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The Biophysical Basis for Phosphorylation-Enhanced DNA-Binding Autoinhibition of the ETS1 Transcription Factor.

Perez-Borrajero C, Lin CS, Okon M, Scheu K, Graves BJ, Murphy MEP, McIntosh LP.

J Mol Biol. 2019 Feb 1;431(3):593-614. doi: 10.1016/j.jmb.2018.12.011. Epub 2018 Dec 28.


Electrostatic repulsion causes anticooperative DNA binding between tumor suppressor ETS transcription factors and JUN-FOS at composite DNA sites.

Madison BJ, Clark KA, Bhachech N, Hollenhorst PC, Graves BJ, Currie SL.

J Biol Chem. 2018 Nov 30;293(48):18624-18635. doi: 10.1074/jbc.RA118.003352. Epub 2018 Oct 12.


Development of High-Throughput Screening Assays for Inhibitors of ETS Transcription Factors.

Currie SL, Warner SL, Vankayalapati H, Liu X, Sharma S, Bearss DJ, Graves BJ.

SLAS Discov. 2019 Jan;24(1):77-85. doi: 10.1177/2472555218798571. Epub 2018 Sep 11.


ETV4 and AP1 Transcription Factors Form Multivalent Interactions with three Sites on the MED25 Activator-Interacting Domain.

Currie SL, Doane JJ, Evans KS, Bhachech N, Madison BJ, Lau DKW, McIntosh LP, Skalicky JJ, Clark KA, Graves BJ.

J Mol Biol. 2017 Oct 13;429(20):2975-2995. doi: 10.1016/j.jmb.2017.06.024. Epub 2017 Jul 17.


Structured and disordered regions cooperatively mediate DNA-binding autoinhibition of ETS factors ETV1, ETV4 and ETV5.

Currie SL, Lau DKW, Doane JJ, Whitby FG, Okon M, McIntosh LP, Graves BJ.

Nucleic Acids Res. 2017 Mar 17;45(5):2223-2241. doi: 10.1093/nar/gkx068.


Conformational Dynamics and the Binding of Specific and Nonspecific DNA by the Autoinhibited Transcription Factor Ets-1.

Desjardins G, Okon M, Graves BJ, McIntosh LP.

Biochemistry. 2016 Jul 26;55(29):4105-18. doi: 10.1021/acs.biochem.6b00460. Epub 2016 Jul 15.


Autoinhibition of ETV6 DNA Binding Is Established by the Stability of Its Inhibitory Helix.

De S, Okon M, Graves BJ, McIntosh LP.

J Mol Biol. 2016 Apr 24;428(8):1515-30. doi: 10.1016/j.jmb.2016.02.020. Epub 2016 Feb 23.


Interaction of the Jhd2 Histone H3 Lys-4 Demethylase with Chromatin Is Controlled by Histone H2A Surfaces and Restricted by H2B Ubiquitination.

Huang F, Ramakrishnan S, Pokhrel S, Pflueger C, Parnell TJ, Kasten MM, Currie SL, Bhachech N, Horikoshi M, Graves BJ, Cairns BR, Bhaskara S, Chandrasekharan MB.

J Biol Chem. 2015 Nov 27;290(48):28760-77. doi: 10.1074/jbc.M115.693085. Epub 2015 Oct 8.


Synergy of aromatic residues and phosphoserines within the intrinsically disordered DNA-binding inhibitory elements of the Ets-1 transcription factor.

Desjardins G, Meeker CA, Bhachech N, Currie SL, Okon M, Graves BJ, McIntosh LP.

Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):11019-24. doi: 10.1073/pnas.1401891111. Epub 2014 Jul 14.


Dual views of SRF: a genomic exposure.

Clark KA, Graves BJ.

Genes Dev. 2014 May 1;28(9):926-8. doi: 10.1101/gad.242420.114.


Steric mechanism of auto-inhibitory regulation of specific and non-specific DNA binding by the ETS transcriptional repressor ETV6.

De S, Chan AC, Coyne HJ 3rd, Bhachech N, Hermsdorf U, Okon M, Murphy ME, Graves BJ, McIntosh LP.

J Mol Biol. 2014 Apr 3;426(7):1390-406. doi: 10.1016/j.jmb.2013.11.031. Epub 2013 Dec 12.


Gene deregulation and chronic activation in natural killer cells deficient in the transcription factor ETS1.

Ramirez K, Chandler KJ, Spaulding C, Zandi S, Sigvardsson M, Graves BJ, Kee BL.

Immunity. 2012 Jun 29;36(6):921-32. doi: 10.1016/j.immuni.2012.04.006. Epub 2012 May 17.


Autoinhibition of ETV6 (TEL) DNA binding: appended helices sterically block the ETS domain.

