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Items: 1 to 50 of 55

1.

Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer.

Ponnusamy S, He Y, Hwang DJ, Thiyagarajan T, Houtman R, Bocharova V, Sumpter BG, Fernandez E, Johnson D, Du Z, Pfeffer LM, Getzenberg RH, McEwan IJ, Miller DD, Narayanan R.

Clin Cancer Res. 2019 Sep 3. doi: 10.1158/1078-0432.CCR-19-1458. [Epub ahead of print]

PMID:
31481513
2.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.

Guan J, Zhou W, Hafner M, Blake RA, Chalouni C, Chen IP, De Bruyn T, Giltnane JM, Hartman SJ, Heidersbach A, Houtman R, Ingalla E, Kategaya L, Kleinheinz T, Li J, Martin SE, Modrusan Z, Nannini M, Oeh J, Ubhayakar S, Wang X, Wertz IE, Young A, Yu M, Sampath D, Hager JH, Friedman LS, Daemen A, Metcalfe C.

Cell. 2019 Aug 8;178(4):949-963.e18. doi: 10.1016/j.cell.2019.06.026. Epub 2019 Jul 25.

PMID:
31353221
3.

A Model of Glucocorticoid Receptor Interaction With Coregulators Predicts Transcriptional Regulation of Target Genes.

Monczor F, Chatzopoulou A, Zappia CD, Houtman R, Meijer OC, Fitzsimons CP.

Front Pharmacol. 2019 Mar 13;10:214. doi: 10.3389/fphar.2019.00214. eCollection 2019.

4.

Corticosteroid Action in the Brain: The Potential of Selective Receptor Modulation.

Viho EMG, Buurstede JC, Mahfouz A, Koorneef LL, van Weert LTCM, Houtman R, Hunt HJ, Kroon J, Meijer OC.

Neuroendocrinology. 2019;109(3):266-276. doi: 10.1159/000499659. Epub 2019 Mar 19. Review.

5.

ARv7 Represses Tumor-Suppressor Genes in Castration-Resistant Prostate Cancer.

Cato L, de Tribolet-Hardy J, Lee I, Rottenberg JT, Coleman I, Melchers D, Houtman R, Xiao T, Li W, Uo T, Sun S, Kuznik NC, Göppert B, Ozgun F, van Royen ME, Houtsmuller AB, Vadhi R, Rao PK, Li L, Balk SP, Den RB, Trock BJ, Karnes RJ, Jenkins RB, Klein EA, Davicioni E, Gruhl FJ, Long HW, Liu XS, Cato ACB, Lack NA, Nelson PS, Plymate SR, Groner AC, Brown M.

Cancer Cell. 2019 Mar 18;35(3):401-413.e6. doi: 10.1016/j.ccell.2019.01.008. Epub 2019 Feb 14.

PMID:
30773341
6.

Natural helix 9 mutants of PPARγ differently affect its transcriptional activity.

Broekema MF, Massink MPG, Donato C, de Ligt J, Schaarschmidt J, Borgman A, Schooneman MG, Melchers D, Gerding MN, Houtman R, Bonvin AMJJ, Majithia AR, Monajemi H, van Haaften GW, Soeters MR, Kalkhoven E.

Mol Metab. 2019 Feb;20:115-127. doi: 10.1016/j.molmet.2018.12.005. Epub 2018 Dec 16.

7.

The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.

Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Han R, Lainé M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL.

Elife. 2018 Nov 29;7. pii: e37161. doi: 10.7554/eLife.37161.

8.

The Nuclear Receptor PPARγ Controls Progressive Macrophage Polarization as a Ligand-Insensitive Epigenomic Ratchet of Transcriptional Memory.

Daniel B, Nagy G, Czimmerer Z, Horvath A, Hammers DW, Cuaranta-Monroy I, Poliska S, Tzerpos P, Kolostyak Z, Hays TT, Patsalos A, Houtman R, Sauer S, Francois-Deleuze J, Rastinejad F, Balint BL, Sweeney HL, Nagy L.

Immunity. 2018 Oct 16;49(4):615-626.e6. doi: 10.1016/j.immuni.2018.09.005.

9.

Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.

Puyang X, Furman C, Zheng GZ, Wu ZJ, Banka D, Aithal K, Agoulnik S, Bolduc DM, Buonamici S, Caleb B, Das S, Eckley S, Fekkes P, Hao MH, Hart A, Houtman R, Irwin S, Joshi JJ, Karr C, Kim A, Kumar N, Kumar P, Kuznetsov G, Lai WG, Larsen N, Mackenzie C, Martin LA, Melchers D, Moriarty A, Nguyen TV, Norris J, O'Shea M, Pancholi S, Prajapati S, Rajagopalan S, Reynolds DJ, Rimkunas V, Rioux N, Ribas R, Siu A, Sivakumar S, Subramanian V, Thomas M, Vaillancourt FH, Wang J, Wardell S, Wick MJ, Yao S, Yu L, Warmuth M, Smith PG, Zhu P, Korpal M.

