Tubulin-interactive stilbene derivatives as anticancer agents

We present the results of molecular modeling of their binding to specific sites on the α- and β-tubulin heterodimer

Renata Mikstacka; Tomasz Stefański; Jakub Różański


Scholarcy highlights

  • The high incidence of cancer and the high cost of its treatment are important factors driving the search for new and effective chemotherapeutic substances with multi-target activity and no toxicity to normal cells
  • This review focuses on the anti-carcinogenic properties of natural and modified stilbenes with respect to their interaction with the cellular protein tubulin
  • The combination of the trans-isomer with combretastatin A-4 increased the anti-tumor efficacy of the latter agent to near that of cis-combretastatin A-1 diphosphate. These findings indicate that while the predominant in vivo effect of CA-1P is due to microtubule disruption and vascular shutdown, the formation of oxiquinones – toxic free radicals – could yield additional cytotoxic effects in vivo
  • The analysis indicated that the paclitaxel-binding site of yew tree tubulin contains several amino acid substitutions compared to human tubulin, all of which reduce the binding affinity of paclitaxel to yew tree tubulin
  • Tubulin is the focus of large-scale studies as a crucial target for anticancer drugs
  • Taking into account the synergistic effect, the use of combretastatins in complex therapy is proposed in clinical trials
  • Studies of the interaction between a drug and tubulin with the use of virtual docking and modeling create new perspectives for the design of synthetic analogs with improved properties and effectiveness in comparison to the parent compound

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