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Items: 1 to 50 of 240

1.

Covalent Modification and Regulation of the Nuclear Receptor Nurr1 by a Dopamine Metabolite.

Bruning JM, Wang Y, Oltrabella F, Tian B, Kholodar SA, Liu H, Bhattacharya P, Guo S, Holton JM, Fletterick RJ, Jacobson MP, England PM.

Cell Chem Biol. 2019 May 16;26(5):674-685.e6. doi: 10.1016/j.chembiol.2019.02.002. Epub 2019 Mar 7.

PMID:
30853418
2.

LRH-1 mitigates intestinal inflammatory disease by maintaining epithelial homeostasis and cell survival.

Bayrer JR, Wang H, Nattiv R, Suzawa M, Escusa HS, Fletterick RJ, Klein OD, Moore DD, Ingraham HA.

Nat Commun. 2018 Oct 10;9(1):4055. doi: 10.1038/s41467-018-06137-w.

3.

Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen.

de Jesus Cortez F, Nguyen P, Truillet C, Tian B, Kuchenbecker KM, Evans MJ, Webb P, Jacobson MP, Fletterick RJ, England PM.

ACS Chem Biol. 2017 Dec 15;12(12):2934-2939. doi: 10.1021/acschembio.7b00702. Epub 2017 Nov 2.

PMID:
28981251
4.

Disulfide-Trapping Identifies a New, Effective Chemical Probe for Activating the Nuclear Receptor Human LRH-1 (NR5A2).

de Jesus Cortez F, Suzawa M, Irvy S, Bruning JM, Sablin E, Jacobson MP, Fletterick RJ, Ingraham HA, England PM.

PLoS One. 2016 Jul 28;11(7):e0159316. doi: 10.1371/journal.pone.0159316. eCollection 2016.

5.

Dlx5 Homeodomain:DNA Complex: Structure, Binding and Effect of Mutations Related to Split Hand and Foot Malformation Syndrome.

Proudfoot A, Axelrod HL, Geralt M, Fletterick RJ, Yumoto F, Deacon AM, Elsliger MA, Wilson IA, Wüthrich K, Serrano P.

J Mol Biol. 2016 Mar 27;428(6):1130-1141. doi: 10.1016/j.jmb.2016.01.023. Epub 2016 Jan 29.

6.

A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver.

Suzawa M, Miranda DA, Ramos KA, Ang KK, Faivre EJ, Wilson CG, Caboni L, Arkin MR, Kim YS, Fletterick RJ, Diaz A, Schneekloth JS, Ingraham HA.

Elife. 2015 Dec 11;4. pii: e09003. doi: 10.7554/eLife.09003.

7.

Structure of Liver Receptor Homolog-1 (NR5A2) with PIP3 hormone bound in the ligand binding pocket.

Sablin EP, Blind RD, Uthayaruban R, Chiu HJ, Deacon AM, Das D, Ingraham HA, Fletterick RJ.

J Struct Biol. 2015 Dec;192(3):342-348. doi: 10.1016/j.jsb.2015.09.012. Epub 2015 Sep 28.

8.

The FKBP52 Cochaperone Acts in Synergy with β-Catenin to Potentiate Androgen Receptor Signaling.

Storer Samaniego C, Suh JH, Chattopadhyay A, Olivares K, Guy N, Sivils JC, Dey P, Yumoto F, Fletterick RJ, Strom AM, Gustafsson JÅ, Webb P, Cox MB.

PLoS One. 2015 Jul 24;10(7):e0134015. doi: 10.1371/journal.pone.0134015. eCollection 2015.

9.

Structure-based discovery of NANOG variant with enhanced properties to promote self-renewal and reprogramming of pluripotent stem cells.

Hayashi Y, Caboni L, Das D, Yumoto F, Clayton T, Deller MC, Nguyen P, Farr CL, Chiu HJ, Miller MD, Elsliger MA, Deacon AM, Godzik A, Lesley SA, Tomoda K, Conklin BR, Wilson IA, Yamanaka S, Fletterick RJ.

Proc Natl Acad Sci U S A. 2015 Apr 14;112(15):4666-71. doi: 10.1073/pnas.1502855112. Epub 2015 Mar 30.

10.

Histone demethylase KDM5A is regulated by its reader domain through a positive-feedback mechanism.

Torres IO, Kuchenbecker KM, Nnadi CI, Fletterick RJ, Kelly MJ, Fujimori DG.

Nat Commun. 2015 Feb 17;6:6204. doi: 10.1038/ncomms7204.

11.

