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Items: 1 to 50 of 71

1.

Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.

Abdelsamie AS, Salah M, Siebenbürger L, Merabet A, Scheuer C, Frotscher M, Müller ST, Zierau O, Vollmer G, Menger MD, Laschke MW, van Koppen CJ, Marchais-Oberwinkler S, Hartmann RW.

J Med Chem. 2019 Aug 8;62(15):7289-7301. doi: 10.1021/acs.jmedchem.9b00932. Epub 2019 Jul 25.

PMID:
31343176
2.

Effects of 17β-HSD2 inhibition in bones on osteoporosis based on an animal rat model.

Müller ST, Pählig S, Merabet A, Abdelsamie AS, van Koppen CJ, Marchais-Oberwinkler S, Hartmann RW, Zierau O, Vollmer G.

J Steroid Biochem Mol Biol. 2019 Sep;192:105405. doi: 10.1016/j.jsbmb.2019.105405. Epub 2019 Jun 8.

PMID:
31185280
3.

Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17β-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.

Abdelsamie AS, Salah M, Siebenbürger L, Hamed MM, Börger C, van Koppen CJ, Frotscher M, Hartmann RW.

Eur J Med Chem. 2019 Sep 15;178:93-107. doi: 10.1016/j.ejmech.2019.05.084. Epub 2019 May 31.

PMID:
31176098
4.

Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.

Abdelsamie AS, Herath S, Biskupek Y, Börger C, Siebenbürger L, Salah M, Scheuer C, Marchais-Oberwinkler S, Frotscher M, Pohlemann T, Menger MD, Hartmann RW, Laschke MW, van Koppen CJ.

J Med Chem. 2019 Feb 14;62(3):1362-1372. doi: 10.1021/acs.jmedchem.8b01493. Epub 2019 Jan 15.

PMID:
30645111
5.

Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy.

Siebenbuerger L, Hernandez-Olmos V, Abdelsamie AS, Frotscher M, van Koppen CJ, Marchais-Oberwinkler S, Scheuer C, Laschke MW, Menger MD, Boerger C, Hartmann RW.

J Med Chem. 2018 Dec 13;61(23):10724-10738. doi: 10.1021/acs.jmedchem.8b01373. Epub 2018 Nov 27.

PMID:
30480443
6.

Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors.

Emmerich J, van Koppen CJ, Burkhart JL, Engeli RT, Hu Q, Odermatt A, Hartmann RW.

Eur J Med Chem. 2018 Jan 1;143:591-597. doi: 10.1016/j.ejmech.2017.11.018. Epub 2017 Nov 21.

PMID:
29207342
7.

Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.

Emmerich J, van Koppen CJ, Burkhart JL, Hu Q, Siebenbürger L, Boerger C, Scheuer C, Laschke MW, Menger MD, Hartmann RW.

J Med Chem. 2017 Jun 22;60(12):5086-5098. doi: 10.1021/acs.jmedchem.7b00437. Epub 2017 Jun 9.

PMID:
28570067
8.

First Structure-Activity Relationship of 17β-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme.

Braun F, Bertoletti N, Möller G, Adamski J, Steinmetzer T, Salah M, Abdelsamie AS, van Koppen CJ, Heine A, Klebe G, Marchais-Oberwinkler S.

J Med Chem. 2016 Dec 8;59(23):10719-10737. Epub 2016 Nov 18.

PMID:
27933965
9.

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study.

Abdelsamie AS, van Koppen CJ, Bey E, Salah M, Börger C, Siebenbürger L, Laschke MW, Menger MD, Frotscher M.

Eur J Med Chem. 2017 Feb 15;127:944-957. doi: 10.1016/j.ejmech.2016.11.004. Epub 2016 Nov 4.

PMID:
27852458
10.

Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.

Abdelsamie AS, Bey E, Gargano EM, van Koppen CJ, Empting M, Frotscher M.

Eur J Med Chem. 2015 Oct 20;103:56-68. doi: 10.1016/j.ejmech.2015.08.030. Epub 2015 Aug 18.

PMID:
26322835
11.

Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Hoyt SB, Petrilli W, London C, Liang GB, Tata J, Hu Q, Yin L, van Koppen CJ, Hartmann RW, Struthers M, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Xiong Y.

ACS Med Chem Lett. 2015 Jul 17;6(8):861-5. doi: 10.1021/acsmedchemlett.5b00048. eCollection 2015 Aug 13.

12.

