Scientific Publications NHR

The number of peer-reviewed publications using PamGene's technology is continuing to increase.

Below you will find a selection of scientific publications where PamGene's technology has been applied.

For further information or reprints, please contact us or send an email to info@pamgene.com

Publications for the Sections:

Nuclear Receptors
 
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. 2018 Dec 16
 
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
 
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
 
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 Jul 10. doi: 10.1158/2159-8290.CD-17-1229.
 
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.
 
 
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 Feb 15:1-10.
 
 
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
 
 
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.
 
 
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.
 
 
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.


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. (2017) Front Immunol. Nov 1;8:1324. eCollection 2017.

 

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. (2017) Sci Rep. Sep 6; 7 (1) : 10633.

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. (2017) Toxicol In Vitro. Oct;44:287-302

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. (2017) Sci Rep. Aug 14;7(1):8063

Characterization of the differential coregulator binding signatures of the Retinoic Acid Receptor subtypes upon (ant)agonist action.
Estruch MI, Melchers D, Houtman R, de Haan LHJ, Groten JP, Louisse J, Rietjens IMCM.
(2017) Biochim Biophys Acta. Sep;1865(9):1195-1206.

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

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

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. (2016) Toxicol Appl Pharmacol. Dec 15;313:138-148. 

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 AC, 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. (2016) Cancer Cell. Jun 13;29(6):846-58. 

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. (2016) Mol Cancer Ther. Jul;15(7):1702-12.

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. (2016) Mol Syst Biol. Apr 22;12(4):864. 

Destabilization of the torsioned conformation of a ligand side chain inverts the LXRβ activity.
Álvarez LD, Virginia Dansey M, Grinman DY, Navalesi D, Samaja GA, Celeste Del Fueyo M, Bastiaensen N, Houtman R, Estrin DA, Veleiro AS, Pecci A, Burton G. Biochim Biophys Acta. (2015) Dec;1851(12):1577-86.

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.

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.

Subtype-specific modulation of estrogen receptor-coactivator interaction by phosphorylation.
Tharun IM, Nieto L, Haase C, Scheepstra M, Balk M, Möcklinghoff S, Adriaens W, Dames SA, Brunsveld L. ACS Chem Biol. (2015) Feb 20;10(2):475-84

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 1;141(1):78-89

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.

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) Jul 8;220C:222-230

A natural-product switch for a dynamic protein interface.
Scheepstra M, Nieto L, Hirsch AK, Fuchs S, Leysen S, Lam CV, in het Panhuis L, van Boeckel CA, Wienk H, Boelens R, Ottmann C, Milroy LG, Brunsveld L. Angew Chem Int Ed Engl. (2014) Jun 16;53(25):6443-8

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. 

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 O1, 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.

Thalidomide increases human hepatic cytochrome P450 3A enzymes by direct activation of the pregnane X receptor.
Murayama N, van Beuningen R, Suemizu H, Guguen-Guillouzo C, 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):304-8.

Understanding stress-effects in the brain via transcriptional signal transduction pathways.
Zalachoras I, Houtman R, Meijer OC. Neuroscience (2013) Jul 9;242:97-109

Differential Targeting of Brain Stress Circuits with a Selective Glucorticoid 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

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.

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.

A 155-plex high-throughput in vitro 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.

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.
 
 

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.
 
 

Effect of synthetic dietary triglycerides: a novel research paradigm for nutrigenomics.
Sanderson LM, de Groot PJ, Hooiveld GJ, Koppen A, Kalkhoven E, Müller M, Kersten S. PLoS One. (2008) Feb 27;3(2):e1681.
 
 

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.