PALO ALTO, Calif., April 17 /PRNewswire-FirstCall/ -- Telik, Inc. (Nasdaq: TELK), a biopharmaceutical company focused on discovering and developing drugs to treat serious diseases, today announced that it made four preclinical data presentations at the 99th Annual Meeting of the American Association for Cancer Research (AACR) in San Diego, Calif. The abstracts highlighted results from Telik's Research and Development programs.
Identification and Characterization of Novel Tyrosine Kinase Inhibitors
Targeting Vascular Endothelial Growth Factor Receptor 2 [Abstract # 1439]
Inhibition of the vascular endothelial growth factor receptor signaling
pathway with antibodies or small molecules has been proven effective as an
anti-cancer therapy. Through the use of Telik's Target-Related Affinity
Profiling (TRAP(R)) screening technology, novel inhibitors of VEGFR2
kinase were discovered. The inhibitors belong to nine structural classes,
among which E2B8 and EAAF are sub-micromolar inhibitors of the kinase.
Mechanism of Induction of Apoptosis by TLK199 (TELINTRA(R)) in Human
Leukemia Cell Lines [Abstract # 2270]
Telik researchers conducted studies with data highlighting TLK199, a novel
glutathione analog inhibitor of the enzyme glutathione S-transferase P1-1,
which induces apoptosis, or programmed cell death, in human HL60
promyelocytic cells and TF-1 erythroleukemic cells. Treatment of the
leukemia cells with TLK199 also resulted in an increase of the
phosphorylation of eIF2alpha, a key signaling event in the integrated
stress response (ISR), and in induction of multiple genes implicated in
ISR. Telik currently has ongoing studies of TLK199 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 diseases. The company's most advanced investigational drug candidates in clinical development are TELINTRA, a modified glutathione analog for the treatment of cytopenias due to myelodysplastic syndrome or chemotherapy, and TELCYTA(R), a tumor-activated prodrug for the treatment of advanced ovarian cancer and non-small cell lung cancer. Telik's product candidates were discovered using its proprietary drug discovery technology, TRAP, which enables the rapid and efficient discovery of small molecule drug candidates.
TELIK, the Telik logo, TELCYTA, TELINTRA and TRAP are trademarks or registered trademarks of Telik, Inc.
|SOURCE Telik, Inc.|
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