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Items: 29

1.

Structure-based and property-driven optimization of N-aryl imidazoles towards potent and selective oral RORγt inhibitors.

Hoegenauer K, Kallen J, Jimenez-Nunez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, Mckay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C.

J Med Chem. 2019 Nov 15. doi: 10.1021/acs.jmedchem.9b01291. [Epub ahead of print]

PMID:
31729873
2.

Nanoscale polarization of the entry fusion complex of vaccinia virus drives efficient fusion.

Gray RDM, Albrecht D, Beerli C, Huttunen M, Cohen GH, White IJ, Burden JJ, Henriques R, Mercer J.

Nat Microbiol. 2019 Oct;4(10):1636-1644. doi: 10.1038/s41564-019-0488-4. Epub 2019 Jul 8.

PMID:
31285583
3.

Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility.

Beerli C, Yakimovich A, Kilcher S, Reynoso GV, Fläschner G, Müller DJ, Hickman HD, Mercer J.

Nat Microbiol. 2019 Feb;4(2):216-225. doi: 10.1038/s41564-018-0288-2. Epub 2018 Nov 12.

4.

Proteotype profiling unmasks a viral signalling network essential for poxvirus assembly and transcriptional competence.

Novy K, Kilcher S, Omasits U, Bleck CKE, Beerli C, Vowinckel J, Martin CK, Syedbasha M, Maiolica A, White I, Mercer J, Wollscheid B.

Nat Microbiol. 2018 May;3(5):588-599. doi: 10.1038/s41564-018-0142-6. Epub 2018 Apr 9.

PMID:
29632367
5.

Inertial picobalance reveals fast mass fluctuations in mammalian cells.

Martínez-Martín D, Fläschner G, Gaub B, Martin S, Newton R, Beerli C, Mercer J, Gerber C, Müller DJ.

Nature. 2017 Oct 25;550(7677):500-505. doi: 10.1038/nature24288.

PMID:
29072271
6.

Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism.

Bigaud M, Dincer Z, Bollbuck B, Dawson J, Beckmann N, Beerli C, Fishli-Cavelti G, Nahler M, Angst D, Janser P, Otto H, Rosner E, Hersperger R, Bruns C, Quancard J.

PLoS One. 2016 Dec 22;11(12):e0168252. doi: 10.1371/journal.pone.0168252. eCollection 2016.

7.

Neutral sphingomyelinase-2, acid sphingomyelinase, and ceramide levels in COPD patients compared to controls.

Lea SR, Metcalfe HJ, Plumb J, Beerli C, Poll C, Singh D, Abbott-Banner KH.

Int J Chron Obstruct Pulmon Dis. 2016 Sep 6;11:2139-2147. eCollection 2016.

8.

VirusMapper: open-source nanoscale mapping of viral architecture through super-resolution microscopy.

Gray RD, Beerli C, Pereira PM, Scherer KM, Samolej J, Bleck CK, Mercer J, Henriques R.

Sci Rep. 2016 Jul 4;6:29132. doi: 10.1038/srep29132.

9.

Sphingosine 1-Phosphate Produced by Sphingosine Kinase 2 Intrinsically Controls Platelet Aggregation In Vitro and In Vivo.

Urtz N, Gaertner F, von Bruehl ML, Chandraratne S, Rahimi F, Zhang L, Orban M, Barocke V, Beil J, Schubert I, Lorenz M, Legate KR, Huwiler A, Pfeilschifter JM, Beerli C, Ledieu D, Persohn E, Billich A, Baumruker T, Mederos y Schnitzler M, Massberg S.

Circ Res. 2015 Jul 31;117(4):376-87. doi: 10.1161/CIRCRESAHA.115.306901. Epub 2015 Jun 30.

PMID:
26129975
10.

Reduced Activity of Sphingosine-1-Phosphate Lyase Induces Podocyte-related Glomerular Proteinuria, Skin Irritation, and Platelet Activation.

Schümann J, Grevot A, Ledieu D, Wolf A, Schubart A, Piaia A, Sutter E, Côté S, Beerli C, Pognan F, Billich A, Moulin P, Walker UJ.

Toxicol Pathol. 2015 Jul;43(5):694-703. doi: 10.1177/0192623314565650. Epub 2015 Jan 27.

PMID:
25630683
11.

Orally active 7-substituted (4-benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitriles as active-site inhibitors of sphingosine 1-phosphate lyase for the treatment of multiple sclerosis.

Weiler S, Braendlin N, Beerli C, Bergsdorf C, Schubart A, Srinivas H, Oberhauser B, Billich A.

J Med Chem. 2014 Jun 26;57(12):5074-84. doi: 10.1021/jm500338n. Epub 2014 May 21.

PMID:
24809814
12.

Pharmacokinetics, biocompatibility and bioavailability of a controlled release monoclonal antibody formulation.

Schweizer D, Vostiar I, Heier A, Serno T, Schoenhammer K, Jahn M, Jones S, Piequet A, Beerli C, Gram H, Goepferich A.

J Control Release. 2013 Dec 28;172(3):975-82. doi: 10.1016/j.jconrel.2013.10.010. Epub 2013 Oct 15.

PMID:
24140353
13.

Partial deficiency of sphingosine-1-phosphate lyase confers protection in experimental autoimmune encephalomyelitis.

Billich A, Baumruker T, Beerli C, Bigaud M, Bruns C, Calzascia T, Isken A, Kinzel B, Loetscher E, Metzler B, Mueller M, Nuesslein-Hildesheim B, Kleylein-Sohn B.

PLoS One. 2013;8(3):e59630. doi: 10.1371/journal.pone.0059630. Epub 2013 Mar 27.

14.

Assay to measure the secretion of sphingosine-1-phosphate from cells induced by S1P lyase inhibitors.