Advances in the treatment of chronic wounds: a patent review.

van Koppen CJ, Hartmann RW.

Expert Opin Ther Pat. 2015;25(8):931-7. doi: 10.1517/13543776.2015.1045879. Epub 2015 Jun 3. Review.

PMID:
26039457
13.

Potent 11β-hydroxylase inhibitors with inverse metabolic stability in human plasma and hepatic S9 fractions to promote wound healing.

Zhu W, Hu Q, Hanke N, van Koppen CJ, Hartmann RW.

J Med Chem. 2014 Sep 25;57(18):7811-7. doi: 10.1021/jm501004t. Epub 2014 Sep 8.

PMID:
25176013
14.

Signaling of an allosteric, nanomolar potent, low molecular weight agonist for the follicle-stimulating hormone receptor.

van Koppen CJ, Verbost PM, van de Lagemaat R, Karstens WJ, Loozen HJ, van Achterberg TA, van Amstel MG, Brands JH, van Doornmalen EJ, Wat J, Mulder SJ, Raafs BC, Verkaik S, Hanssen RG, Timmers CM.

Biochem Pharmacol. 2013 Apr 15;85(8):1162-70. doi: 10.1016/j.bcp.2013.02.001. Epub 2013 Feb 13.

PMID:
23415902
15.

Complete inhibition of rhTSH-, Graves' disease IgG-, and M22-induced cAMP production in differentiated orbital fibroblasts by a low-molecular-weight TSHR antagonist.

van Zeijl CJ, van Koppen CJ, Surovtseva OV, de Gooyer ME, Plate R, Conti P, Karstens WJ, Timmers M, Saeed P, Wiersinga WM, Miltenburg AM, Fliers E, Boelen A.

J Clin Endocrinol Metab. 2012 May;97(5):E781-5. doi: 10.1210/jc.2011-2931. Epub 2012 Mar 14.

PMID:
22419705
16.

Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor.

van Koppen CJ, de Gooyer ME, Karstens WJ, Plate R, Conti PG, van Achterberg TA, van Amstel MG, Brands JH, Wat J, Berg RJ, Lane JR, Miltenburg AM, Timmers CM.

Br J Pharmacol. 2012 Apr;165(7):2314-24. doi: 10.1111/j.1476-5381.2011.01709.x.

17.

Contraception by induction of luteinized unruptured follicles with short-acting low molecular weight FSH receptor agonists in female animal models.

van de Lagemaat R, van Koppen CJ, Krajnc-Franken MA, Folmer BJ, van Diepen HA, Mulders SM, Timmers CM.

Reproduction. 2011 Dec;142(6):893-905. doi: 10.1530/REP-11-0234. Epub 2011 Sep 19.

PMID:
21930683
18.

Rescue of expression and signaling of human luteinizing hormone G protein-coupled receptor mutants with an allosterically binding small-molecule agonist.

Newton CL, Whay AM, McArdle CA, Zhang M, van Koppen CJ, van de Lagemaat R, Segaloff DL, Millar RP.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):7172-6. doi: 10.1073/pnas.1015723108. Epub 2011 Apr 11.

19.

Development of Selective LH Receptor Agonists by Heterodimerization with a FSH Receptor Antagonist.

Bonger KM, Hoogendoorn S, van Koppen CJ, Timmers CM, van der Marel GA, Overkleeft HS.

ACS Med Chem Lett. 2010 Nov 8;2(1):85-9. doi: 10.1021/ml100229v. eCollection 2011 Jan 13.

20.

Thyrotropin receptor-stimulating Graves' disease immunoglobulins induce hyaluronan synthesis by differentiated orbital fibroblasts from patients with Graves' ophthalmopathy not only via cyclic adenosine monophosphate signaling pathways.

van Zeijl CJ, Fliers E, van Koppen CJ, Surovtseva OV, de Gooyer ME, Mourits MP, Wiersinga WM, Miltenburg AM, Boelen A.

Thyroid. 2011 Feb;21(2):169-76. doi: 10.1089/thy.2010.0123. Epub 2010 Oct 18.

PMID:
20954819
21.

Oligoproline helices as structurally defined scaffolds for oligomeric G protein-coupled receptor ligands.

Bonger KM, Kapoerchan VV, Grotenbreg GM, van Koppen CJ, Timmers CM, van der Marel GA, Overkleeft HS.

Org Biomol Chem. 2010 Apr 21;8(8):1881-4. doi: 10.1039/b923556f.

