PMID- 24530888
OWN - NLM
STAT- MEDLINE
DCOM- 20141124
LR  - 20140331
IS  - 1873-488X (Electronic)
IS  - 1056-8719 (Linking)
VI  - 69
IP  - 3
DP  - 2014 May-Jun
TI  - Development of yeast reporter assay for screening specific ligands of retinoic 
      acid and retinoid X receptor subtypes.
PG  - 245-52
LID - S1056-8719(14)00016-1 [pii]
LID - 10.1016/j.vascn.2014.01.007 [doi]
AB  - INTRODUCTION: Retinoic acids are essential for embryonic development, tissue 
      organization, and homeostasis and act via retinoic acid receptors (RARs) that 
      form heterodimers with retinoid X receptors (RXRs). Human RARs and RXRs include 
      the three subtypes alpha, beta, and gamma, which have varying distributions and 
      physiological functions among human tissues. Recent reports show that 
      subtype-specific binding of several chemicals to RARs or RXRs may lead to 
      endocrine disruption. To evaluate these ligand-like chemicals, convenient assay 
      systems for each receptor subtype are required. METHODS: We developed reporter 
      assay yeasts to screen ligands for RXR subtype receptor homodimers. To screen RAR 
      ligands, yeasts were engineered to express RAR subtypes with defective RXRalpha, 
      which fails to bind to coactivators because of its shortened c-terminus. RESULTS: 
      These assay yeasts were validated using known RXR- and RAR-specific ligands and 
      subtype-specific responses were clearly shown. Subtype-specific ligand activities 
      of the suspected chemical RAR or RXR ligands o-t-butylphenol, triphenyltin 
      chloride, tributyltin chloride, and 4-nonylphenol were determined. DISCUSSION: 
      The present assay yeasts may be valuable tools for subtype-specific assessments 
      of unidentified environmental ligand chemicals and receptor-specific 
      pharmaceuticals.
CI  - Copyright (c) 2014 Elsevier Inc. All rights reserved.
FAU - Shiizaki, Kazuhiro
AU  - Shiizaki K
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Yoshikawa, Tomoya
AU  - Yoshikawa T
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Takada, Eiji
AU  - Takada E
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Hirose, Shizuma
AU  - Hirose S
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Ito-Harashima, Sayoko
AU  - Ito-Harashima S
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Kawanishi, Masanobu
AU  - Kawanishi M
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan.
FAU - Yagi, Takashi
AU  - Yagi T
AD  - Department of Biology, Graduate School of Science, Osaka Prefecture University, 
      Osaka, Japan; Department of Life Science, Dongguk University, Seoul, Republic of 
      Korea. Electronic address: yagi-t@riast.osakafu-u.ac.jp.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20140212
PL  - United States
TA  - J Pharmacol Toxicol Methods
JT  - Journal of pharmacological and toxicological methods
JID - 9206091
RN  - 0 (Ligands)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Retinoid X Receptors)
RN  - 5688UTC01R (Tretinoin)
SB  - IM
MH  - Genes, Reporter/genetics
MH  - Humans
MH  - Ligands
MH  - Receptors, Retinoic Acid/*metabolism
MH  - Retinoid X Receptors/*metabolism
MH  - Saccharomyces cerevisiae/*genetics
MH  - Tretinoin/*metabolism
OTO - NOTNLM
OT  - Endocrine disruptors
OT  - Reporter assay
OT  - Retinoic acid receptor alpha, beta, gamma
OT  - Retinoid X receptor alpha, beta, gamma
OT  - Saccharomyces cerevisiae
EDAT- 2014/02/18 06:00
MHDA- 2014/12/15 06:00
CRDT- 2014/02/18 06:00
PHST- 2014/01/06 00:00 [received]
PHST- 2014/01/28 00:00 [accepted]
PHST- 2014/02/18 06:00 [entrez]
PHST- 2014/02/18 06:00 [pubmed]
PHST- 2014/12/15 06:00 [medline]
AID - S1056-8719(14)00016-1 [pii]
AID - 10.1016/j.vascn.2014.01.007 [doi]
PST - ppublish
SO  - J Pharmacol Toxicol Methods. 2014 May-Jun;69(3):245-52. doi: 
      10.1016/j.vascn.2014.01.007. Epub 2014 Feb 12.