Coyne HJ 3rd, De S, Okon M, Green SM, Bhachech N, Graves BJ, McIntosh LP.

J Mol Biol. 2012 Aug 3;421(1):67-84. doi: 10.1016/j.jmb.2012.05.010. Epub 2012 May 12.


Oncogenic ETS proteins mimic activated RAS/MAPK signaling in prostate cells.

Hollenhorst PC, Ferris MW, Hull MA, Chae H, Kim S, Graves BJ.

Genes Dev. 2011 Oct 15;25(20):2147-57. doi: 10.1101/gad.17546311.


Genomic and biochemical insights into the specificity of ETS transcription factors.

Hollenhorst PC, McIntosh LP, Graves BJ.

Annu Rev Biochem. 2011;80:437-71. doi: 10.1146/annurev.biochem.79.081507.103945. Review.


Synthesis and Processing of Viral RNA.

Rabson AB, Graves BJ.

In: Coffin JM, Hughes SH, Varmus HE, editors. Retroviruses. Cold Spring Harbor (NY): Cold Spring Harbor Laboratory Press; 1997.


ETS-4 is a transcriptional regulator of life span in Caenorhabditis elegans.

Thyagarajan B, Blaszczak AG, Chandler KJ, Watts JL, Johnson WE, Graves BJ.

PLoS Genet. 2010 Sep 16;6(9):e1001125. doi: 10.1371/journal.pgen.1001125.


Ras signaling requires dynamic properties of Ets1 for phosphorylation-enhanced binding to coactivator CBP.

Nelson ML, Kang HS, Lee GM, Blaszczak AG, Lau DK, McIntosh LP, Graves BJ.

Proc Natl Acad Sci U S A. 2010 Jun 1;107(22):10026-31. doi: 10.1073/pnas.0915137107. Epub 2010 May 13.


Human RNA polymerase III transcriptomes and relationships to Pol II promoter chromatin and enhancer-binding factors.

Oler AJ, Alla RK, Roberts DN, Wong A, Hollenhorst PC, Chandler KJ, Cassiday PA, Nelson CA, Hagedorn CH, Graves BJ, Cairns BR.

Nat Struct Mol Biol. 2010 May;17(5):620-8. doi: 10.1038/nsmb.1801. Epub 2010 Apr 25.


DNA binding by the ETS protein TEL (ETV6) is regulated by autoinhibition and self-association.

Green SM, Coyne HJ 3rd, McIntosh LP, Graves BJ.

J Biol Chem. 2010 Jun 11;285(24):18496-504. doi: 10.1074/jbc.M109.096958. Epub 2010 Apr 16.


DNA specificity determinants associate with distinct transcription factor functions.

Hollenhorst PC, Chandler KJ, Poulsen RL, Johnson WE, Speck NA, Graves BJ.

PLoS Genet. 2009 Dec;5(12):e1000778. doi: 10.1371/journal.pgen.1000778. Epub 2009 Dec 18.


The GNUMAP algorithm: unbiased probabilistic mapping of oligonucleotides from next-generation sequencing.

Clement NL, Snell Q, Clement MJ, Hollenhorst PC, Purwar J, Graves BJ, Cairns BR, Johnson WE.

Bioinformatics. 2010 Jan 1;26(1):38-45. doi: 10.1093/bioinformatics/btp614. Epub 2009 Oct 27.


Detection and assignment of phosphoserine and phosphothreonine residues by (13)C- (31)P spin-echo difference NMR spectroscopy.

McIntosh LP, Kang HS, Okon M, Nelson ML, Graves BJ, Brutscher B.

J Biomol NMR. 2009 Jan;43(1):31-7. doi: 10.1007/s10858-008-9287-6. Epub 2008 Nov 12.


The affinity of Ets-1 for DNA is modulated by phosphorylation through transient interactions of an unstructured region.

Lee GM, Pufall MA, Meeker CA, Kang HS, Graves BJ, McIntosh LP.

J Mol Biol. 2008 Oct 17;382(4):1014-30. doi: 10.1016/j.jmb.2008.07.064. Epub 2008 Jul 29.


Microsatellites as EWS/FLI response elements in Ewing's sarcoma.

Gangwal K, Sankar S, Hollenhorst PC, Kinsey M, Haroldsen SC, Shah AA, Boucher KM, Watkins WS, Jorde LB, Graves BJ, Lessnick SL.

Proc Natl Acad Sci U S A. 2008 Jul 22;105(29):10149-54. doi: 10.1073/pnas.0801073105. Epub 2008 Jul 14.


Role of Ets-1 phosphorylation in the effector function of Th cells.

Grenningloh R, Miaw SC, Moisan J, Graves BJ, Ho IC.

