Publications

Publications


2020


Blocking sodium-taurocholate cotransporting polypeptide stimulates biliary cholesterol and phospholipid secretion.

Roscam Abbing RLP, Slijepcevic D, Donkers JM, Havinga R, Duijst S, Paulusma CC, Kuiper J, Kuipers F, Groen AK, Oude Elferink RPJ and Van de Graaf SFJ.

Hepatology, 2020 Jan;71(1):247-258. PMID: 31136002




2019


FDA-drug screening identifies deptropine inhibiting hepatitis E virus involving the NF-κB-RIPK1-caspase axis

Qu C, Li Y, Li Y, Yu P, Li P, Donkers JM, Van de Graaf SFJ, de Man RA, Peppelenbosch MP, Pan Q.

Antiviral Res. 2019 Oct;170:104588. PMID: 31415805


Mechanistic insights to the inhibition of NTCP by Myrcludex B

Joanne M. Donkers, Monique D. Appelman and Stan F.J. van de Graaf.

Journal Of Hepatology Reports, 2019 Aug 1;1(4):278-285. PMID: 32039379


NTCP deficiency in mice protects against obesity and hepatosteatosis

Donkers JM, Kooijman S, Slijepcevic D, Kunst R, Roscam Abbing RLP, Haazen L, De Waart DR, Levels JHM, Schoonjans K, Rensen PCN, Oude Elferink RPJ and Van de Graaf SFJ.

CI Insight, 2019. doi: 10.1172/jci.insight.127197. PMID: 31237863


Developments in bile salt based therapies: A critical overview.

Donkers JM, Roscam Abbing RLP, Van de Graaf SFJ. PMID: 30582898

Biochemical Pharmacology. 2019 Mar;161:1-13


Identification of FDA-approved drugs targeting the Farnesoid X Receptor

Van de Wiel SMW, Bijsmans ITGW, Van Mil SWC, Van de Graaf SFJ.

Sci Rep. 2019 Feb 18;9(1):2193. PMID: 30778102




2018


Calnexin depletion by ER-stress during cholestasis inhibits the Na+-taurocholate Cotransporting Polypeptide (NTCP)

Robin MJD, Monique D. Appelman MD, Vos HR, Van Es RM, Paton JC, Paton AW, Burgering B, Fickert P, Heijmans J, Van de Graaf SFJ. Hepatology Communications, 2018 Oct 23;2(12):1550-1566. PMID: 30556041


The case for combining treatments for primary sclerosing cholangitis

Roscam Abbing RLP, de Lannoy LM, van de Graaf SFJ.

Lancet Gastroenterol Hepatol. 2018 Aug;3(8):526-528. PMID: 30047442


Na+ -taurocholate cotransporting polypeptide inhibition has hepatoprotective effects in cholestasis in mice

Slijepcevic D, Roscam Abbing RLP, Fuchs CD, Haazen LCM, Beuers U, Trauner M, Oude Elferink RPJ, Van de Graaf SFJ.

Hepatology. 2018, 68: 3, p.1057-1069. PMID: 29572910


Bioengineered bile ducts recapitulate key cholangiocyte functions

Chen C, Jochems PGM, Salz L, Schneeberger K, Penning LC, van de Graaf SFJ, Beuers U, Clevers H, Geijsen N, Masereeuw R, Spee B.  Biofabrication. 2018 Jun 12;10(3):034103. PMID: 29848792


The somatic FAH C.1061C>A change counteracts the frequent FAH c.1062+5G>A mutation and permits U1snRNA-based splicing correction.

Scalet D, Sacchetto C, Bernardi F, Pinotti M, Van de Graaf SFJ, Balestra D.

J Hum Genet. 2018 May;63(5):683-686. PMID: 29497141


Annexin A11 is targeted by IgG4 and IgG1 autoantibodies in IgG4-related disease

Hubers LM, Vos H, Schuurman AR, Erken R, Oude Elferink RP, Burgering B, van de Graaf SFJ*, Beuers U*.

Gut. 2018 Apr;67(4):728-735. PMID: 28765476


On the role of IgG4 in inflammatory conditions: lessons for IgG4-related disease

Trampert DC, Hubers LM, Van de Graaf SF, Beuers U.

BBA - Molecular Basis of Disease, 2018 Apr;1864(4 Pt B):1401-1409. PMID: 28782655


The NTCP - inhibitor myrcludex B: Effects on bile acid disposition and tenofovir pharmacokinetics

Blank A, Eidam A, Haag M, Hohmann N, Burhenne J, Schwab M, Van de Graaf S, Meyer MR, Maurer HH, Meier K, Weiss J, Bruckner T, Alexandrov A, Urban S, Mikus G, Haefeli WE.

