Alkynol natural products target ALDH2 in cancer cells by irreversible binding to the active site.

@article{Heydenreuter2015AlkynolNP,
  title={Alkynol natural products target ALDH2 in cancer cells by irreversible binding to the active site.},
  author={Wolfgang Heydenreuter and Elena Kunold and Stephan A Sieber},
  journal={Chemical communications},
  year={2015},
  volume={51 87},
  pages={
          15784-7
        }
}
Falcarinol and stipudiol are natural products with potent anti-cancer activity found in several vegetables. Here, we use a chemical proteomic strategy to identify ALDH2 as a molecular target of falcarinol in cancer cells and confirm enzyme inhibition via covalent alkylation of the active site. Furthermore, the synthesis of stipudiol led to the observation that ALDH2 exhibits preference for alkynol-based binders. Inhibition of ALDH2 impairs detoxification of reactive aldehydes and limits… CONTINUE READING

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References

Publications referenced by this paper.
Showing 1-10 of 13 references

and M

S. Nickel, R. A. Serwa, +3 authors E. W. Tat
Kaiser, Chemistry, • 2015

F

M. M. Czyzewska, L. Chrobok, A. Kania, M. Jatczak
d he Pollastro, G. Appendino and J. W. Mozrzymas, J Nat Prod, is bl • 2014

and A

K. W. Tan, D. P. Killeen, Y. Li, J. W. Paxton, N. P. Birc
Scheepens, Eur J Pharmacol, • 2014

and E

W. P. Heal, T. H. Dan
W. Tate, Chem Soc Rev, • 2011

and J

M. Leonti, L. Casu, +3 authors K. H. Se Altman
Gertsch, Biochem Pharmacol, • 2010

and M

M. Fonovi
Bogyo, Expert Rev Proteomics, • 2008

and C

J. F. Young, S. J. Duthie, L. Milne, L. P. Christensen, G. G. Duthi
S. Bestwick, J Agric Food Chem, • 2007

and B

M. J. Evan
F. Cravatt, Chem Rev, • 2006
View 1 Excerpt

and K

L. P. Christense
Brandt, J Pharm Biomed Anal, 15 20 • 2006

and H

C. Zidorn, K. Johrer, +5 authors E. P. Ellmere
Stuppner, J Agric Food Chem, • 2005