Peptidomimetic

Peptidomimetic

A peptidomimetic is a small protein-like chain designed to mimic a peptide. They typically arise from modification of an existing peptide in order to alter the molecule's properties. For example, they may arise from modifications to change the molecule's stability or biological activity. This can have a role in the development of drug-like compounds from existing peptides. These modifications involve changes to the peptide that will not occur naturally (such as altered backbones and the incorporation of nonnatural amino acids).

An example of peptidomimetics were those 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, these work 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" [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 succeeded 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" [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 [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15353788] .

See also

*Apoptosis
*Cancer
*Beta-peptide
*Foldamers


Wikimedia Foundation. 2010.

Игры ⚽ Поможем сделать НИР

Look at other dictionaries:

  • peptidomimetic — noun pɛpˌtaɪdoʊmɪˈmɛtɪk A small protein like chain designed to mimic a peptide, but with altered chemical properties …   Wiktionary

  • Discovery and development of HIV-protease inhibitors — Many major physiological processes depend on regulation of proteolytic enzyme activity and there can be dramatic consequences when equilibrium between an enzyme and its substrates is disturbed. In this prospective, the discovery of small molecule …   Wikipedia

  • Jerini — Infobox Company company name = Jerini AG company company type = foundation = Berlin, Germany (1994) location=Berlin, Germany key people = Jens Schneider Mergener, CEO Adi Hoess, Chief Commercial Officer Jochen Knolle, Chief Scientific Officer,… …   Wikipedia

  • Discovery and development of renin inhibitors — Renin inhibitors are antihypertensive drugs that inhibit the first and rate limiting step of the renin angiotensin aldosterone system (RAAS). Since the 1970s scientists have been trying to develop potent inhibitors with acceptable oral… …   Wikipedia

  • Melanocyte-inhibiting factor — Systematic (IUPAC) name (S) N ((S) 1 (2 amino 2 oxoethylamino) 4 methyl 1 oxopentan 2 yl)pyrrolidine 2 carboxamide Clinical data MedlineP …   Wikipedia

  • Small molecule — In pharmacology, a small molecule is a small organic compound that is biologically active (biomolecule) but is not a polymer. This term is very loosely used and it may or may not include monomers or primary metabolites, in fact it is generally… …   Wikipedia

  • Ribonucleotide reductase — protein Name = ribonucleotide reductase M1 polypeptide caption = width = HGNCid = 10451 Symbol = RRM1 AltSymbols = EntrezGene = 6240 OMIM = 180410 RefSeq = NM 001033 UniProt = P23921 PDB = ECnumber = 1.17.4.1 Chromosome = 11 Arm = p Band = 15.5… …   Wikipedia

  • Peptoid — Peptoids, or N substituted glycines, are a specific subclass of peptidomimetics. They are closely related to their natural peptide counterparts, but differ chemically in that their side chains are appended to nitrogen atoms along the molecule s… …   Wikipedia

  • Beta-peptide — β peptides consist of β amino acids, which have their amino group bonded to the β carbon rather than the α carbon as in the 20 standard biological amino acids. The only commonly naturally occurring β amino acid is β alanine; although it is used… …   Wikipedia

  • Factor XI — Coagulation factor XI PDB rendering based on 1xx9 …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”