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PubMed · 14583004

Toward artificial developmental regulators.

Hans-Dieter Arndt·Karl E Hauschild·David P Sullivan·Kara Lake·Peter B Dervan·Aseem Z Ansari
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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-gamma-Im-Py-Py-Py-beta-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.

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Biomimetic MaterialsDNADrosophila ProteinsHomeodomain ProteinsKineticsModels, MolecularNylonsProtein Structure, TertiaryTranscription FactorsJournal ArticleResearch Support, Non-U.S. Gov'tResearch Support, U.S. Gov't, Non-P.H.S.Research Support, U.S. Gov't, P.H.S.

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Hans-Dieter Arndt, Karl E Hauschild, David P Sullivan, Kara Lake, Peter B Dervan, Aseem Z Ansari. 2003-11-05. Toward artificial developmental regulators.. https://doi.org/10.1021/ja0371395

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