Purine-scaffold Hsp90 inhibitors Journal Article
| Authors: | Chiosis, G.; Tao, H. |
| Article Title: | Purine-scaffold Hsp90 inhibitors |
| Abstract: | Heat shock protein 90 (Hsp90) has emerged as an important target, the inhibition of which is aimed at a wide range of cell transformations that lead to malignancy. A clinical evaluation of 17-AAG, the first Hsp90 inhibitor to enter the clinic, revealed evidence of activity for the compound at a manageable level of toxicity. However, clinical results have also demonstrated the limitations of this drug. The identification of novel Hsp90 inhibitor classes with improved structural characteristics and better pharmacological profiles has therefore become a major focus of interest in the field of cancer therapeutics. This feature describes the purine-scaffold class of Hsp90 inhibitors, focusing on research efforts from the discovery stage to the clinical translation of such compounds. © The Thomson Corporation. |
| Keywords: | cancer chemotherapy; unclassified drug; clinical trial; drug activity; nonhuman; antineoplastic agents; drug targeting; antineoplastic agent; animals; liver toxicity; drug structure; drug design; structure-activity relationship; cell transformation, neoplastic; cell transformation; neoplasms, experimental; heat shock protein 90 inhibitor; heat shock protein 90; hsp90 heat-shock proteins; malignant neoplastic disease; purines; drug bioavailability; drug blood level; malignant transformation; clinical trials; lactams, macrocyclic; purine; geldanamycin; radicicol; hsp90; ansamycin derivative; pu 3; 17 allylamino 17 demethoxygeldanamycin; 17 dimethylaminoethylamino 17 demethoxygeldanamycin; ipi 504; cancer therapeutics; purine scaffold; pu 24fc 1 |
| Journal Title: | IDrugs |
| Volume: | 9 |
| Issue: | 11 |
| ISSN: | 1369-7056 |
| Publisher: | Thomson Reuters (scientific) Ltd |
| Date Published: | 2006-11-01 |
| Start Page: | 778 |
| End Page: | 782 |
| Language: | English |
| PUBMED: | 17096299 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 13" - "Export Date: 4 June 2012" - "CODEN: IDRUF" - "Source: Scopus" |
