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Molecular and Cellular Biology, December 1999, p. 8226-8239, Vol. 19, No. 12
0270-7306/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Dissection of the LXXLL Nuclear Receptor-Coactivator Interaction Motif Using Combinatorial Peptide Libraries: Discovery of Peptide Antagonists of Estrogen Receptors alpha  and beta

Ching-yi Chang,1 John D. Norris,1 Hanne Grøn,2 Lisa A. Paige,2 Paul T. Hamilton,2 Daniel J. Kenan,3 Dana Fowlkes,2 and Donald P. McDonnell1,*

Department of Pharmacology and Cancer Biology1 and Combinatorial Science Center,3 Duke University Medical Center, Durham, North Carolina 27710, and Novalon Pharmaceutical Corp., Durham, North Carolina 277032

Received 26 April 1999/Returned for modification 25 June 1999/Accepted 18 August 1999

Recruitment of transcriptional coactivators following ligand activation is a critical step in nuclear receptor-mediated target gene expression. Upon binding an agonist, the receptor undergoes a conformational change which facilitates the formation of a specific coactivator binding pocket within the carboxyl terminus of the receptor. This permits the alpha -helical LXXLL motif within some coactivators to interact with the nuclear receptors. Until recently, the LXXLL motif was thought to function solely as a docking module; however, it now appears that sequences flanking the core motif may play a role in determining receptor selectivity. To address this issue, we used a combinatorial phage display approach to evaluate the role of flanking sequences in influencing these interactions. We sampled more than 108 variations of the core LXXLL motif with estradiol-activated estrogen receptor alpha (ERalpha ) as a target and found three different classes of peptides. All of these peptides interacted with ERalpha in an agonist-dependent manner and disrupted ERalpha -mediated transcriptional activity when introduced into target cells. Using a series of ERalpha -mutants, we found that these three classes of peptides showed different interaction patterns from each other, suggesting that not all LXXLL motifs are the same and that receptor binding selectivity can be achieved by altering sequences flanking the LXXLL core motif. Most notable in this regard was the discovery of a peptide which, when overexpressed in cells, selectively disrupted ERbeta - but not ERalpha -mediated reporter gene expression. This novel ERbeta -specific antagonist may be useful in identifying and characterizing the ERbeta -regulated process in estradiol-responsive cells. In conclusion, using a combinatorial approach to define cofactor-receptor interactions, we have clearly been able to demonstrate that not all LXXLL motifs are functionally equivalent, a finding which suggests that it may be possible to target receptor-LXXLL interactions to develop receptor-specific antagonists.

* Corresponding author. Mailing address: Department of Pharmacology and Cancer Biology, Duke University Medical Center, P.O. Box 3813, Durham, NC 27710. Phone: (919) 684-6035. Fax: (919) 681-7139. E-mail: mcdon016{at}acpub.duke.edu.

Molecular and Cellular Biology, December 1999, p. 8226-8239, Vol. 19, No. 12
0270-7306/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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