Research Topics
Genomes and Genes | Frank ClaessensSummaryAffiliation: Katholieke Universiteit Leuven Country: Belgium Publications
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Publications
Selective DNA binding by the androgen receptor as a mechanism for hormone-specific gene regulationF Claessens
Laboratory for Biochemistry, Gasthuisberg, Catholic University of Leuven, Herestraat 49, B 3000, Leuven, Belgium
J Steroid Biochem Mol Biol 76:23-30. 2001....- DNA recognition by nuclear receptorsFrank Claessens
Department of Molecular Cell Biology, Faculty of Medicine, Campus GHB O N, Herestraat 49, 3000 Leuven, Belgium
Essays Biochem 40:59-72. 2004..The DNA-binding domain therefore plays a central role, not only in the correct binding of the receptors to the target genes, but also in the control of other steps of the action mechanism of nuclear receptors... 
Loss of androgen receptor binding to selective androgen response elements causes a reproductive phenotype in a knockin mouse modelKris Schauwaers
Molecular Endocrinology Laboratory, Department of Molecular Cell Biology, Catholic University of Leuven, Campus Gasthuisberg, Herestraat 49, B 3000 Leuven, Belgium
Proc Natl Acad Sci U S A 104:4961-6. 2007..In this report, we present the first in vivo evidence of the existence of two functionally different types of AREs and demonstrate that AR-regulated gene expression can be targeted based on this distinction...
A 629RKLKK633 motif in the hinge region controls the androgen receptor at multiple levelsTamzin M Tanner
Molecular Endocrinology Laboratory, Department of Molecular Cell Biology, Catholic University of Leuven, Campus Gasthuisberg O and N1, Herestraat 49, Box 901, 3000, Leuven, Belgium
Cell Mol Life Sci 67:1919-27. 2010..Taken together, the (629)RKLKK(633) motif is a multifunctional motif that integrates nuclear localization, receptor stability, DNA binding, transactivation potential and intranuclear mobility...- Identification of an androgen response element in intron 8 of the sterol regulatory element-binding protein cleavage-activating protein gene allowing direct regulation by the androgen receptorHannelore Heemers
Laboratory for Experimental Medicine and Endocrinology, Faculty of Medicine, Onderwijs en Navorsing, Gasthuisberg, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium
J Biol Chem 279:30880-7. 2004..The identification of a steroid response element in intron 8 of the SCAP gene further supports the contention that SCAP is a direct target for steroid hormone action... - The rules of DNA recognition by the androgen receptorSarah Denayer
Katholieke Universiteit Leuven, Campus Gasthuisberg, O N1, Herestraat 49, 3000 Leuven, Belgium
Mol Endocrinol 24:898-913. 2010..So far, all AR-binding genomic fragments that were analyzed contain AREs defined as receptor-dimer binding motifs with the ability to confer responsiveness to a reporter gene... - A role for selective androgen response elements in the development of the epididymis and the androgen control of the 5α reductase II geneStefanie Kerkhofs
Department of Cellular and Molecular Medicine, Katholieke Univesiteit Leuven, Campus Gasthuisberg O and N1 P O Box 901, Herestraat 49, 3000 Leuven, Belgium
FASEB J 26:4360-72. 2012..We conclude that the SPARKI model can be considered a knockout model for AR functioning via selective AREs and that this has a dramatic effect on sperm maturation in the epididymis... - Implications of a polyglutamine tract in the function of the human androgen receptorLeen Callewaert
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg O N, University of Leuven, O N, Herestraat 49, B 3000, Louvain, Belgium
Biochem Biophys Res Commun 306:46-52. 2003..This is reflected by an enhanced coactivation of the AR by SRC-1e... - Characterization of the two coactivator-interacting surfaces of the androgen receptor and their relative role in transcriptional controlValerie Christiaens
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Herestraat 49, B-3000 Leuven, Belgium
