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A peptidomimetic is a small protein-like chain (a peptide) that contains both natural and nonnatural amino acids. It is designed and synthesized with the purpose of binding to target proteins in order to induce cancer cells into a form of programmed cell death called apoptosis. Basically, a peptidomimetic works by mimicking key interactions that activate apoptotic pathway in the cell.
All healthy cells in metazoa (multi-celled animals) are subject to programmed cell death when they are no longer wanted; but cancer cells have the ability to evade apoptosis and the body's attempts to get rid of them. So peptidomimetics are part of the wide effort by researchers, research labs and institutions to create cures for cancer by means of restoring or activating apoptotic pathways in specific cells.
An impressive advance in this effort was reported by Loren D. Walensky and colleagues in the 3 September 2004 issue of the journal Science [1] (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15353804). This team succeeded in reducing a variety of human leukemic cells that had been xenografted (transplanted) into mice. The peptidomimetic that they succeedid in synthesizing, SAHB (stabilized alpha-helix of BCL-2 domains) specifically activates the mitochondrial apoptotic pathway in the aforementioned malignant cells (see intrinsic and extrinsic inducers of the apoptotic process), without harming healthy tissues.
Lin Li and co-workers reported another impressive advance in the same issue of Science [2] (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15353805). They were able to synthesize a molecule that mimics the proapoptotic protein called SMAC (whose function is described in biochemical execution of apoptosis).
Further reading
Denicourt, Catherine, and Dowdy, Steven F.: "Targeting Apoptotic Pathways in Cancer Cells", Science Vol. 305 p. 1411, 3 Sept. 2004 [3] (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15353788).
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