ansamycin


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ansamycin

Any of a family of chemicals (e.g., the rifamycin family)
which have antibacterial, antitubeculous, antiviral and possibly also antineoplastic activity.
References in periodicals archive ?
Rifalazil represents the lead compound in a new generation of ansamycin antibiotics, with very long acting antibacterial potency, to be commercialized by ActivBiotics.
In addition to rifalazil, ActivBiotics expects to have a full pipeline of long lasting, extremely potent ansamycins with broad spectrum coverage in clinical development during this timeframe.
Ono Y, Kozai Y, Ootsu K (1982) Antitumor and cytocidal activities of a newly isolated benzenoid ansamycin, macbecin I Gann 73: 938-944
Among the viral inhibitors; suramin, HPA23, phosphonoformate, ribavirin, interferon, ansamycin.
Abstract 5636, "Correlation between In Vitro and In Vivo Activities of Hsp90 Inhibitors," presented data showing the KOS-2484, Kosan's lead non-benzoquinone ansamycin, has demonstrated the tightest binding affinity for Hsp90 reported to date, accumulates in tumor cells and has superior retention properties leading to a long lifetime in tumor tissue.
Abstract 5630, "Anti-Tumor Activity of Non-Benzoquinone Ansamycin Hsp90 Inhibitors in Murine Xenograft Models," presented data showing that KOS-2484 induces tumor regression at well-tolerated doses in xenograft models of both liquid and solid tumors, including acute myelogenous leukemia (AML), multiple myeloma and colon cancer models.
Our plan is to continue on the path of drug development with our new generation of ansamycin antibiotics shown to be uniquely effective in vitro and in vivo against Chlamydia.
Development of these early Hsp90 inhibitors, however, has been hampered by several drawbacks, including the hepatotoxicity associated with chemical properties of this ansamycin family of compounds.
Ganetespib is able to enter the ATP binding pocket of Hsp90 in either the open or closed pocket lid conformation, whereas due to their larger size the ansamycin analogs can only occupy the ATP binding pocket in the open pocket lid conformation.