Silencing LRH-1 in colon cancer cell lines impairs proliferation and alters gene expression programs.

Bayrer JR, Mukkamala S, Sablin EP, Webb P, Fletterick RJ.

Proc Natl Acad Sci U S A. 2015 Feb 24;112(8):2467-72. doi: 10.1073/pnas.1500978112. Epub 2015 Feb 9.

12.

Advances in our structural understanding of orphan nuclear receptors.

Gallastegui N, Mackinnon JA, Fletterick RJ, Estébanez-Perpiñá E.

Trends Biochem Sci. 2015 Jan;40(1):25-35. doi: 10.1016/j.tibs.2014.11.002. Epub 2014 Dec 11. Review.

PMID:
25499868
13.

The signaling phospholipid PIP3 creates a new interaction surface on the nuclear receptor SF-1.

Blind RD, Sablin EP, Kuchenbecker KM, Chiu HJ, Deacon AM, Das D, Fletterick RJ, Ingraham HA.

Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15054-9. doi: 10.1073/pnas.1416740111. Epub 2014 Oct 6.

14.

The human orphan nuclear receptor tailless (TLX, NR2E1) is druggable.

Benod C, Villagomez R, Filgueira CS, Hwang PK, Leonard PG, Poncet-Montange G, Rajagopalan S, Fletterick RJ, Gustafsson JÅ, Webb P.

PLoS One. 2014 Jun 17;9(6):e99440. doi: 10.1371/journal.pone.0099440. eCollection 2014.

15.

Structural and functional insight into TAF1-TAF7, a subcomplex of transcription factor II D.

Bhattacharya S, Lou X, Hwang P, Rajashankar KR, Wang X, Gustafsson JÅ, Fletterick RJ, Jacobson RH, Webb P.

Proc Natl Acad Sci U S A. 2014 Jun 24;111(25):9103-8. doi: 10.1073/pnas.1408293111. Epub 2014 Jun 10.

16.

Computer modeling of a newly identified THRB gene mutation (S350L) associated with resistance to thyroid hormone in three unrelated patients.

Nagavalli S, Fletterick RJ, Ford G, Boston BA, Gianoukakis AG.

Thyroid. 2014 Sep;24(9):1430-1. doi: 10.1089/thy.2014.0086. Epub 2014 Jul 1. No abstract available.

17.

Plant Kinesin-Like Calmodulin Binding Protein Employs Its Regulatory Domain for Dimerization.

Vinogradova MV, Malanina GG, Waitzman JS, Rice SE, Fletterick RJ.

PLoS One. 2013 Jun 21;8(6):e66669. doi: 10.1371/journal.pone.0066669. Print 2013.

18.

Structure-based discovery of antagonists of nuclear receptor LRH-1.

Benod C, Carlsson J, Uthayaruban R, Hwang P, Irwin JJ, Doak AK, Shoichet BK, Sablin EP, Fletterick RJ.

J Biol Chem. 2013 Jul 5;288(27):19830-44. doi: 10.1074/jbc.M112.411686. Epub 2013 May 10.

19.

Structure of a novel winged-helix like domain from human NFRKB protein.

Kumar A, Möcklinghoff S, Yumoto F, Jaroszewski L, Farr CL, Grzechnik A, Nguyen P, Weichenberger CX, Chiu HJ, Klock HE, Elsliger MA, Deacon AM, Godzik A, Lesley SA, Conklin BR, Fletterick RJ, Wilson IA.

PLoS One. 2012;7(9):e43761. doi: 10.1371/journal.pone.0043761. Epub 2012 Sep 11.

20.

Structural basis of coactivation of liver receptor homolog-1 by β-catenin.

Yumoto F, Nguyen P, Sablin EP, Baxter JD, Webb P, Fletterick RJ.

Proc Natl Acad Sci U S A. 2012 Jan 3;109(1):143-8. doi: 10.1073/pnas.1117036108. Epub 2011 Dec 20.

21.

Nuclear receptor liver receptor homologue 1 (LRH-1) regulates pancreatic cancer cell growth and proliferation.

Benod C, Vinogradova MV, Jouravel N, Kim GE, Fletterick RJ, Sablin EP.

Proc Natl Acad Sci U S A. 2011 Oct 11;108(41):16927-31. doi: 10.1073/pnas.1112047108. Epub 2011 Sep 26.

22.

A conserved surface on the ligand binding domain of nuclear receptors for allosteric control.

Buzón V, Carbó LR, Estruch SB, Fletterick RJ, Estébanez-Perpiñá E.

