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Telik Presents Preclinical Data at 99th Annual Meeting of the American Association for Cancer Research
Date:4/17/2008

LK199 in clinical

development for the treatment of myelodysplastic syndrome (MDS).

Identification of a Novel Class of Nonpeptidyl Small-Molecule Inhibitors of the Human Proteasome [Abstract # 3271]

The ubiquitin-proteasome system (UPS) mediated protein turnover underlies

many signaling pathways that are fundamental to cell proliferation,

survival and death. Many important cellular proteins that are

dysregulated in cancer are proteasome substrates. Telik researchers have

identified multiple nonpeptidyl small-molecule hits that inhibited human

proteasome activity both biochemically and in cells. The best series

exhibited many desirable features including excellent cellular specificity,

equal activity against all three proteolytic sites of the proteasome, and

potent and broad anti-tumor activity in vitro.

Target-Related Affinity Profiling (TRAP(R)): Efficient Cancer Drug Discovery at Telik [Abstract # 4754]

Compounds for these preclinical studies came through the use of Telik's

TRAP technology, which provides an alternative screening method that is

based on a unique molecular descriptor called an affinity fingerprint. An

affinity fingerprint is based on the binding energy of small molecules to

proteins. Advanced computational methods are used to determine affinity

fingerprints, and to select compounds for screening. Advantages to using

TRAP include: a "low throughput" approach using complex, physiologically

relevant assays; identification of small molecule drug leads after testing

as few as 200 compounds; high level of success against a wide range of

cancer targets; enables scaffold hopping; and can speed the optimization

of small molecule drugs.

Telik, Inc. of Palo Alto, CA, is a biopharmaceutical company focused on discovering, developing and commercializing novel small molecule drugs to treat serious d
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SOURCE Telik, Inc.
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