Cancer Discov. 2018 Sep;8(9):1176-1193. doi: 10.1158/2159-8290.CD-17-1229. Epub 2018 Jul 10.

10.

Profiling of 3696 Nuclear Receptor-Coregulator Interactions: A Resource for Biological and Clinical Discovery.

Broekema MF, Hollman DAA, Koppen A, van den Ham HJ, Melchers D, Pijnenburg D, Ruijtenbeek R, van Mil SWC, Houtman R, Kalkhoven E.

Endocrinology. 2018 Jun 1;159(6):2397-2407. doi: 10.1210/en.2018-00149.

PMID:
29718163
11.

ZB716, a steroidal selective estrogen receptor degrader (SERD), is orally efficacious in blocking tumor growth in mouse xenograft models.

Guo S, Zhang C, Bratton M, Mottamal M, Liu J, Ma P, Zheng S, Zhong Q, Yang L, Wiese TE, Wu Y, Ellis MJ, Matossian M, Burow ME, Miele L, Houtman R, Wang G.

Oncotarget. 2018 Jan 8;9(6):6924-6937. doi: 10.18632/oncotarget.24023. eCollection 2018 Jan 23.

12.

The effects of all-trans retinoic acid on estrogen receptor signaling in the estrogen-sensitive MCF/BUS subline.

Miro Estruch I, de Haan LHJ, Melchers D, Houtman R, Louisse J, Groten JP, Rietjens IMCM.

J Recept Signal Transduct Res. 2018 Apr;38(2):112-121. doi: 10.1080/10799893.2018.1436559. Epub 2018 Feb 15.

PMID:
29447503
13.

Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations.

Jeselsohn R, Bergholz JS, Pun M, Cornwell M, Liu W, Nardone A, Xiao T, Li W, Qiu X, Buchwalter G, Feiglin A, Abell-Hart K, Fei T, Rao P, Long H, Kwiatkowski N, Zhang T, Gray N, Melchers D, Houtman R, Liu XS, Cohen O, Wagle N, Winer EP, Zhao J, Brown M.

Cancer Cell. 2018 Feb 12;33(2):173-186.e5. doi: 10.1016/j.ccell.2018.01.004.

14.

Selective Mineralocorticoid Receptor Cofactor Modulation as Molecular Basis for Finerenone's Antifibrotic Activity.

Grune J, Beyhoff N, Smeir E, Chudek R, Blumrich A, Ban Z, Brix S, Betz IR, Schupp M, Foryst-Ludwig A, Klopfleisch R, Stawowy P, Houtman R, Kolkhof P, Kintscher U.

Hypertension. 2018 Apr;71(4):599-608. doi: 10.1161/HYPERTENSIONAHA.117.10360. Epub 2018 Feb 5.

PMID:
29437893
15.

Differential in Vitro Biological Action, Coregulator Interactions, and Molecular Dynamic Analysis of Bisphenol A (BPA), BPAF, and BPS Ligand-ERα Complexes.

Li Y, Perera L, Coons LA, Burns KA, Tyler Ramsey J, Pelch KE, Houtman R, van Beuningen R, Teng CT, Korach KS.

Environ Health Perspect. 2018 Jan 31;126(1):017012. doi: 10.1289/EHP2505.

16.

Coregulator profiling of the glucocorticoid receptor in lymphoid malignancies.

Clarisse D, Thommis J, Van Wesemael K, Houtman R, Ratman D, Tavernier J, Offner F, Beck I, De Bosscher K.

Oncotarget. 2017 Nov 30;8(65):109675-109691. doi: 10.18632/oncotarget.22764. eCollection 2017 Dec 12.

17.

Selective Glucocorticoid Receptor Properties of GSK866 Analogs with Cysteine Reactive Warheads.

Chirumamilla CS, Palagani A, Kamaraj B, Declerck K, Verbeek MWC, Oksana R, De Bosscher K, Bougarne N, Ruttens B, Gevaert K, Houtman R, De Vos WH, Joossens J, Van Der Veken P, Augustyns K, Van Ostade X, Bogaerts A, De Winter H, Vanden Berghe W.

Front Immunol. 2017 Nov 1;8:1324. doi: 10.3389/fimmu.2017.01324. eCollection 2017.

