Orally bioavailable farnesyltransferase inhibitors as anticancer agents in transgenic and xenograft models
| Autor: | M, Liu, W R, Bishop, L L, Nielsen, M S, Bryant, P, Kirschmeier |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Alkyl and Aryl Transferases
Administration Oral Biological Availability Antineoplastic Agents Apoptosis Mice Transgenic 3T3 Cells Fibroblasts Xenograft Model Antitumor Assays Mice Cell Transformation Neoplastic Genes ras Neoplasms Tumor Cells Cultured Animals Farnesyltranstransferase Humans Enzyme Inhibitors Cell Division |
| Zdroj: | Methods in enzymology. 333 |
| ISSN: | 0076-6879 |
| Popis: | The in vivo evaluation process described here was instrumental in the identification of SCH 66336 as a clinical candidate. Our lead FTI, SCH 66336, and several other FTIs are being evaluated in early-phase clinical trials to establish proof-of-principle for farnesyl transferase inhibition in human patients. The preclinical studies described here suggest that FTIs may have utility against a wide array of human cancers as a single agent and may, at least in some cases, lead to tumor regression. In addition, the results to date in combination with cytotoxic chemotherapeutic agents in animal models indicate that these combinations may enhance the clinical efficacy of FPT inhibitors. Further preclinical studies should help to guide the clinical development of this class of novel antitumor agents. |
| Databáze: | OpenAIRE |
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