263410-12-4Relevant articles and documents
Investigation of B,C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors for use as anti-breast cancer agents
Kim, Ho Shin,Hoang, Van-Hai,Hong, Mannkyu,Chul Kim, Kyung,Ann, Jihyae,Nguyen, Cong-Truong,Seo, Ji Hae,Choi, Hoon,Yong Kim, Jun,Kim, Kyu-Won,Sub Byun, Woong,Lee, Sangkook,Lee, Seungbeom,Suh, Young-Ger,Chen, Jie,Park, Hyun-Ju,Cho, Tae-Min,Kim, Ji Young,Seo, Jae Hong,Lee, Jeewoo
, p. 1370 - 1381 (2019/03/04)
On the basis of deguelin, a series of the B,C-ring truncated surrogates with N-substituted amide linkers were investigated as HSP90 inhibitors. The structure activity relationship of the template was studied by incorporating various substitutions on the nitrogen of the amide linker and examining their HIF-1α inhibition. Among them, compound 57 showed potent HIF-1α inhibition and cytotoxicity in triple-negative breast cancer lines in a dose-dependent manner. Compound 57 downregulated expression and phosphorylation of major client proteins of HSP90 including AKT, ERK and STAT3, indicating that its antitumor activity was derived from the inhibition of HSP90 function. The molecular modeling of 57 demonstrated that 57 bound well to the C-terminal ATP-binding pocket in the open conformation of the hHSP90 homodimer with hydrogen bonding and pi-cation interactions. Overall, compound 57 is a potential antitumor agent for triple-negative breast cancer as a HSP90 C-terminal inhibitor.
CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR ANTICANCER THERAPIES
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, (2014/06/24)
Conjugates or pharmaceutical compositions comprising conjugates of the B-subunit of Shiga toxin that are useful for cancer therapies are disclosed. More specifically, the pharmaceutical compositions comprise STxB conjugated to at least one antimitotic age
SHIGA TOXIN B-SUBUNIT/CHEMOTHERAPEUTICS CONJUGATES
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, (2011/07/06)
The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.