Clin Pharmacol Ther. 2018 Feb;103(2):341-348. PMID: 28543042




2017


Role of the Bile Acid Transporter SLC10A1 in Liver Targeting of the Lipid-Lowering Thyroid Hormone Analog Eprotirome

Kersseboom S, van Gucht ALM, van Mullem A, Brigante G, Farina S, Carlsson B, Donkers JM, van de Graaf SFJ, Peeters RP, Visser TJ.

Endocrinology. 2017 Oct 1;158(10):3307-3318. PMID: 28938430


Biliverdin Reductase inhibitors did not improve severe unconjugated hyperbilirubinemia in vivo

van Dijk R, Aronson SJ, de Waart DR, van de Graaf SF, Duijst S, Seppen J, Elferink RO, Beuers U, Bosma PJ.

Sci Rep. 2017 May 10;7(1):1646. PMID: 28490767


Current and future therapies for inherited cholestatic liver diseases

van der Woerd WL, Houwen RH, van de Graaf SF.

World J Gastroenterol. 2017 Feb 7;23(5):763-775. doi: 10.3748/wjg.v23.i5.763. Review. PMID: 28223721  /  PMCID: 2596193


N-Glycosylation of the Na+-Taurocholate Cotransporting Polypeptide (NTCP) Determines Its Trafficking and Stability and Is Required for Hepatitis B Virus Infection

Appelman MD, Chakraborty A, Protzer U, McKeating JA, van de Graaf SF.

PLoS One. 2017 Jan 26;12(1):e0170419. doi: 10.1371/journal.pone.0170419.  PMID: 28125599


Knockout of the Primary Sclerosing Cholangitis-Risk Gene Fut2 Causes Liver Disease in Mice

Maroni L, Hohenester SD, van de Graaf SF, Tolenaars D, van Lienden K, Verheij J, Marzioni M, Karlsen TH, Oude Elferink RP, Beuers U.

Hepatology. 2017 Jan 5. doi: 10.1002/hep.29029. [Epub ahead of print] PMID: 28056490


Bile Acid Uptake Transporters as Targets for Therapy

Slijepcevic D, van de Graaf SF.

Dig Dis. 2017;35(3):251-258. doi: 10.1159/000450983.  PMID: 28249291


Hepatic uptake of conjugated bile acids is mediated by both NTCP and OATPs and modulated by intestinal sensing of plasma bile acid levels in mice

Slijepcevic D, Roscam Abbing RLP, Katafuchi T, Blank A, Donkers JM, van Hoppe S, de Waart DR, Tolenaars D, van der Meer JHM, Wildenberg M, Beuers U, Oude Elferink RPJ, Schinkel AH, Van de Graaf SF.

Hepatology. 2017 Nov;66(5):1631-1643  (see also Hepatology. 2018 Mar;67(3):1185-1186). PMID: 28498614


Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP

Joanne M. Donkers, Benno Zehnder, Gerard J. P. van Westen, Mark J. Kwakkenbos,Adriaan P. IJzerman, Ronald P. J. Oude Elferink, Ulrich Beuers, Stephan Urban & Stan F. J. van de Graaf

Scientific Reports | 7: 15307 | DOI:10.1038/s41598-017-15338-0. PMID: 29127322


Intestinal FXR activation by pharmacological inhibition of the organic solute transporter α-β

Sandra M.W. van de Wiel, D. Rudi de Waart, Ronald P.J. Oude Elferink and Stan F.J. van de Graaf.

Cellular and Molecular Gastroenterology and Hepatology, 2017 Nov 28;5(3):223-237. PMID: 29675448 / PMCID: 5904037




2016


Immunoglobulin G4+ B-cell receptor clones distinguish immunoglobulin G 4-related disease from primary sclerosing cholangitis and biliary/pancreatic malignancies

Doorenspleet ME, Hubers LM, Culver EL, Maillette de Buy Wenniger LJ, Klarenbeek PL, Chapman RW, Baas F, van de Graaf SF, Verheij J, van Gulik TM, Barnes E, Beuers U, de Vries N.

Hepatology. 2016;64(2):501-7. doi: 10.1002/hep.28568. PMID: 27015613


Rescue of defective ATP8B1 trafficking by CFTR correctors as a therapeutic strategy for familial intrahepatic cholestasis

Van der Woerd WL, Wichers CG, Vestergaard AL, Andersen JP, Paulusma CC, Houwen RH, van de Graaf SF.