Mol Cell Endocrinol. 2012 Jan 30;348(2):394-402. doi: 10.1016/j.mce.2011.08.012. Epub 2011 Aug 22. Review.

PMID:
21878368
23.

Targeting the regulation of androgen receptor signaling by the heat shock protein 90 cochaperone FKBP52 in prostate cancer cells.

De Leon JT, Iwai A, Feau C, Garcia Y, Balsiger HA, Storer CL, Suro RM, Garza KM, Lee S, Kim YS, Chen Y, Ning YM, Riggs DL, Fletterick RJ, Guy RK, Trepel JB, Neckers LM, Cox MB.

Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):11878-83. doi: 10.1073/pnas.1105160108. Epub 2011 Jul 5.

24.

Decoration of microtubules in solution by the kinesin-14, Ncd.

Hjelm RP, Stone DB, Fletterick RJ, Mendelson RA.

Acta Crystallogr D Biol Crystallogr. 2010 Nov;66(Pt 11):1218-23. doi: 10.1107/S0907444910021323. Epub 2010 Oct 20.

25.

Conformation switching of clathrin light chain regulates clathrin lattice assembly.

Wilbur JD, Hwang PK, Ybe JA, Lane M, Sellers BD, Jacobson MP, Fletterick RJ, Brodsky FM.

Dev Cell. 2010 May 18;18(5):841-8. doi: 10.1016/j.devcel.2010.04.007.

26.

Hormone binding and co-regulator binding to the glucocorticoid receptor are allosterically coupled.

Pfaff SJ, Fletterick RJ.

J Biol Chem. 2010 May 14;285(20):15256-67. doi: 10.1074/jbc.M110.108118. Epub 2010 Mar 24.

27.

Accommodation of structural rearrangements in the huntingtin-interacting protein 1 coiled-coil domain.

Wilbur JD, Hwang PK, Brodsky FM, Fletterick RJ.

Acta Crystallogr D Biol Crystallogr. 2010 Mar;66(Pt 3):314-8. doi: 10.1107/S0907444909054535. Epub 2010 Feb 12.

28.

Structure of the complex of a mitotic kinesin with its calcium binding regulator.

Vinogradova MV, Malanina GG, Reddy AS, Fletterick RJ.

Proc Natl Acad Sci U S A. 2009 May 19;106(20):8175-9. doi: 10.1073/pnas.0811131106. Epub 2009 May 5.

29.

The structure of corepressor Dax-1 bound to its target nuclear receptor LRH-1.

Sablin EP, Woods A, Krylova IN, Hwang P, Ingraham HA, Fletterick RJ.

Proc Natl Acad Sci U S A. 2008 Nov 25;105(47):18390-5. doi: 10.1073/pnas.0808936105. Epub 2008 Nov 17.

30.

Structure of SF-1 bound by different phospholipids: evidence for regulatory ligands.

Sablin EP, Blind RD, Krylova IN, Ingraham JG, Cai F, Williams JD, Fletterick RJ, Ingraham HA.

Mol Endocrinol. 2009 Jan;23(1):25-34. doi: 10.1210/me.2007-0508. Epub 2008 Nov 6.

31.

Molecular basis for dimer formation of TRbeta variant D355R.

Jouravel N, Sablin E, Togashi M, Baxter JD, Webb P, Fletterick RJ.

Proteins. 2009 Apr;75(1):111-7. doi: 10.1002/prot.22225.

32.

Actin binding by Hip1 (huntingtin-interacting protein 1) and Hip1R (Hip1-related protein) is regulated by clathrin light chain.

Wilbur JD, Chen CY, Manalo V, Hwang PK, Fletterick RJ, Brodsky FM.

J Biol Chem. 2008 Nov 21;283(47):32870-9. doi: 10.1074/jbc.M802863200. Epub 2008 Sep 12.

33.

6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.

Cruz LA, Estébanez-Perpiñá E, Pfaff S, Borngraeber S, Bao N, Blethrow J, Fletterick RJ, England PM.

J Med Chem. 2008 Sep 25;51(18):5856-60. doi: 10.1021/jm701517b.

34.

Structural dynamics of the microtubule binding and regulatory elements in the kinesin-like calmodulin binding protein.

Vinogradova MV, Malanina GG, Reddy VS, Reddy AS, Fletterick RJ.

J Struct Biol. 2008 Jul;163(1):76-83. doi: 10.1016/j.jsb.2008.04.004. Epub 2008 May 5.

PMID:
18513992
35.

Interaction between the androgen receptor and a segment of its corepressor SHP.

