Toward Artificial Developmental Regulators

Hans Dieter Arndt, Karl E. Hauschild, David P. Sullivan, Kara Lake, Peter B. Dervan*, Aseem Z. Ansari

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

44 Scopus citations

Abstract

A polyamide?peptide conjugate is designed which recruits sequence specifically the developmental regulator Exd to a cognate DNA site. In particular, an eight-ring hairpin polyamide (Im-Im-Py(C3H6NHR)-Py-γ-Im-Py-Py-Py-β-Dp) with a heptapeptide (R = Ac-Phe-Tyr-Pro-Trp-Met-Lys-Gly-) attached on a central ring was shown to induce cooperative binding of the Drosophila Hox protein cofactor Exd with a Kd of 4.4 nM in vitro, an order of magnitude more efficient than the natural Hox protein partner Ubx. The conjugate joins two sequence specific domains, one for DNA and one for the protein. This small molecule thus serves as a cooperative protein?DNA dimerizer, which mimics the natural Hox family of developmental regulators.

Original languageEnglish (US)
Pages (from-to)13322-13323
Number of pages2
JournalJournal of the American Chemical Society
Volume125
Issue number44
DOIs
StatePublished - Nov 5 2003

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

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