct checkpoint activation.

Li, Y. et al. Proc. Natl Acad. Sci. USA 100, 2674–2678 (2003)

The cell-proliferation cycle has inbuilt checkpoints at which apoptosis is activated if DNA damage is irreparable, thereby safeguarding genomic integrity. Many traditional anticancer drugs kill cancer cells by causing nonselective DNA damage, leading to activation of checkpoint-mediated apoptosis, but are therefore also toxic to normal cells. Li et al. report that -lapachone can selectively induce apoptosis in cancer cells through a regulatory pathway that links checkpoint activation with apoptosis, indicating that direct checkpoint activation could be a novel anticancer strategy.

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