A Spiroligomer α-Helix Mimic That Binds HDM2, Penetrates Human Cells and Stabilizes HDM2 in Cell Culture

@inproceedings{Brown2012AS,
  title={A Spiroligomer α-Helix Mimic That Binds HDM2, Penetrates Human Cells and Stabilizes HDM2 in Cell Culture},
  author={Zachary Z. Brown and Kavitha Akula and Alla Arzumanyan and Jennifer L Alleva and Marcus A Jackson and Eugeney Bichenkov and Joel B. Sheffield and Mark Alan Feitelson and Christian E Schafmeister},
  booktitle={PloS one},
  year={2012}
}
We demonstrate functionalized spiroligomers that mimic the HDM2-bound conformation of the p53 activation domain. Spiroligomers are stereochemically defined, functionalized, spirocyclic monomers coupled through pairs of amide bonds to create spiro-ladder oligomers. Two series of spiroligomers were synthesized, one of structural analogs and one of stereochemical analogs, from which we identified compound 1, that binds HDM2 with a Kd value of 400 nM. The spiroligomer 1 penetrates human liver… CONTINUE READING

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Referenced Papers

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Showing 1-8 of 8 references

Biopolymers

  • Z Z Brown, J Alleva, C E Schafmeister
  • Biopolymers
  • 2011

Cell Cycle

  • A Czarna, G Popowicz, A Pecak, S Wolf, G Dubin, T Holak
  • Cell Cycle
  • 2009

Acc. Chem. Res

  • C E Schafmeister, Z Z Brown, S Gupta
  • Acc. Chem. Res
  • 2008

Nucl Acids Res

  • Mw Pfaffl
  • Nucl Acids Res
  • 2001

Int J Biochem Cell Biol

  • F Toledo, G M Wahl
  • Int J Biochem Cell Biol
  • 1476

Biochemistry

  • S Zondlo, A Lee, Zondlo
  • Biochemistry
  • 1194

Information References

  • Information References

Org. Lett

  • Z Z Brown, C E Schafmeister
  • Org. Lett

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