J Hepatol. 2016;64(6):1339-47. doi: 10.1016/j.jhep.2016.02.001. PMID: 26879107


Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor

Sandra Van de Wiel, Maarten Merkx and Stan van de Graaf

Journal of Visualized Experiments, JoVE (http://www.jove.com/video/53659)




2015


ATP8B1-mediated spatial organization of Cdc42 signaling maintains singularity during enterocyte polarization.

Bruurs LJ, Donker L, Zwakenberg S, Zwartkruis FJ, Begthel H, Knisely AS, Posthuma G, van de Graaf SF, Paulusma CC, Bos JL.

J Cell Biol. 2015 Sep 28;210(7):1055-63. PMID: 26416959


Impaired uptake of conjugated bile acids and hepatitis b virus pres1-binding in Na(+) -taurocholate cotransporting polypeptide knockout mice

Slijepcevic D, Kaufman C, Wichers CG, Gilglioni EH, Lempp FA, Duijst S, de Waart DR, Oude Elferink RP, Mier W, Stieger B, Beuers U, Urban S, Van de Graaf SF.

Hepatology. 2015 Jul;62(1):207-19] PubMed PMID: 25641256.


Analysis of aberrant pre-messenger RNA splicing resulting from mutations in ATP8B1 and efficient in vitro rescue by adapted U1 small nuclear RNA

Van der Woerd WL, Mulder J, Pagani F, Beuers U, Houwen RH, Van de Graaf SF.

Hepatology. 2015 Apr;61(4):1382-91. doi: 10.1002/hep.27620. Epub 2015 Feb 23. PubMed PMID: 25421123.


IgG4-Associated Cholangitis: A Comprehensive Review

Hubers LM, Maillette de Buy Wenniger LJ, Doorenspleet ME, Klarenbeek PL, Verheij J, Rauws EA, Van Gulik TM, Oude Elferink RP, Van de Graaf SF, de Vries N, Beuers U.

Clin Rev Allergy Immunol. 2015 Jun;48(2-3):198-206. doi: 10.1007/s12016-014-8430-2. PubMed PMID: 24958363


Fucosyltransferase 2: a genetic risk factor for primary sclerosing cholangitis and Crohn's disease-a comprehensive review

Maroni L, Van de Graaf SF, Hohenester SD, Oude Elferink RP, Beuers U. .

Clin Rev Allergy Immunol. 2015 Jun;48(2-3):182-91. doi: 10.1007/s12016-014-8423-1. PubMed PMID: 24828903.




2014


Quantifying stickiness: thermodynamic characterization of intramolecular domain interactions to guide the design of förster resonance energy transfer sensors

Lindenburg LH, Malisauskas M, Sips T, Van Oppen L, Wijnands SP, Van de Graaf SF, Merkx M.

Biochemistry. 2014 Oct 14;53(40):6370-81. doi: 10.1021/bi500433j. Epub 2014 Sep 26. PubMed PMID: 25216081


IgG4-associated cholangitis

Beuers U, Maillette de Buy Wenniger LJ, Doorenspleet M, Hubers L, Verheij J, Van Gulik T, Van de Graaf SF, de Vries N. 

Dig Dis. 2014;32(5):605-8. doi: 10.1159/000360513. Epub 2014 Jul 14. Review. PubMed PMID: 25034294


Autophagy - another piece of the puzzle towards understanding primary biliary cirrhosis?

Van de Graaf S, Beuers U.

Liver Int. 2014 Apr;34(4):481-3. doi: 10.1111/liv.12357. No abstract available.  PMID:  24612169




2013


Mutational analysis of ATP8B1 in patients with chronic pancreatitis

Van der Woerd WL, Van Haaften-Visser DY, Van de Graaf SF, Férec C, Masson E, Stapelbroek JM, Bugert P, Witt H, Houwen RH.

PLoS One. 2013 Nov 19;8(11):e80553. doi: 10.1371/journal.pone.0080553. eCollection 2013. PubMed PMID: 24260417; PubMed Central PMCID: PMC3834041.


Early adipogenesis is regulated through USP7-mediated deubiquitination of the histone acetyltransferase TIP60

Gao Y, Koppen A, Rakhshandehroo M, Tasdelen I, Van de Graaf SF, Van Loosdregt  J, Van Beekum O, Hamers N, Van Leenen D, Berkers CR, Berger R, Holstege FC, Coffer PJ, Brenkman AB, Ovaa H, Kalkhoven E.

