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Toward artificial developmental regulators

Arndt, Hans-Dieter and Hauschild, Karl E. and Sullivan, David P. and Lake, Kara and Dervan, Peter B. and Ansari, Aseem Z. (2003) Toward artificial developmental regulators. Journal of the American Chemical Society, 125 (44). pp. 13322-13323. ISSN 0002-7863.

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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.

Item Type:Article
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URLURL TypeDescription Information
Arndt, Hans-Dieter0000-0002-0792-1422
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2003 American Chemical Society. Received July 8, 2003. Publication Date (Web): October 9, 2003. This work was supported in part by the UW-I & EDR and Steenbock Funds to A.Z.A., a NIH grant to P.B.D., and a DAAD postdoctoral fellowship to H.D.A.
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University of WisconsinUNSPECIFIED
Deutscher Akademischer Austauschdienst (DAAD)UNSPECIFIED
Issue or Number:44
Record Number:CaltechAUTHORS:20160510-080147534
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Official Citation:Toward Artificial Developmental Regulators Hans-Dieter Arndt, Karl E. Hauschild, David P. Sullivan, Kara Lake, Peter B. Dervan, and Aseem Z. Ansari Journal of the American Chemical Society 2003 125 (44), 13322-13323 DOI: 10.1021/ja0371395
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66797
Deposited By: Victoria Brennan
Deposited On:17 May 2016 23:27
Last Modified:26 Nov 2019 11:15

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