PMID:
20449493
22.

Effects of thyrotropin and thyrotropin-receptor-stimulating Graves' disease immunoglobulin G on cyclic adenosine monophosphate and hyaluronan production in nondifferentiated orbital fibroblasts of Graves' ophthalmopathy patients.

van Zeijl CJ, Fliers E, van Koppen CJ, Surovtseva OV, de Gooyer ME, Mourits MP, Wiersinga WM, Miltenburg AM, Boelen A.

Thyroid. 2010 May;20(5):535-44. doi: 10.1089/thy.2009.0447.

PMID:
20384487
23.

Synthesis and pharmacological evaluation of dimeric follicle-stimulating hormone receptor antagonists.

Bonger KM, Hoogendoorn S, van Koppen CJ, Timmers CM, Overkleeft HS, van der Marel GA.

ChemMedChem. 2009 Dec;4(12):2098-102. doi: 10.1002/cmdc.200900344.

PMID:
19902448
24.

Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1.

van der Lee MM, Blomenröhr M, van der Doelen AA, Wat JW, Smits N, Hanson BJ, van Koppen CJ, Zaman GJ.

J Biomol Screen. 2009 Aug;14(7):811-23. doi: 10.1177/1087057109337937. Epub 2009 Jun 11.

PMID:
19520790
25.

Discovery of selective luteinizing hormone receptor agonists using the bivalent ligand method.

Bonger KM, van den Berg RJ, Knijnenburg AD, Heitman LH, van Koppen CJ, Timmers CM, Overkleeft HS, van der Marel GA.

ChemMedChem. 2009 Jul;4(7):1189-95. doi: 10.1002/cmdc.200900058.

PMID:
19475639
26.

beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1.

van Der Lee MM, Bras M, van Koppen CJ, Zaman GJ.

J Biomol Screen. 2008 Dec;13(10):986-98. doi: 10.1177/1087057108326144. Epub 2008 Nov 25.

PMID:
19036707
27.

G protein-independent cell-based assays for drug discovery on seven-transmembrane receptors.

Verkaar F, van Rosmalen JW, Blomenröhr M, van Koppen CJ, Blankesteijn WM, Smits JF, Zaman GJ.

Biotechnol Annu Rev. 2008;14:253-74. doi: 10.1016/S1387-2656(08)00010-0. Review.

PMID:
18606367
28.

A signaling-selective, nanomolar potent allosteric low molecular weight agonist for the human luteinizing hormone receptor.

van Koppen CJ, Zaman GJ, Timmers CM, Kelder J, Mosselman S, van de Lagemaat R, Smit MJ, Hanssen RG.

Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378(5):503-14. doi: 10.1007/s00210-008-0318-3. Epub 2008 Jun 13.

PMID:
18551279
29.

Cryopreserved cells facilitate cell-based drug discovery.

Zaman GJ, de Roos JA, Blomenröhr M, van Koppen CJ, Oosterom J.

Drug Discov Today. 2007 Jul;12(13-14):521-6. Epub 2007 Jun 27. Review.

PMID:
17631245
30.

Regulation and functional roles of sphingosine kinases.

Alemany R, van Koppen CJ, Danneberg K, Ter Braak M, Meyer Zu Heringdorf D.

Naunyn Schmiedebergs Arch Pharmacol. 2007 Feb;374(5-6):413-28. Epub 2007 Jan 23. Review.

PMID:
17242884
31.

Arrestin-independent internalization of G protein-coupled receptors.

van Koppen CJ, Jakobs KH.

Mol Pharmacol. 2004 Sep;66(3):365-7. No abstract available.

PMID:
15322226
32.

Regulation of muscarinic acetylcholine receptor signaling.

van Koppen CJ, Kaiser B.

Pharmacol Ther. 2003 May;98(2):197-220. Review.

PMID:
12725869
33.

Muscarinic receptors in the mammalian heart.

Dhein S, van Koppen CJ, Brodde OE.

Pharmacol Res. 2001 Sep;44(3):161-82. Review.

PMID:
11529684
34.

Multiple pathways for the dynamin-regulated internalization of muscarinic acetylcholine receptors.

van Koppen CJ.

Biochem Soc Trans. 2001 Aug;29(Pt 4):505-8. Review.

PMID:
11498018
35.

Sphingosine kinase-mediated calcium signaling by muscarinic acetylcholine receptors.

van Koppen CJ, Meyer zu Heringdorf D, Alemany R, Jakobs KH.

