A set of time-resolved fluorescence resonance energy transfer assays for the discovery of inhibitors of estrogen receptor-coactivator binding

Journal of Biomolecular Screening

Volumn 14, Issue 2, 2009, Pages 181-193

  Gunther, Jillian R ^a   Du, Yuhong ^b   Rhoden, Eric ^b   Lewis, Iestyn ^b   Revennaugh, Brian ^b   Moore, Terry W ^a   Kim, Sung Hoon ^a   Dingledine, Raymond ^b   Fu, Haian ^b   Katzenellenbogen, John A ^a  

^a UNIVERSITY OF ILLINOIS AT URBANA CHAMPAIGN   (United States)

^b EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Coactivator binding inhibitors; Estrogen receptor; High throughput screening; Time resolved fluorescence resonance energy transfer

Indexed keywords

ESTRADIOL; ESTROGEN RECEPTOR; HORMONE INHIBITOR; LIGAND; PROTEIN INHIBITOR; STEROID RECEPTOR COACTIVATOR 3;

ARTICLE; COLORIMETRY; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG POTENCY; ENZYME LINKED IMMUNOSORBENT ASSAY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; IC 50; INHIBITION KINETICS; PRIORITY JOURNAL; PROTEIN BINDING; SIGNAL NOISE RATIO; TITRIMETRY;

CALIBRATION; COMPETITIVE BEHAVIOR; DRUG DISCOVERY; ENZYME-LINKED IMMUNOSORBENT ASSAY; ESTROGEN ANTAGONISTS; FLUORESCENCE RESONANCE ENERGY TRANSFER; HISTONE ACETYLTRANSFERASES; HUMANS; MODELS, BIOLOGICAL; PROTEIN BINDING; RECEPTORS, ESTROGEN; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANS-ACTIVATORS;

EID: 61849123737     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057108329349     Document Type: Article

References (19)

1. Katzenellenbogen BS: Estrogen receptors: bioactivities and interactions with cell signaling pathways. Biol Reprod 1996 ; 54: 287-293.
2. Schiff R., Massarweh SA, Shou J., Bharwani L., Arpino G., Rimawi M., et al. Advanced concepts in estrogen receptor biology and breast cancer endocrine resistance: implicated role of growth factor signaling and estrogen receptor coregulators. Cancer Chemother Pharmacol 2005 ; 56 (suppl 1). 10-20.
3. Tamrazi A., Carlson KE, Rodriguez AL, Katzenellenbogen JA: Coactivator proteins as determinants of estrogen receptor structure and function: spectroscopic evidence for a novel coactivator-stabilized receptor conformation. Mol Endocrinol 2005 ; 19: 1516-1528.
4. van de Wijngaart DJ, van Royen ME, Hersmus R., Pike ACW, Houtsmuller AB, Jenster G., et al. Novel FXXFF and FXXMF motifs in androgen receptor cofactors mediate high affinity and specific interactions with the ligand-binding domain. J Biol Chem 2006 ; 281: 19407-19416.
5. Norris JD, Paige LA, Christensen DJ, Chang C-Y., Huacani MR, Fan D., et al. Peptide antagonists of the human estrogen receptor. Science 1999 ; 285: 744-746.
6. Becerril J., Hamilton AD: Helix mimetics as inhibitors of the interaction of the estrogen receptor with coactivator peptides. Angew Chem Int Ed Engl 2007 ; 46: 4471-4473.
7. Gunther JR, Moore TW, Collins ML, Katzenellenbogen JA: Amphipathic benzenes are designed inhibitors of the estrogen receptor alpha/steroid receptor coactivator interaction. ACS Chem Biol 2008 ; 3: 282-286.
8. Rodriguez AL, Tamrazi A., Collins ML, Katzenellenbogen JA: Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding. J Med Chem 2004 ; 47: 600-611.
9. Zhou HB, Collins ML, Gunther JR, Comninos JS, Katzenellenbogen JA: Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. Bioorg Med Chem Lett 2007 ; 17: 4118-4122.
10. Shao D., Berrodin TJ, Manas E., Hauze D., Powers R., Bapat A., et al. Identification of novel estrogen receptor a antagonists. J Steroid Biochem Mol Biol 2004 ; 88: 351-360.
11. Bramlett KS, Wu Y., Burris TP: Ligands specify coactivator nuclear receptor (NR) box affinity for estrogen receptor subtypes. Mol Endocrinol 2001 ; 15: 909-922.
12. Mueller SO: Xenoestrogens: mechanisms of action and detection methods. Anal Bioanal Chem 2004 ; 378: 582-587.
13. Ozers MS, Ervin KM, Steffen CL, Fronczak JA, Lebakken CS, Carnahan KA, et al. Analysis of ligand-dependent recruitment of coactivator peptides to estrogen receptor using fluorescence polarization. Mol Endocrinol 2005 ; 19: 25-34.
14. Gowda K., Marks BD, Zielinski TK, Ozers MS: Development of a coactivator displacement assay for the orphan receptor estrogen-related receptor-[gamma] using time-resolved fluorescence resonance energy transfer. Anal Biochem 2006 ; 357: 105-115.
15. Liu J., Knappenberger KS, Kack H., Andersson G., Nilsson E., Dartsch C., et al. A homogeneous in vitro functional assay for estrogen receptors: coactivator recruitment. Mol Endocrinol 2003 ; 17: 346-355.
16. Zhou G., Cummings R., Li Y., Mitra S., Wilkinson HA, Elbrecht A., et al. Nuclear receptors have distinct affinities for coactivators: characterization by fluorescence resonance energy transfer. Mol Endocrinol 1998 ; 12: 1594-1604.
17. Tamrazi A., Carlson KE, Daniels JR, Hurth KM, Katzenellenbogen JA: Estrogen receptor dimerization: ligand binding regulates dimer affinity and dimer dissociation rate. Mol Endocrinol 2002 ; 16: 2706-2719.
18. Carlson KE, Choi I., Gee A., Katzenellenbogen BS, Katzenellenbogen JA: Altered ligand binding properties and enhanced stability of a constitutively active estrogen receptor: evidence that an open pocket conformation is required for ligand interaction. Biochemistry 1997 ; 36: 14897-14905.
19. Katzenellenbogen JA, Johnson HJ Jr, Myers HN: Photoaffinity labels for estrogen binding proteins of rat uterus. Biochemistry 1973 ; 12: 4085-4092.