J Biol Chem 277:49230-7. 2002..We propose, therefore, that the androgen receptor-coactivator complex has several alternative conformations, depending partially on the context of the enhancer... - The hinge region regulates DNA binding, nuclear translocation, and transactivation of the androgen receptorAnnemie Haelens
Molecular Endocrinology Laboratory, Department of Molecular Cell Biology, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Leuven, Belgium
Cancer Res 67:4514-23. 2007..In conclusion, the description of prostate cancer mutations has led to the discovery of a complex role of the hinge region in nuclear localization, DNA binding, coactivator recruitment, and N/C interaction of the AR... - Expression of Tubb3, a beta-tubulin isotype, is regulated by androgens in mouse and rat Sertoli cellsKarel De Gendt
Laboratory of Experimental Medicine and Endocrinology, Catholic University of Leuven, Leuven, Belgium
Biol Reprod 85:934-45. 2011.... - Structural basis for nuclear hormone receptor DNA bindingChristine Helsen
Molecular Endocrinology Laboratory, Department Molecular Cell Biology, Campus GHB, ON1, Herestraat 49, 3000 Leuven, Belgium
Mol Cell Endocrinol 348:411-7. 2012..Moreover, allosteric signals passing through towards other receptor domains, explain why to some extent, the DNA elements can also be considered as controlling ligands... - Dual function of an amino-terminal amphipatic helix in androgen receptor-mediated transactivation through specific and nonspecific response elementsLeen Callewaert
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Herestraat 49, Belgium
J Biol Chem 278:8212-8. 2003.... - DNA recognition by the androgen receptor: evidence for an alternative DNA-dependent dimerization, and an active role of sequences flanking the response element on transactivationAnnemie Haelens
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Herestraat 49, B-3000 Leuven, Belgium
Biochem J 369:141-51. 2003..In addition, the sequences flanking an androgen-response element can control the activity of the androgen receptor... - Fracture risk and zoledronic acid therapy in men with osteoporosisSteven Boonen
Katholieke Universiteit Leuven, Leuven, Belgium
N Engl J Med 367:1714-23. 2012..Fractures in men are a major health issue, and data on the antifracture efficacy of therapies for osteoporosis in men are limited. We studied the effect of zoledronic acid on fracture risk among men with osteoporosis... - Interplay between two hormone-independent activation domains in the androgen receptorLeen Callewaert
Molecular Endocrinology Laboratory, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Leuven, Belgium
Cancer Res 66:543-53. 2006..This better definition of the mechanisms of action of both Tau-1 and Tau-5 is instrumental for the design of alternative therapeutic strategies against prostate cancer... - Identification of androgen-selective androgen-response elements in the human aquaporin-5 and Rad9 genesUdo Moehren
Laboratory of Molecular Endocrinology, Department of Molecular Cell Biology, Faculty of Medicine, Catholic University of Leuven, Campus Gasthuisberg, Onderwijs en Navorsing I, Box 901, Herestraat 49, B 3000 Leuven, Belgium
Biochem J 411:679-86. 2008..Our data indicate the validity of the hypothesis that selective AREs are recognizable as direct 5'-TGTTCT-3' repeats, and extend the list of currently known selective elements... - Functional interplay between two response elements with distinct binding characteristics dictates androgen specificity of the mouse sex-limited protein enhancerGuy Verrijdt
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg, University of Leuven, Leuven B-3000, Belgium
J Biol Chem 277:35191-201. 2002.... - Diverse roles of androgen receptor (AR) domains in AR-mediated signalingFrank Claessens
Molecular Endocrinology Laboratory, Campus Gasthuisberg, University of Leuven, Leuven, Belgium
Nucl Recept Signal 6:e008. 2008.... - Evidence for DNA-binding domain--ligand-binding domain communications in the androgen receptorChristine Helsen
Laboratory of Molecular Endocrinology, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium
