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(Received for publication, July 10, 1996)
From the Departments of Based on the finding that some transcription
factors contain multiple transcriptional regulatory activities, we
constructed a panel of rat androgen receptor (AR) mutants containing
small internal deletions and point mutations within the amino-terminal
region of the receptor. Trans-activation assays in CV-1 cells using
AR-responsive reporter genes were performed and led to the
identification of two noncontiguous trans-activation regions in the AR
amino terminus. One of these regions, termed activator function 1a
(AF-1a) is a highly-conserved 14-amino acid segment that is predicted
to form a
Volume 271, Number 43,
Issue of October 25, 1996
pp. 26772-26778
©1996 by The American Society for Biochemistry and Molecular Biology, Inc.
,¶
Biochemistry and
¶ Molecular and Cellular Biology, University of Arizona,
Tucson, Arizona 85721
-turn followed by an acidic amphipathic 
-helix. Point
mutagenesis within AF-1a revealed that two adjacent hydrophobic
residues were required for full AR trans-activation function, as
arginine substitutions resulted in a 60% reduction in transcriptional
activity. A second amino-terminal region was also identified and has
been designated AF-1b. Deletion of the 65-amino acid AF-1b segment,
which contains numerous glutamate and aspartate residues, caused a 55%
decrease in trans-activation function. An AF-1a/AF-1b double mutant
retains less than 10% trans-activation function compared with
wild-type AR, suggesting that AF-1a and AF-1b may each contribute
separately to maximal AR activity. To determine whether AF-1a and AF-1b
play a role in AR-mediated trans-repression of AP-1 function, we tested
single and double AF-1a/AF-1b mutants in a transient trans-repression
assay. Our results showed that neither AF-1a nor AF-1b was required for
AP-1 trans-repression, demonstrating that AR-mediated trans-repression
and trans-activation are discrete functions.
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