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Multivalent peptidomimetic conjugates: a versatile platform for modulating androgen receptor activity.

We introduce a family of multivalent peptidomimetic conjugates that modulate the activity of the androgen receptor (AR). Bioactive ethisterone ligands were conjugated to a set of sequence-specific peptoid oligomers. Certain multivalent peptoid conjugates enhance AR-mediated transcriptional activatio... Full description

Journal Title: Journal of the American Chemical Society April 25, 2012, Vol.134(16), pp.6912-6915
Main Author: Levine, Paul M
Other Authors: Imberg, Keren , Garabedian, Michael J , Kirshenbaum, Kent
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: E-ISSN: 1520-5126 ; DOI: 1520-5126 ; DOI: 10.1021/ja300170n
Link: http://search.proquest.com/docview/1020833482/?pq-origsite=primo
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recordid: proquest1020833482
title: Multivalent peptidomimetic conjugates: a versatile platform for modulating androgen receptor activity.
format: Article
creator:
  • Levine, Paul M
  • Imberg, Keren
  • Garabedian, Michael J
  • Kirshenbaum, Kent
subjects:
  • Antineoplastic Agents–Chemical Synthesis
  • Cell Line, Tumor–Chemistry
  • Cell Proliferation–Pharmacology
  • Drug Screening Assays, Antitumor–Drug Effects
  • Hek293 Cells–Chemical Synthesis
  • Humans–Chemistry
  • Ligands–Pharmacology
  • Male–Drug Therapy
  • Models, Molecular–Pathology
  • Molecular Structure–Chemistry
  • Peptides–Metabolism
  • Prostatic Neoplasms–Metabolism
  • Receptors, Androgen–Metabolism
  • Structure-Activity Relationship–Metabolism
  • Antineoplastic Agents
  • Ligands
  • Peptides
  • Receptors, Androgen
ispartof: Journal of the American Chemical Society, April 25, 2012, Vol.134(16), pp.6912-6915
description: We introduce a family of multivalent peptidomimetic conjugates that modulate the activity of the androgen receptor (AR). Bioactive ethisterone ligands were conjugated to a set of sequence-specific peptoid oligomers. Certain multivalent peptoid conjugates enhance AR-mediated transcriptional activation. We identify a linear and a cyclic conjugate that exhibit potent anti-proliferative activity in LNCaP-abl cells, a model of therapy-resistant prostate cancer. The linear conjugate blocks AR action by competing for ligand binding. In contrast, the cyclic conjugate is active despite its inability to compete against endogenous ligand for binding to AR in vitro, suggesting a non-competitive mode of action. These results establish a versatile platform to design competitive and non-competitive AR modulators with potential therapeutic significance.
language: eng
source:
identifier: E-ISSN: 1520-5126 ; DOI: 1520-5126 ; DOI: 10.1021/ja300170n
fulltext: fulltext
issn:
  • 15205126
  • 1520-5126
url: Link


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titleMultivalent peptidomimetic conjugates: a versatile platform for modulating androgen receptor activity.
creatorLevine, Paul M ; Imberg, Keren ; Garabedian, Michael J ; Kirshenbaum, Kent
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subjectAntineoplastic Agents–Chemical Synthesis ; Cell Line, Tumor–Chemistry ; Cell Proliferation–Pharmacology ; Drug Screening Assays, Antitumor–Drug Effects ; Hek293 Cells–Chemical Synthesis ; Humans–Chemistry ; Ligands–Pharmacology ; Male–Drug Therapy ; Models, Molecular–Pathology ; Molecular Structure–Chemistry ; Peptides–Metabolism ; Prostatic Neoplasms–Metabolism ; Receptors, Androgen–Metabolism ; Structure-Activity Relationship–Metabolism ; Antineoplastic Agents ; Ligands ; Peptides ; Receptors, Androgen
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descriptionWe introduce a family of multivalent peptidomimetic conjugates that modulate the activity of the androgen receptor (AR). Bioactive ethisterone ligands were conjugated to a set of sequence-specific peptoid oligomers. Certain multivalent peptoid conjugates enhance AR-mediated transcriptional activation. We identify a linear and a cyclic conjugate that exhibit potent anti-proliferative activity in LNCaP-abl cells, a model of therapy-resistant prostate cancer. The linear conjugate blocks AR action by competing for ligand binding. In contrast, the cyclic conjugate is active despite its inability to compete against endogenous ligand for binding to AR in vitro, suggesting a non-competitive mode of action. These results establish a versatile platform to design competitive and non-competitive AR modulators with potential therapeutic significance.
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