Macrocyclic Lactams

02/14/2002 - "Thus, pharmacological inhibition of Akt activation is achievable with ansamycins and may be useful for the treatment of HER2 driven tumors."
05/02/2006 - "Therefore, the in vivo accumulation of the high-affinity dihydroquinone ansamycins in tumor cells contributes to the antitumor activity of these compounds and alters our understanding of the active species driving the efficacy of this class of compounds."
06/01/2021 - "Ansamitocin (AP-3) is an ansamycins antibiotic isolated from Actinosynnema pretiosum and demonstrating high anti-tumor activity. "
06/01/2011 - "Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity."
04/01/2009 - "The ansamycins, such as geldanamycin and 17-allylamino-17-demethoxygeldanamycin (17-AAG) act as specific HSP90 inhibitors, are potent anti-tumor agents and are currently undergoing clinical trials. "

08/01/2001 - "Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. "
08/01/2001 - "Münster et al., Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. "
10/01/2006 - "An isogenic pair of human breast cancer cell lines, MDA468 and MDA468/NQ16, differing in expression of NQO1, was used, and HPLC analysis showed that hydroquinone ansamycins were formed by the MDA468/NQ16 cells, which could be prevented by ES936 pretreatment. "
04/01/2001 - "Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells."

05/01/2005 - "PC-3M prostate carcinoma cells were treated in vitro with increasing radiation doses in the presence or absence of Hsp90-active and Hsp90-inactive benzoquinone-ansamycins. "
01/01/1999 - "We evaluated the effects of benzoquinone ansamycins on FAK steady-state protein level and FAK half-life in breast and prostate carcinoma, Ewing's sarcoma, and 3T3 fibroblasts. "

05/01/2011 - "The benzoquinone ansamycins inhibit the ATPase activity of the 90-kDa heat shock protein (Hsp90), disrupting the function of numerous client proteins involved in oncogenesis. "

02/15/2013 - "In contrast to ansamycins, PU-H71 weakly affects EAE clinical course. "