mTOR revisited

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Figure taken from Ref. 1.

The PI3K/Akt/mTOR pathway is an intracellular signaling pathway important in regulating the cell cycle. It is directly related to cellular quiescence, proliferation, cancer, and longevity. This pathway can be regulated by genes involved in response to hypoxia. Discoveries that have been made over the last decade show that the mTOR pathway is activated during various cellular processes (e.g. tumour formation and angiogenesis, insulin resistance, adipogenesis and T-lymphocyte activation) and is deregulated in human diseases such as cancer and type 2 diabetes (1). [Read more…]

Microtubule destabilization by suprafenacine: Template for novel anti-cancer drugs

Recently, B.-H. Choi et al. characterized a novel anti-mitotic molecule termed suprafenacine which destabilizes microtubules, resulting in cell cycle arrest in the G2/M phase and apoptotic cell death.  In silico screening identified several novel anti-cancer molecules based on their ability to inhibit in vitro cell proliferation and tubulin Tubulin cartoonpolymerization.  Structure Activity Relationship studies guided the synthesis of several analogues.  Of these analogues, suprafenacine was the most potent based on its in vitro ability to 1. specifically target cancer cells from multiple tumor types and 2. inhibit tubulin polymerization (IC50 = 0.38 mM).  [Read more…]