Mol Cell Biol 32:3033-43. 2012..We therefore propose that these residues are involved in allosteric communications between the AR-DBD and AR-LBD... - The hinge region in androgen receptor controlLiesbeth Clinckemalie
Molecular Endocrinology Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Campus Gasthuisberg O and N1, Herestraat 49, 3000 Leuven, Belgium
Mol Cell Endocrinol 358:1-8. 2012..In conclusion, the hinge region serves as an integrator for signals coming from different pathways that provide feedback to the control of AR activity... - Time to onset of antifracture efficacy and year-by-year persistence of effect of zoledronic acid in women with osteoporosisSteven Boonen
University of Leuven, Leuven, Belgium
J Bone Miner Res 27:1487-93. 2012..097). This analysis shows that zoledronic acid offered significant protection from clinical fractures as early as 12 months. When administered annually, its beneficial effects persisted for at least 3 years... - Inhibition of cathepsin K for treatment of osteoporosisSteven Boonen
Leuven University Division of Geriatric Medicine and Centre for Metabolic Bone Diseases, UZ Leuven Campus Gasthuisberg, Herestraat 49, B 3000 Leuven, Belgium
Curr Osteoporos Rep 10:73-9. 2012..The usefulness of cathepsin K inhibitors in osteoporosis is now being examined in phase 2 and phase 3 clinical trials of postmenopausal osteoporotic women... - Androgens and skeletal muscle: cellular and molecular action mechanisms underlying the anabolic actionsVanessa Dubois
Molecular Endocrinology Laboratory, Department of Molecular Cell Biology, K U Leuven, Campus Gasthuisberg, O and N1, Herestraat 49, Leuven, Belgium
Cell Mol Life Sci 69:1651-67. 2012..In conclusion, the anabolic effect of androgens on skeletal muscle is not only explained by activation of the myocyte androgen receptor but is also the combined result of many genomic and non-genomic actions... - Squalene synthase, a determinant of Raft-associated cholesterol and modulator of cancer cell proliferationKoen Brusselmans
Laboratory for Experimental Medicine and Endocrinology, Department of Molecular Cell Biology, Katholieke Universiteit Leuven, Herestraat 49, B 3000 Leuven, Belgium
J Biol Chem 282:18777-85. 2007..These findings significantly underscore the importance of de novo cholesterol synthesis for cancer cell biology and suggest that SQS is a potential novel target for antineoplastic intervention... - Selective DNA recognition by the androgen receptor as a mechanism for hormone-specific regulation of gene expressionGuy Verrijdt
Division of Biochemistry, Laboratory of Biochemistry, Catholic University of Leuven, Campus Gasthuisberg O and N, Herestraat 49, B 3000 Leuven, Belgium
Mol Genet Metab 78:175-85. 2003..It creates new possibilities in the research on hormone-selective action and provides a new angle in the search for selective ligands or co-factors that might influence androgen receptor action via either type of DNA motif... - Comparison of different androgen bioassays in the screening for environmental (anti)androgenic activityValerie Christiaens
Division of Biochemistry, Faculty of Medicine, Campus Gasthuisberg, K.U.Leuven, Herestraat 49, B-3000 Leuven, Belgium
Environ Toxicol Chem 24:2646-56. 2005..A number of environmental samples were tested in the bioassay. The bioassay also could be used to detect antiandrogenic activity, because known AR-antagonists were able to inhibit R1881-mediated transactivation... - Androgen receptor (AR) in osteocytes is important for the maintenance of male skeletal integrity: Evidence from targeted AR disruption in mouse osteocytesMieke Sinnesael
Clinical and Experimental Endocrinology, Department of Experimental Medicine, KU Leuven, Leuven, Belgium
J Bone Miner Res 27:2535-43. 2012..These findings provide evidence for a direct role of androgens in the maintenance of trabecular bone through actions of the AR in osteocytes. © 2012 American Society for Bone and Mineral Research... - The hinge region of the androgen receptor plays a role in proteasome-mediated transcriptional activationTamzin Tanner