Loetscher E, Schneider K, Beerli C, Billich A.

Biochem Biophys Res Commun. 2013 Apr 12;433(3):345-8. doi: 10.1016/j.bbrc.2013.03.004. Epub 2013 Mar 14.

PMID:
23499842
15.

Cellular assay for the characterization of sphingosine-1-phosphate lyase inhibitors.

Billich A, Beerli C, Bergmann R, Bruns C, Loetscher E.

Anal Biochem. 2013 Mar 15;434(2):247-53. doi: 10.1016/j.ab.2012.11.026. Epub 2012 Dec 13.

PMID:
23246729
16.

An oral sphingosine 1-phosphate receptor 1 (S1P(1)) antagonist prodrug with efficacy in vivo: discovery, synthesis, and evaluation.

Angst D, Janser P, Quancard J, Buehlmayer P, Berst F, Oberer L, Beerli C, Streiff M, Pally C, Hersperger R, Bruns C, Bassilana F, Bollbuck B.

J Med Chem. 2012 Nov 26;55(22):9722-34. doi: 10.1021/jm3009508. Epub 2012 Oct 26.

PMID:
23067318
17.

A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis.

Quancard J, Bollbuck B, Janser P, Angst D, Berst F, Buehlmayer P, Streiff M, Beerli C, Brinkmann V, Guerini D, Smith PA, Seabrook TJ, Traebert M, Seuwen K, Hersperger R, Bruns C, Bassilana F, Bigaud M.

Chem Biol. 2012 Sep 21;19(9):1142-51. doi: 10.1016/j.chembiol.2012.07.016.

18.

Sotrastaurin (AEB071) alone and in combination with cyclosporine A prolongs survival times of non-human primate recipients of life-supporting kidney allografts.

Bigaud M, Wieczorek G, Beerli C, Audet M, Blancher A, Heusser C, Morris RE, Wagner J.

Transplantation. 2012 Jan 27;93(2):156-64. doi: 10.1097/TP.0b013e31823cf92f.

PMID:
22179400
19.

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.

Wagner J, von Matt P, Faller B, Cooke NG, Albert R, Sedrani R, Wiegand H, Jean C, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S.

J Med Chem. 2011 Sep 8;54(17):6028-39. doi: 10.1021/jm200469u. Epub 2011 Aug 8.

PMID:
21797275
20.

Small molecule CXCR3 antagonist NIBR2130 has only a limited impact on type 1 diabetes in a virus-induced mouse model.

Christen S, Holdener M, Beerli C, Thoma G, Bayer M, Pfeilschifter JM, Hintermann E, Zerwes HG, Christen U.

Clin Exp Immunol. 2011 Sep;165(3):318-28. doi: 10.1111/j.1365-2249.2011.04426.x. Epub 2011 Jun 7.

21.

BZM055, an iodinated radiotracer candidate for PET and SPECT imaging of myelin and FTY720 brain distribution.

Briard E, Orain D, Beerli C, Billich A, Streiff M, Bigaud M, Auberson YP.

ChemMedChem. 2011 Apr 4;6(4):667-77. doi: 10.1002/cmdc.201000477. Epub 2011 Jan 30.

PMID:
21280229
22.

Effects of the novel protein kinase C inhibitor AEB071 (Sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or FTY720.

Weckbecker G, Pally C, Beerli C, Burkhart C, Wieczorek G, Metzler B, Morris RE, Wagner J, Bruns C.

Transpl Int. 2010 May 1;23(5):543-52. doi: 10.1111/j.1432-2277.2009.01015.x. Epub 2009 Dec 9.

23.

Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.

Wagner J, von Matt P, Sedrani R, Albert R, Cooke N, Ehrhardt C, Geiser M, Rummel G, Stark W, Strauss A, Cowan-Jacob SW, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S.

J Med Chem. 2009 Oct 22;52(20):6193-6. doi: 10.1021/jm901108b.

PMID:
19827831
24.

Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.

Thoma G, Streiff MB, Kovarik J, Glickman F, Wagner T, Beerli C, Zerwes HG.

J Med Chem. 2008 Dec 25;51(24):7915-20. doi: 10.1021/jm801065q.

PMID:
19053768
25.

Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.

Thoma G, Beerli C, Bigaud M, Bruns C, Cooke NG, Streiff MB, Zerwes HG.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2000-5. doi: 10.1016/j.bmcl.2008.01.108. Epub 2008 Feb 2.

PMID:
18267361
26.

Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: consequences for mode of action in multiple sclerosis.

Foster CA, Howard LM, Schweitzer A, Persohn E, Hiestand PC, Balatoni B, Reuschel R, Beerli C, Schwartz M, Billich A.

J Pharmacol Exp Ther. 2007 Nov;323(2):469-75. Epub 2007 Aug 6.

PMID:
17682127
27.

A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.

Pan S, Mi Y, Pally C, Beerli C, Chen A, Guerini D, Hinterding K, Nuesslein-Hildesheim B, Tuntland T, Lefebvre S, Liu Y, Gao W, Chu A, Brinkmann V, Bruns C, Streiff M, Cannet C, Cooke N, Gray N.

Chem Biol. 2006 Nov;13(11):1227-34.

28.

Orally bioavailable competitive CCR5 antagonists.

Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG.

J Med Chem. 2004 Apr 8;47(8):1939-55.

PMID:
15055994
29.

Aromatic quinolinecarboxamides as selective, orally active antibody production inhibitors for prevention of acute xenograft rejection.

Papageorgiou C, von Matt A, Joergensen J, Andersen E, Wagner K, Beerli C, Than T, Borer X, Florineth A, Rihs G, Schreier MH, Weckbecker G, Heusser C.

J Med Chem. 2001 Jun 7;44(12):1986-92.

PMID:
11384243

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