18.

Carbonyl reductase 1 catalyzes 20β-reduction of glucocorticoids, modulating receptor activation and metabolic complications of obesity.

Morgan RA, Beck KR, Nixon M, Homer NZM, Crawford AA, Melchers D, Houtman R, Meijer OC, Stomby A, Anderson AJ, Upreti R, Stimson RH, Olsson T, Michoel T, Cohain A, Ruusalepp A, Schadt EE, Björkegren JLM, Andrew R, Kenyon CJ, Hadoke PWF, Odermatt A, Keen JA, Walker BR.

Sci Rep. 2017 Sep 6;7(1):10633. doi: 10.1038/s41598-017-10410-1.

19.

Compound A influences gene regulation of the Dexamethasone-activated glucocorticoid receptor by alternative cofactor recruitment.

Desmet SJ, Bougarne N, Van Moortel L, De Cauwer L, Thommis J, Vuylsteke M, Ratman D, Houtman R, Tavernier J, De Bosscher K.

Sci Rep. 2017 Aug 14;7(1):8063. doi: 10.1038/s41598-017-07941-y.

20.

Binding of bisphenol A, bisphenol AF, and bisphenol S on the androgen receptor: Coregulator recruitment and stimulation of potential interaction sites.

Perera L, Li Y, Coons LA, Houtman R, van Beuningen R, Goodwin B, Auerbach SS, Teng CT.

Toxicol In Vitro. 2017 Oct;44:287-302. doi: 10.1016/j.tiv.2017.07.020. Epub 2017 Jul 24.

21.

Characterization of the differential coregulator binding signatures of the Retinoic Acid Receptor subtypes upon (ant)agonist action.

Miro Estruch I, Melchers D, Houtman R, de Haan LHJ, Groten JP, Louisse J, Rietjens IMCM.

Biochim Biophys Acta Proteins Proteom. 2017 Sep;1865(9):1195-1206. doi: 10.1016/j.bbapap.2017.06.011. Epub 2017 Jun 20.

PMID:
28642153
22.

The AF-1-deficient estrogen receptor ERα46 isoform is frequently expressed in human breast tumors.

Chantalat E, Boudou F, Laurell H, Palierne G, Houtman R, Melchers D, Rochaix P, Filleron T, Stella A, Burlet-Schiltz O, Brouchet A, Flouriot G, Métivier R, Arnal JF, Fontaine C, Lenfant F.

Breast Cancer Res. 2016 Dec 7;18(1):123.

23.

Co-activator candidate interactions for orphan nuclear receptor NR2E1.

Corso-Díaz X, de Leeuw CN, Alonso V, Melchers D, Wong BK, Houtman R, Simpson EM.

BMC Genomics. 2016 Oct 26;17(1):832.

24.

Differential modulation of FXR activity by chlorophacinone and ivermectin analogs.

Hsu CW, Hsieh JH, Huang R, Pijnenburg D, Khuc T, Hamm J, Zhao J, Lynch C, van Beuningen R, Chang X, Houtman R, Xia M.

Toxicol Appl Pharmacol. 2016 Dec 15;313:138-148. doi: 10.1016/j.taap.2016.10.017. Epub 2016 Oct 20.

25.

Trade-offs and efficiencies in optimal budget-constrained multispecies corridor networks.

Dilkina B, Houtman R, Gomes CP, Montgomery CA, McKelvey KS, Kendall K, Graves TA, Bernstein R, Schwartz MK.

Conserv Biol. 2017 Feb;31(1):192-202. doi: 10.1111/cobi.12814. Epub 2016 Sep 27.

PMID:
27677418
26.

TRIM24 Is an Oncogenic Transcriptional Activator in Prostate Cancer.

Groner AC, Cato L, de Tribolet-Hardy J, Bernasocchi T, Janouskova H, Melchers D, Houtman R, Cato ACB, Tschopp P, Gu L, Corsinotti A, Zhong Q, Fankhauser C, Fritz C, Poyet C, Wagner U, Guo T, Aebersold R, Garraway LA, Wild PJ, Theurillat JP, Brown M.

Cancer Cell. 2016 Jun 13;29(6):846-858. doi: 10.1016/j.ccell.2016.04.012. Epub 2016 May 26.

27.

The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide.

Prekovic S, van Royen ME, Voet AR, Geverts B, Houtman R, Melchers D, Zhang KY, Van den Broeck T, Smeets E, Spans L, Houtsmuller AB, Joniau S, Claessens F, Helsen C.

Mol Cancer Ther. 2016 Jul;15(7):1702-12. doi: 10.1158/1535-7163.MCT-15-0892. Epub 2016 May 16.