Nat Commun. 2013;4:2656. doi: 10.1038/ncomms3656. PubMed PMID: 24141283


Monitoring bile acid transport in single living cells using a genetically encoded Förster resonance energy transfer sensor

Van der Velden LM, Golynskiy MV, Bijsmans IT, Van Mil SW, Klomp LW, Merkx M, Van de Graaf SF.

Hepatology. 2013 Feb;57(2):740-52. doi: 10.1002/hep.26012. Epub 2013 Jan 8. PubMed PMID: 22899095




2012


Natural killer T cells in adipose tissue prevent insulin resistance

Schipper HS, Rakhshandehroo M, Van de Graaf SF, Venken K, Koppen A, Stienstra R, Prop S, Meerding J, Hamers N, Besra G, Boon L, Nieuwenhuis EE, Elewaut D, Prakken B, Kersten S, Boes M, Kalkhoven E.

J Clin Invest. 2012 Sep;122(9):3343-54. doi: 10.1172/JCI62739. Epub 2012 Aug 6. PubMed PMID: 22863618; PubMed Central PMCID:

PMC3428087.


Homo- and hetero-dimeric architecture of the human liver Na⁺-dependent taurocholate co-transporting protein

Bijsmans IT, Bouwmeester RA, Geyer J, Faber KN, Van de Graaf SF.

Biochem J. 2012 Feb 1;441(3):1007-15. doi: 10.1042/BJ20111234. PubMed PMID: 22029531




2010


Familial cholestasis: progressive familial intrahepatic cholestasis, benign recurrent intrahepatic cholestasis and intrahepatic cholestasis of pregnancy

Van der Woerd WL, Van Mil SW, Stapelbroek JM, Klomp LW, Van de Graaf SF, Houwen RH. 

Best Pract Res Clin Gastroenterol. 2010 Oct;24(5):541-53. doi: 10.1016/j.bpg.2010.07.010. Review. PubMed PMID: 20955958


Heteromeric interactions required for abundance and subcellular localization of human CDC50 proteins and class 1 P4-ATPases

Van der Velden LM, Wichers CG, Van Breevoort AE, Coleman JA, Molday RS, Berger R, Klomp LW, Van de Graaf SF.

J Biol Chem. 2010 Dec 17;285(51):40088-96. doi: 10.1074/jbc.M110.139006. Epub 2010 Oct 14. PubMed PMID: 20947505; PubMed Central PMCID: PMC3000991.


Biochemical and cellular functions of P4 ATPases

Van der Velden LM, Van de Graaf SF, Klomp LW.

Biochem J. 2010 Oct 1;431(1):1-11. doi: 10.1042/BJ20100644. Review. PubMed PMID: 20836764


Folding defects in P-type ATP 8B1 associated with hereditary cholestasis are ameliorated by 4-phenylbutyrate

Van der Velden LM, Stapelbroek JM, Krieger E, Van den Berghe PV, Berger R, Verhulst PM, Holthuis JC, Houwen RH, Klomp LW, Van de Graaf SF.

Hepatology. 2010 Jan;51(1):286-96. doi: 10.1002/hep.23268. PubMed PMID: 19918981




2009


Reduced expression of ATP7B affected by Wilson disease-causing mutations is rescued by pharmacological folding chaperones 4-phenylbutyrate and curcumin

Van den Berghe PV, Stapelbroek JM, Krieger E, de Bie P, Van de Graaf SF, de Groot RE, Van Beurden E, Spijker E, Houwen RH, Berger R, Klomp LW.

Hepatology. 2009 Dec;50(6):1783-95. doi: 10.1002/hep.23209. PubMed PMID: 19937698


Conditional fast expression and function of multimeric TRPV5 channels using Shield-1

Schoeber JP, Van de Graaf SF, Lee KP, Wittgen HG, Hoenderop JG, Bindels RJ.

Am J Physiol Renal Physiol. 2009 Jan;296(1):F204-11. doi: 10.1152/ajprenal.90473.2008. Epub 2008 Oct 8. PubMed PMID: 18842822




2008 and before


Van de Graaf SF, Rescher U, Hoenderop JG, Verkaart S, Bindels RJ, Gerke V. TRPV5 is internalized via clathrin-dependent endocytosis to enter a Ca2+-controlled recycling pathway. J Biol Chem. 2008 Feb 15;283(7):4077-86. Epub  2007 Dec 12. PubMed PMID: 18077461.