Life Sci. 2001 Apr 27;68(22-23):2535-40.

PMID:
11392623
36.
37.

Essential role of dynamin in internalization of M2 muscarinic acetylcholine and angiotensin AT1A receptors.

Werbonat Y, Kleutges N, Jakobs KH, van Koppen CJ.

J Biol Chem. 2000 Jul 21;275(29):21969-74.

38.

Distinct internalization of M2 muscarinic acetylcholine receptors confers selective and long-lasting desensitization of signaling to phospholipase C.

Krudewig R, Langer B, Vögler O, Markschies N, Erl M, Jakobs KH, van Koppen CJ.

J Neurochem. 2000 Apr;74(4):1721-30.

39.

Regulation of muscarinic acetylcholine receptor sequestration and function by beta-arrestin.

Vögler O, Nolte B, Voss M, Schmidt M, Jakobs KH, van Koppen CJ.

J Biol Chem. 1999 Apr 30;274(18):12333-8.

40.

Formyl peptide receptor signaling in HL-60 cells through sphingosine kinase.

Alemany R, Meyer zu Heringdorf D, van Koppen CJ, Jakobs KH.

J Biol Chem. 1999 Feb 12;274(7):3994-9.

41.

RhoA-sensitive trafficking of muscarinic acetylcholine receptors.

Vögler O, Krummenerl P, Schmidt M, Jakobs KH, Van Koppen CJ.

J Pharmacol Exp Ther. 1999 Jan;288(1):36-42.

PMID:
9862750
42.

Discrimination between plasma membrane and intracellular target sites of sphingosylphosphorylcholine.

Meyer zu Heringdorf D, Niederdräing N, Neumann E, Fröde R, Lass H, Van Koppen CJ, Jakobs KH.

Eur J Pharmacol. 1998 Jul 31;354(1):113-22.

PMID:
9726638
43.

Guanine nucleotide-sensitive inhibition of L-type Ca2+ current by lysosphingolipids in RINm5F insulinoma cells.

Himmel HM, Meyer zu Heringdorf D, Windorfer B, van Koppen CJ, Ravens U, Jakobs KH.

Mol Pharmacol. 1998 May;53(5):862-9.

PMID:
9584212
44.

Receptor subtype-specific regulation of muscarinic acetylcholine receptor sequestration by dynamin. Distinct sequestration of m2 receptors.

Vögler O, Bogatkewitsch GS, Wriske C, Krummenerl P, Jakobs KH, van Koppen CJ.

J Biol Chem. 1998 May 15;273(20):12155-60.

45.

Sphingosine kinase-mediated Ca2+ signalling by G-protein-coupled receptors.

Meyer zu Heringdorf D, Lass H, Alemany R, Laser KT, Neumann E, Zhang C, Schmidt M, Rauen U, Jakobs KH, van Koppen CJ.

EMBO J. 1998 May 15;17(10):2830-7.

46.

Molecular diversity of sphingolipid signalling.

Meyer zu Heringdorf D, van Koppen CJ, Jakobs KH.

FEBS Lett. 1997 Jun 23;410(1):34-8. Review.

47.

Calcium signalling by G protein-coupled sphingolipid receptors in bovine aortic endothelial cells.

Meyer zu Heringdrof D, van Koppen CJ, Windorfer B, Himmel HM, Jakobs KH.

Naunyn Schmiedebergs Arch Pharmacol. 1996 Oct;354(4):397-403.

PMID:
8897440
48.

Receptor internalization delays m4 muscarinic acetylcholine receptor resensitization at the plasma membrane.

Bogatkewitsch GS, Lenz W, Jakobs KH, Van Koppen CJ.

Mol Pharmacol. 1996 Aug;50(2):424-9.

PMID:
8700152
49.

Muscarinic acetylcholine receptor trafficking in streptolysin O-permeabilized MDCK cells.

Vogt S, Vögler O, Zhang C, Weller U, Jakobs KH, van Koppen CJ.

Naunyn Schmiedebergs Arch Pharmacol. 1996 Jul;354(2):128-35.

PMID:
8857589
50.

A distinct G(i) protein-coupled receptor for sphingosylphosphorylcholine in human leukemia HL-60 cells and human neutrophils.

Van Koppen CJ, Meyer Zu Heringdorf D, Zhang C, Laser KT, Jakobs KH.

Mol Pharmacol. 1996 Jun;49(6):956-61.

PMID:
8649355

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