28.

Predictive features of ligand-specific signaling through the estrogen receptor.

Nwachukwu JC, Srinivasan S, Zheng Y, Wang S, Min J, Dong C, Liao Z, Nowak J, Wright NJ, Houtman R, Carlson KE, Josan JS, Elemento O, Katzenellenbogen JA, Zhou HB, Nettles KW.

Mol Syst Biol. 2016 Apr 22;12(4):864. doi: 10.15252/msb.20156701.

29.

Destabilization of the torsioned conformation of a ligand side chain inverts the LXRβ activity.

Álvarez LD, Dansey MV, Grinman DY, Navalesi D, Samaja GA, Del Fueyo MC, Bastiaensen N, Houtman R, Estrin DA, Veleiro AS, Pecci A, Burton G.

Biochim Biophys Acta. 2015 Dec;1851(12):1577-86. doi: 10.1016/j.bbalip.2015.09.007. Epub 2015 Oct 3.

PMID:
26434697
30.

The effect of glucuronidation on isoflavone induced estrogen receptor (ER)α and ERβ mediated coregulator interactions.

Beekmann K, de Haan LH, Actis-Goretta L, Houtman R, van Bladeren PJ, Rietjens IM.

J Steroid Biochem Mol Biol. 2015 Nov;154:245-53. doi: 10.1016/j.jsbmb.2015.09.002. Epub 2015 Sep 7.

PMID:
26361015
31.

A Mixed Glucocorticoid/Mineralocorticoid Selective Modulator With Dominant Antagonism in the Male Rat Brain.

Atucha E, Zalachoras I, van den Heuvel JK, van Weert LT, Melchers D, Mol IM, Belanoff JK, Houtman R, Hunt H, Roozendaal B, Meijer OC.

Endocrinology. 2015 Nov;156(11):4105-14. doi: 10.1210/en.2015-1390. Epub 2015 Aug 25.

PMID:
26305887
32.

Cofactor profiling of the glucocorticoid receptor from a cellular environment.

Desmet SJ, Dejager L, Clarisse D, Thommis J, Melchers D, Bastiaensen N, Ruijtenbeek R, Beck IM, Libert C, Houtman R, Meijer OC, De Bosscher K.

Methods Mol Biol. 2014;1204:83-94. doi: 10.1007/978-1-4939-1346-6_8.

PMID:
25182763
33.

Identification of coregulators influenced by estrogen receptor subtype specific binding of the ER antagonists 4-hydroxytamoxifen and fulvestrant.

Evers NM, Wang S, van den Berg JH, Houtman R, Melchers D, de Haan LH, Ederveen AG, Groten JP, Rietjens IM.

Chem Biol Interact. 2014 Sep 5;220:222-30. doi: 10.1016/j.cbi.2014.06.019. Epub 2014 Jul 8.

PMID:
25014417
34.

Extending an in vitro panel for estrogenicity testing: the added value of bioassays for measuring antiandrogenic activities and effects on steroidogenesis.

Wang S, Rijk JC, Besselink HT, Houtman R, Peijnenburg AA, Brouwer A, Rietjens IM, Bovee TF.

Toxicol Sci. 2014 Sep;141(1):78-89. doi: 10.1093/toxsci/kfu103. Epub 2014 Jun 13.

35.

Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists.

Evers NM, van den Berg JH, Wang S, Melchers D, Houtman R, de Haan LH, Ederveen AG, Groten JP, Rietjens IM.

J Steroid Biochem Mol Biol. 2014 Sep;143:376-85. doi: 10.1016/j.jsbmb.2014.06.002. Epub 2014 Jun 9.

PMID:
24923734
36.

Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network.

Nwachukwu JC, Srinivasan S, Bruno NE, Parent AA, Hughes TS, Pollock JA, Gjyshi O, Cavett V, Nowak J, Garcia-Ordonez RD, Houtman R, Griffin PR, Kojetin DJ, Katzenellenbogen JA, Conkright MD, Nettles KW.

Elife. 2014 Apr 25;3:e02057. doi: 10.7554/eLife.02057.

37.

Thalidomide increases human hepatic cytochrome P450 3A enzymes by direct activation of the pregnane X receptor.

Murayama N, van Beuningen R, Suemizu H, Guillouzo CG, Shibata N, Yajima K, Utoh M, Shimizu M, Chesné C, Nakamura M, Guengerich FP, Houtman R, Yamazaki H.

Chem Res Toxicol. 2014 Feb 17;27(2):304-308. doi: 10.1021/tx4004374. Epub 2014 Feb 5.