Eur J Immunol. 2008 Jun;38(6):1700-5. doi: 10.1002/eji.200738112.


Identification and structural characterization of a CBP/p300-binding domain from the ETS family transcription factor GABP alpha.

Kang HS, Nelson ML, Mackereth CD, Schärpf M, Graves BJ, McIntosh LP.

J Mol Biol. 2008 Mar 28;377(3):636-46. doi: 10.1016/j.jmb.2008.01.054. Epub 2008 Jan 30.


Genome-wide analyses reveal properties of redundant and specific promoter occupancy within the ETS gene family.

Hollenhorst PC, Shah AA, Hopkins C, Graves BJ.

Genes Dev. 2007 Aug 1;21(15):1882-94. Epub 2007 Jul 24.


Transcription saga tells developmental stories.

Graves BJ, Tamkun JW.

Development. 2006 Nov;133(22):4393-7. Review. No abstract available.


Beads-on-a-string, characterization of ETS-1 sumoylated within its flexible N-terminal sequence.

Macauley MS, Errington WJ, Schärpf M, Mackereth CD, Blaszczak AG, Graves BJ, McIntosh LP.

J Biol Chem. 2006 Feb 17;281(7):4164-72. Epub 2005 Nov 29.


Variable control of Ets-1 DNA binding by multiple phosphates in an unstructured region.

Pufall MA, Lee GM, Nelson ML, Kang HS, Velyvis A, Kay LE, McIntosh LP, Graves BJ.

Science. 2005 Jul 1;309(5731):142-5.


The structural and dynamic basis of Ets-1 DNA binding autoinhibition.

Lee GM, Donaldson LW, Pufall MA, Kang HS, Pot I, Graves BJ, McIntosh LP.

J Biol Chem. 2005 Feb 25;280(8):7088-99. Epub 2004 Dec 9.


Ras/mitogen-activated protein kinase signaling activates Ets-1 and Ets-2 by CBP/p300 recruitment.

Foulds CE, Nelson ML, Blaszczak AG, Graves BJ.

Mol Cell Biol. 2004 Dec;24(24):10954-64.


Expression profiles frame the promoter specificity dilemma of the ETS family of transcription factors.

Hollenhorst PC, Jones DA, Graves BJ.

Nucleic Acids Res. 2004 Oct 21;32(18):5693-702. Print 2004.


Structural analysis of the autoinhibition of Ets-1 and its role in protein partnerships.

Garvie CW, Pufall MA, Graves BJ, Wolberger C.

J Biol Chem. 2002 Nov 22;277(47):45529-36. Epub 2002 Sep 6.


Autoinhibitory domains: modular effectors of cellular regulation.

Pufall MA, Graves BJ.

Annu Rev Cell Dev Biol. 2002;18:421-62. Epub 2002 Apr 2. Review.


Ets-1 flips for new partner Pax-5.

Pufall MA, Graves BJ.

Structure. 2002 Jan;10(1):11-4. Review.


Inhibitory module of Ets-1 allosterically regulates DNA binding through a dipole-facilitated phosphate contact.

Wang H, McIntosh LP, Graves BJ.

J Biol Chem. 2002 Jan 18;277(3):2225-33. Epub 2001 Oct 31.


Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.

Lew W, Wu H, Chen X, Graves BJ, Escarpe PA, MacArthur HL, Mendel DB, Kim CU.

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1257-60.


Phosphorylation represses Ets-1 DNA binding by reinforcing autoinhibition.

Cowley DO, Graves BJ.

Genes Dev. 2000 Feb 1;14(3):366-76.


Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.

Zhang L, Williams MA, Mendel DB, Escarpe PA, Chen X, Wang KY, Graves BJ, Lawton G, Kim CU.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1751-6.


Autoinhibition as a transcriptional regulatory mechanism.

Graves BJ, Cowley DO, Goetz TL, Petersen JM, Jonsen MD, Gillespie ME.

Cold Spring Harb Symp Quant Biol. 1998;63:621-9. Review. No abstract available.


Inhibition of Ets-1 DNA binding and ternary complex formation between Ets-1, NF-kappaB, and DNA by a designed DNA-binding ligand.

Dickinson LA, Trauger JW, Baird EE, Dervan PB, Graves BJ, Gottesfeld JM.

J Biol Chem. 1999 Apr 30;274(18):12765-73.


Equilibrium analysis of high affinity interactions using BIACORE.

Myszka DG, Jonsen MD, Graves BJ.

Anal Biochem. 1998 Dec 15;265(2):326-30.


A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity.

Lew W, Wu H, Mendel DB, Escarpe PA, Chen X, Laver WG, Graves BJ, Kim CU.

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3321-4.


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