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【drug-news】Entremed公司出示了微管蛋白抑制剂治疗
Entremed Presents Preclinical Data For Tubulin Inhibitors In Oncology
EntreMed, Inc. (Nasdaq: ENMD), a clinical-stage pharmaceutical company developing therapeutics for the treatment of cancer and inflammatory diseases, announced the presentation of results for its preclinical tubulin inhibitor program. The data were presented by EntreMed scientists at the 18th European Organization for Research and Treatment of Cancer, National Cancer Institute, American Association for Cancer Research (EORTC-NCI-AACR) Symposium on "Molecular Targets and Cancer Therapeutics" at the Prague Congress Centre in Prague, Czech Republic.
Tubulins are the proteins that form microtubules, which are key components of the cellular cytoskeleton (structural network). Microtubules are necessary for cell division (mitosis), cell structure, transport, signaling and motility. Given their primary role in cell division, microtubules have been an important target for anticancer drugs -- often referred to as tubulin inhibitors or microtubule targeting agents. These compounds bind to tubulin protein, either in the monomer form or polymerized in microtubules, and prevent cancer cell proliferation by interfering with the microtubule dynamics required for cell division. This interference blocks the cell cycle sequence, leading to cell death (apoptosis).
Results of the studies presented at the Prague meeting demonstrate that ENMD-1420 (previously CC-5079) inhibits tubulin polymerization and TNF-Alpha production and has both in vitro and in vivo antitumor activity. Each tubulin inhibitor in this class of compounds represented by ENMD-1420 can exist in two chemical configurations termed the Z or E isomer. In vitro studies with analogs related to ENMD-1420 showed that the Z isomer is more potent than the E isomer for antiproliferative activity. The potency difference ranges from 7 to 40-fold depending on the molecule and the cell line tested.
These molecules have potent in vitro antiproliferative and antiangiogenic effects against both tumor cells and endothelial cells. Preclinical data also suggest that these molecules have significant in vivo antitumor activity in a model of lung metastatic disease. This study shows that therapeutic dosing regimens can be developed with the Z isomers that result in antitumor activity in preclinical tumor models. Additionally, these data suggest that a synthetic strategy targeting a particular isomer can be used to optimize antitumor activity and lead compound identification.
Carolyn F. Sidor, M.D., M.B.A., EntreMed Vice President and Chief Medical Officer, stated, "We continue to make progress with the tubulin inhibitor program and the results of this study are an important component in reaching our goal of selecting a lead compound. ENMD-1420 and other tubulin inhibitors were licensed exclusively from Celgene Corporation in early 2005 for development in oncology. We remain on our year-end schedule of selecting several lead candidates for further optimization."
About EntreMed
EntreMed, Inc. (Nasdaq: ENMD) is a clinical-stage pharmaceutical company developing therapeutic candidates primarily for the treatment of cancer and inflammation. Panzem(R) (2-methoxyestradiol or 2ME2), the Company's lead drug candidate, is currently in Phase 1 and 2 clinical trials for cancer, as well as in preclinical development for rheumatoid arthritis. MKC-1, an oral cell cycle regulator, is in Phase 1 and 2 clinical trials for cancer. ENMD-1198, a novel tubulin binding agent, is also in Phase 1 studies in advanced cancers. EntreMed's goal is to develop and commercialize new compounds based on the Company's expertise in angiogenesis, cell cycle regulation, signaling pathways, and inflammation -- processes vital to the treatment of cancer and other diseases, such as rheumatoid arthritis. Additional information about EntreMed is available on the Company's website at http://www.entremed.com and in various filings with the Securities and Exchange Commission. 本人已经认领此文，如在48小时内未能提交译文，其他战友可自由认领。 EntreMed, Inc. (Nasdaq: ENMD), a clinical-stage pharmaceutical company developing therapeutics for the treatment of cancer and inflammatory diseases, announced the presentation of results for its preclinical tubulin inhibitor program. The data were presented by EntreMed scientists at the 18th European Organization for Research and Treatment of Cancer, National Cancer Institute, American Association for Cancer Research (EORTC-NCI-AACR) Symposium on "Molecular Targets and Cancer Therapeutics" at the Prague Congress Centre in Prague, Czech Republic.
EntreMed是一家临床期药物公司，开发治疗癌症和炎症疾病药物，宣布了微管蛋白抑制剂临床前研究结果。该资料在布拉格会议中心召开的分子靶向和癌症治疗EORTC-NCI-AACR座谈会上发表。
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作者:admin@医学,生命科学 2011-05-28 17:11
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