Van de Graaf SF, Bindels RJ, Hoenderop JG. Physiology of epithelial Ca2+ and  Mg2+ transport. Rev Physiol Biochem Pharmacol. 2007;158:77-160. Review. PubMed PMID: 17729442.



Van de Graaf SF, Hoenderop JG, Bindels RJ. Regulation of TRPV5 and TRPV6 by associated proteins. Am J Physiol Renal Physiol. 2006 Jun;290(6):F1295-302. Review. PubMed PMID: 16682485.


Van de Graaf SF, Hoenderop JG, Van der Kemp AW, Gisler SM, Bindels RJ. Interaction of the epithelial Ca2+ channels TRPV5 and TRPV6 with the intestine-and kidney-enriched PDZ protein NHERF4. Pflugers Arch. 2006 Jul;452(4):407-17. Epub 2006 Mar 25. PubMed PMID: 16565876.


Van de Graaf SF, Van der Kemp AW, Van den Berg D, Van Oorschot M, HoenderopJG, Bindels RJ. Identification of BSPRY as a novel auxiliary protein inhibiting TRPV5 activity. J Am Soc Nephrol. 2006 Jan;17(1):26-30. PubMed PMID: 16380433.


Van de Graaf SF, Chang Q, Mensenkamp AR, Hoenderop JG, Bindels RJ. Direct interaction with Rab11a targets the epithelial Ca2+ channels TRPV5 and TRPV6 to the plasma membrane. Mol Cell Biol. 2006 Jan;26(1):303-12. PubMed PMID: 16354700; PubMed Central PMCID: PMC1317621.


den Dekker E, Schoeber J, Topala CN, Van de Graaf SF, Hoenderop JG, Bindels RJ. Characterization of a Madin-Darby canine kidney cell line stably expressing TRPV5. Pflugers Arch. 2005 Jul;450(4):236-44. Epub 2005 May 28. PubMed PMID: 15924239.


Palmada M, Poppendieck S, Embark HM, Van de Graaf SF, Boehmer C, Bindels RJ, Lang F. Requirement of PDZ domains for the stimulation of the epithelial Ca2+ channel TRPV5 by the NHE regulating factor NHERF2 and the serum and glucocorticoid inducible kinase SGK1. Cell Physiol Biochem. 2005;15(1-4):175-82. PubMed PMID: 15665527.


Chang Q, Gyftogianni E, Van de Graaf SF, Hoefs S, Weidema FA, Bindels RJ, Hoenderop JG. Molecular determinants in TRPV5 channel assembly. J Biol Chem. 2004 Dec 24;279(52):54304-11. Epub 2004 Oct 15. PubMed PMID: 15489237.


Embark HM, Setiawan I, Poppendieck S, Van de Graaf SF, Boehmer C, Palmada M, Wieder T, Gerstberger R, Cohen P, Yun CC, Bindels RJ, Lang F. Regulation of the epithelial Ca2+ channel TRPV5 by the NHE regulating factor NHERF2 and the serum and glucocorticoid inducible kinase isoforms SGK1 and SGK3 expressed in Xenopus oocytes. Cell Physiol Biochem. 2004;14(4-6):203-12. PubMed PMID: 15319523.


Van de Graaf SF, Boullart I, Hoenderop JG, Bindels RJ. Regulation of the epithelial Ca2+ channels TRPV5 and TRPV6 by 1alpha,25-dihydroxy Vitamin D3 and dietary Ca2+. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):303-8. Review. PubMed PMID: 15225790.


Van de Graaf SF, Hoenderop JG, Gkika D, Lamers D, Prenen J, Rescher U, Gerke  V, Staub O, Nilius B, Bindels RJ. Functional expression of the epithelial Ca2+ channels (TRPV5 and TRPV6) requires association of the S100A10-annexin 2 complex. EMBO J. 2003 Apr 1;22(7):1478-87. PubMed PMID: 12660155; PubMed Central PMCID: PMC152906.


Danahay H, Withey L, Poll CT, Van de Graaf SF, Bridges RJ. Protease-activated receptor-2-mediated inhibition of ion transport in human bronchial epithelial cells. Am J Physiol Cell Physiol. 2001 Jun;280(6):C1455-64. PubMed PMID:11350741.


Hoenderop JG, Van der Kemp AW, Hartog A, Van de Graaf SF, Van Os CH, Willems PH, Bindels RJ. Molecular identification of the apical Ca2+ channel in 1,25-dihydroxyvitamin D3-responsive epithelia. J Biol Chem. 1999 Mar26;274(13):8375-8. PubMed PMID: 10085067.