Jouravel N, Sablin E, Arnold LA, Guy RK, Fletterick RJ.

Acta Crystallogr D Biol Crystallogr. 2007 Nov;63(Pt 11):1198-200. Epub 2007 Oct 17.

PMID:
18007036
36.

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

Arnold LA, Kosinski A, Estébanez-Perpiñá E, Fletterick RJ, Guy RK.

J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.

37.

A surface on the androgen receptor that allosterically regulates coactivator binding.

Estébanez-Perpiñá E, Arnold LA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ.

Proc Natl Acad Sci U S A. 2007 Oct 9;104(41):16074-9. Epub 2007 Oct 2. Erratum in: Proc Natl Acad Sci U S A. 2007 Nov 20;104(47):18874. Arnold, Alexander A [corrected to Arnold, Leggy A].

38.

Perspectives on designs of antiandrogens for prostate cancer.

Estébanez-Perpiñá E, Jouravel N, Fletterick RJ.

Expert Opin Drug Discov. 2007 Oct;2(10):1341-55. doi: 10.1517/17460441.2.10.1341.

PMID:
23484530
39.

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor.

Estébanez-Perpiñá E, Arnold LA, Jouravel N, Togashi M, Blethrow J, Mar E, Nguyen P, Phillips KJ, Baxter JD, Webb P, Guy RK, Fletterick RJ.

Mol Endocrinol. 2007 Dec;21(12):2919-28. Epub 2007 Sep 6.

PMID:
17823305
40.

The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family.

Wang SX, Pandey KC, Scharfstein J, Whisstock J, Huang RK, Jacobelli J, Fletterick RJ, Rosenthal PJ, Abrahamson M, Brinen LS, Rossi A, Sali A, McKerrow JH.

Structure. 2007 May;15(5):535-43.

41.

Ca ion and the troponin switch.

Vinogradova MV, Stone DB, Malanina GG, Mendelson RA, Fletterick RJ.

Adv Exp Med Biol. 2007;592:47-57. Review. No abstract available.

PMID:
17278355
42.

Directed evolution of an anti-prion protein scFv fragment to an affinity of 1 pM and its structural interpretation.

Luginbühl B, Kanyo Z, Jones RM, Fletterick RJ, Prusiner SB, Cohen FE, Williamson RA, Burton DR, Plückthun A.

J Mol Biol. 2006 Oct 13;363(1):75-97. Epub 2006 Jul 21.

PMID:
16962610
43.

Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease.

Wang SX, Pandey KC, Somoza JR, Sijwali PS, Kortemme T, Brinen LS, Fletterick RJ, Rosenthal PJ, McKerrow JH.

Proc Natl Acad Sci U S A. 2006 Aug 1;103(31):11503-8. Epub 2006 Jul 24.

44.

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding.

Arnold LA, Estébanez-Perpiñá E, Togashi M, Shelat A, Ocasio CA, McReynolds AC, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK.

Sci STKE. 2006 Jun 27;2006(341):pl3.

PMID:
16804159
45.

An atomic model of the thin filament in the relaxed and Ca2+-activated states.

Pirani A, Vinogradova MV, Curmi PM, King WA, Fletterick RJ, Craig R, Tobacman LS, Xu C, Hatch V, Lehman W.

J Mol Biol. 2006 Mar 31;357(3):707-17. Epub 2006 Jan 13.

PMID:
16469331
46.

Dynamics of the C-terminal region of TnI in the troponin complex in solution.

Blumenschein TM, Stone DB, Fletterick RJ, Mendelson RA, Sykes BD.

Biophys J. 2006 Apr 1;90(7):2436-44. Epub 2006 Jan 13.

48.

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators.

Arnold LA, Estébanez-Perpiñá E, Togashi M, Jouravel N, Shelat A, McReynolds AC, Mar E, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK.

J Biol Chem. 2005 Dec 30;280(52):43048-55. Epub 2005 Oct 31.

49.

Conformational adaptation of nuclear receptor ligand binding domains to agonists: potential for novel approaches to ligand design.

Togashi M, Borngraeber S, Sandler B, Fletterick RJ, Webb P, Baxter JD.

J Steroid Biochem Mol Biol. 2005 Feb;93(2-5):127-37. Epub 2005 Feb 19. Review.

PMID:
15860255
50.

Calcium-dependent changes in the flexibility of the regulatory domain of troponin C in the troponin complex.

Blumenschein TM, Stone DB, Fletterick RJ, Mendelson RA, Sykes BD.

J Biol Chem. 2005 Jun 10;280(23):21924-32. Epub 2005 Apr 12.

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