38.

A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23 reference compounds.

Wang S, Houtman R, Melchers D, Aarts J, Peijnenburg A, van Beuningen R, Rietjens I, Bovee TF.

ALTEX. 2013;30(2):145-57. doi: 10.14573/altex.2013.2.145.

39.

Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator.

Zalachoras I, Houtman R, Atucha E, Devos R, Tijssen AM, Hu P, Lockey PM, Datson NA, Belanoff JK, Lucassen PJ, Joëls M, de Kloet ER, Roozendaal B, Hunt H, Meijer OC.

Proc Natl Acad Sci U S A. 2013 May 7;110(19):7910-5. doi: 10.1073/pnas.1219411110. Epub 2013 Apr 23.

40.

Understanding stress-effects in the brain via transcriptional signal transduction pathways.

Zalachoras I, Houtman R, Meijer OC.

Neuroscience. 2013 Jul 9;242:97-109. doi: 10.1016/j.neuroscience.2013.03.038. Epub 2013 Mar 29. Review.

PMID:
23545270
41.

Robust array-based coregulator binding assay predicting ERα-agonist potency and generating binding profiles reflecting ligand structure.

Aarts JM, Wang S, Houtman R, van Beuningen RM, Westerink WM, Van De Waart BJ, Rietjens IM, Bovee TF.

Chem Res Toxicol. 2013 Mar 18;26(3):336-46. doi: 10.1021/tx300463b. Epub 2013 Mar 6.

PMID:
23383871
42.

Short-chain fatty acids stimulate angiopoietin-like 4 synthesis in human colon adenocarcinoma cells by activating peroxisome proliferator-activated receptor γ.

Alex S, Lange K, Amolo T, Grinstead JS, Haakonsson AK, Szalowska E, Koppen A, Mudde K, Haenen D, Al-Lahham S, Roelofsen H, Houtman R, van der Burg B, Mandrup S, Bonvin AM, Kalkhoven E, Müller M, Hooiveld GJ, Kersten S.

Mol Cell Biol. 2013 Apr;33(7):1303-16. doi: 10.1128/MCB.00858-12. Epub 2013 Jan 22.

43.

Serine-305 phosphorylation modulates estrogen receptor alpha binding to a coregulator peptide array, with potential application in predicting responses to tamoxifen.

Houtman R, de Leeuw R, Rondaij M, Melchers D, Verwoerd D, Ruijtenbeek R, Martens JW, Neefjes J, Michalides R.

Mol Cancer Ther. 2012 Apr;11(4):805-16. doi: 10.1158/1535-7163.MCT-11-0855. Epub 2012 Feb 7.

44.

Nuclear receptor-coregulator interaction profiling identifies TRIP3 as a novel peroxisome proliferator-activated receptor gamma cofactor.

Koppen A, Houtman R, Pijnenburg D, Jeninga EH, Ruijtenbeek R, Kalkhoven E.

Mol Cell Proteomics. 2009 Oct;8(10):2212-26. doi: 10.1074/mcp.M900209-MCP200. Epub 2009 Jul 10.

45.

Estrogenic effects in the immature rat uterus after dietary exposure to ethinylestradiol and zearalenone using a systems biology approach.

Heneweer M, Houtman R, Poortman J, Groot M, Maliepaard C, Peijnenburg A.

Toxicol Sci. 2007 Sep;99(1):303-14. Epub 2007 Jun 8.

PMID:
17557909
46.

Asthma, the ugly duckling of lung disease proteomics?

Houtman R, van den Worm E.

J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 5;815(1-2):285-94. Review.

PMID:
15652817
47.

Lung proteome alterations in a mouse model for nonallergic asthma.

Houtman R, Krijgsveld J, Kool M, Romijn EP, Redegeld FA, Nijkamp FP, Heck AJ, Humphery-Smith I.

Proteomics. 2003 Oct;3(10):2008-18.

PMID:
14625863
48.

Integrin VLA-5: modulator and activator of mast cells.

Houtman R, Koster AS, Nijkamp FP.

Clin Exp Allergy. 2001 Jun;31(6):817-22. Review. No abstract available.

PMID:
11422144
49.

Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands.

Houtman R, Ten Broeke R, Blalock JE, Villain M, Koster AS, Nijkamp FP.

J Immunol. 2001 Jan 15;166(2):861-7.

50.

Psychological aspects of bone marrow transplantation: a retrospective study of 17 long-term survivors.

Hengeveld MW, Houtman RB, Zwaan FE.

Bone Marrow Transplant. 1988 Jan;3(1):69-75.

PMID:
3048473

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