Toward artificial developmental regulators
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.
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.Attached Files
Supplemental Material - ja0371395si20030912_025452.pdf
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Additional details
- Eprint ID
- 66797
- Resolver ID
- CaltechAUTHORS:20160510-080147534
- University of Wisconsin
- NIH
- Deutscher Akademischer Austauschdienst (DAAD)
- Created
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2016-05-17Created from EPrint's datestamp field
- Updated
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2021-11-11Created from EPrint's last_modified field