PMID- 17997524
OWN - NLM
STAT- MEDLINE
DCOM- 20080221
LR  - 20211020
IS  - 0003-2700 (Print)
IS  - 1520-6882 (Electronic)
IS  - 0003-2700 (Linking)
VI  - 79
IP  - 24
DP  - 2007 Dec 15
TI  - Screening for ligands of human retinoid X receptor-alpha using ultrafiltration 
      mass spectrometry.
PG  - 9398-402
AB  - Retinoid X receptors (RXRs) function as ligand-activated transcription factors 
      and are obligatory components of a large number of nuclear receptor heterodimers. 
      RXRs help regulate diverse physiological responses including the cancer 
      prevention responses of cell proliferation, inflammation, cell differentiation, 
      and apoptosis. Since RXRs represent important targets for cancer chemoprevention, 
      an ultrafiltration mass spectrometry-based assay was developed to facilitate the 
      discovery of potential chemoprevention agents that bind to human RXRalpha. 
      Natural and synthetic ligands for RXRalpha including 9-cis-retinoic acid, 
      docosahexaenoic acid, and LG100268 could be detected and identified in DMSO 
      (dimethyl sulfoxide) or even complex matrixes such as extracts of marine 
      bacteria. Specific binding of ligands to RXRalpha was demonstrated through 
      competitive binding using ultrafiltration LC-MS/MS (liquid chromatography-tandem 
      mass spectrometry), and ligands could be ranked in order of affinity for 
      RXRalpha. Therefore, ultrafiltration LC-MS/MS is suitable for the screening of 
      complex mixtures such as natural product extracts for the discovery of new 
      ligands to RXRalpha.
FAU - Liu, Dongting
AU  - Liu D
AD  - Department of Medicinal Chemistry and Pharmacognosy, University of Illinois 
      College of Pharmacy, 833 South Wood Street, Chicago, Illinois 60612, USA.
FAU - Guo, Jian
AU  - Guo J
FAU - Luo, Yan
AU  - Luo Y
FAU - Broderick, David J
AU  - Broderick DJ
FAU - Schimerlik, Michael I
AU  - Schimerlik MI
FAU - Pezzuto, John M
AU  - Pezzuto JM
FAU - van Breemen, Richard B
AU  - van Breemen RB
LA  - eng
GR  - P01 CA048112/CA/NCI NIH HHS/United States
GR  - P01 CA048112-150010/CA/NCI NIH HHS/United States
GR  - P01 CA048112-160010/CA/NCI NIH HHS/United States
GR  - 5 P01 CA48112/CA/NCI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
DEP - 20071113
PL  - United States
TA  - Anal Chem
JT  - Analytical chemistry
JID - 0370536
RN  - 0 (Ligands)
RN  - 0 (Retinoid X Receptors)
SB  - IM
MH  - Chemoprevention
MH  - Chromatography, Liquid
MH  - Drug Evaluation, Preclinical/*methods
MH  - Humans
MH  - Ligands
MH  - Mass Spectrometry/*methods
MH  - Retinoid X Receptors/*chemistry/metabolism
MH  - Ultrafiltration
PMC - PMC2570161
MID - NIHMS62904
EDAT- 2007/11/14 09:00
MHDA- 2008/02/22 09:00
PMCR- 2008/12/15
CRDT- 2007/11/14 09:00
PHST- 2007/11/14 09:00 [pubmed]
PHST- 2008/02/22 09:00 [medline]
PHST- 2007/11/14 09:00 [entrez]
PHST- 2008/12/15 00:00 [pmc-release]
AID - 10.1021/ac701701k [doi]
PST - ppublish
SO  - Anal Chem. 2007 Dec 15;79(24):9398-402. doi: 10.1021/ac701701k. Epub 2007 Nov 13.