Biochemistry Division, Laboratory of Molecular Endocrinology, Catholic University of Leuven, Campus Gasthuisberg O and N, Herestraat 49, Leuven, 3000, Belgium
Ann N Y Acad Sci 1030:587-92. 2004.... - Once-yearly zoledronic acid in older men compared with women with recent hip fractureSteven Boonen
Center for Musculoskeletal Research, Leuven University, Leuven, Belgium
J Am Geriatr Soc 59:2084-90. 2011.... - Variations in the exome of the LNCaP prostate cancer cell lineLien Spans
Molecular Endocrinology Laboratory, Department of Molecular Cell Biology, University of Leuven, 3000 Leuven, Belgium
Prostate 72:1317-27. 2012..The LNCaP cell line is widely used as a model for prostate cancer. However, information on protein-changing mutations, genetic heterogeneity and genetic (in)stability is largely lacking for these cells... - Comparative analysis of the influence of the high-mobility group box 1 protein on DNA binding and transcriptional activation by the androgen, glucocorticoid, progesterone and mineralocorticoid receptorsGuy Verrijdt
Division of Biochemistry, Faculty of Medicine, Catholic University of Leuven, Herestraat 49, B-3000 Leuven, Belgium
Biochem J 361:97-103. 2002..This 26-residue fragment is therefore essential for the influence of HMGB1 on DNA recognition by all steroid hormone receptors that were tested. However, it is dispensable for DNA binding by the androgen receptor... - Identification and characterization of MEL-3, a novel AR antagonist that suppresses prostate cancer cell growthChristine Helsen
Laboratory of Molecular Endocrinology, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium
Mol Cancer Ther 11:1257-68. 2012.... - A Sertoli cell-selective knockout of the androgen receptor causes spermatogenic arrest in meiosisKarel De Gendt
Laboratory for Experimental Medicine and Endocrinology, Department of Developmental Biology, Flanders Interuniversity Institute for Biotechnology, Catholic University of Leuven, B 3000 Leuven, Belgium
Proc Natl Acad Sci U S A 101:1327-32. 2004..It is concluded that cell-autonomous action of the AR in SC is an absolute requirement for androgen maintenance of complete spermatogenesis, and that spermatocyte/spermatid development/survival critically depends on androgens... - Influence of bone remodelling rate on quantitative ultrasound parameters at the calcaneus and DXA BMDa of the hip and spine in middle-aged and elderly European men: the European Male Ageing Study (EMAS)Steven Boonen
Division of Geriatric Medicine and Centre for Metabolic Bone Diseases, Katholieke Universiteit Leuven, UZ Leuven Campus Gasthuisberg, Leuven, Belgium
Eur J Endocrinol 165:977-86. 2011..To assess the influence of sex hormones on markers of bone turnover and to explore the association between these markers and bone health in middle-aged and elderly European men... - Superagonistic action of 14-epi-analogs of 1,25-dihydroxyvitamin D explained by vitamin D receptor-coactivator interactionGuy Eelen
Laboratorium voor Experimentele Geneeskunde en Endocrinologie, Katholieke Universiteit Leuven, Belgium
Mol Pharmacol 67:1566-73. 2005..In conclusion, this study provides deeper insight into the docking of TX522 in the LBP and shows that stronger VDR-coactivator interactions underlie the superagonistic activity of the two 14-epi-analogs... - Structural basis of androgen receptor binding to selective androgen response elementsPaul L Shaffer
Department of Biochemistry, Duke University Medical Center, Durham, NC 27710, USA
Proc Natl Acad Sci U S A 101:4758-63. 2004..This increased interfacial stability compared with the other steroid receptors may account for the selective binding of AR to ADR3 response elements... - Targeting the BAF57 SWI/SNF subunit in prostate cancer: a novel platform to control androgen receptor activityKevin A Link
Departments of Cancer Biology and Urology, and Kimmel Cancer Center, Thomas Jefferson University College of Medicine, Philadelphia, Pennsylvania, USA
Cancer Res 68:4551-8. 2008....