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Items: 1 to 50 of 71

1.

In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Vaupel A, Holzer P, Ferretti S, Guagnano V, Kallen J, Mah R, Masuya K, Ruetz S, Rynn C, Schlapbach A, Stachyra T, Stutz S, Todorov M, Jeay S, Furet P.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3404-3408. doi: 10.1016/j.bmcl.2018.08.027. Epub 2018 Aug 26.

PMID:
30217415
2.

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Jeay S, Ferretti S, Holzer P, Fuchs J, Chapeau EA, Wartmann M, Sterker D, Romanet V, Murakami M, Kerr G, Durand EY, Gaulis S, Cortes-Cros M, Ruetz S, Stachyra TM, Kallen J, Furet P, Würthner J, Guerreiro N, Halilovic E, Jullion A, Kauffmann A, Kuriakose E, Wiesmann M, Jensen MR, Hofmann F, Sellers WR.

Cancer Res. 2018 Nov 1;78(21):6257-6267. doi: 10.1158/0008-5472.CAN-18-0338. Epub 2018 Aug 22.

PMID:
30135191
3.

Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface.

Mesrouze Y, Bokhovchuk F, Izaac A, Meyerhofer M, Zimmermann C, Fontana P, Schmelzle T, Erdmann D, Furet P, Kallen J, Chène P.

Protein Sci. 2018 Oct;27(10):1810-1820. doi: 10.1002/pro.3493.

PMID:
30058229
4.

Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S.

J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24.

PMID:
29990434
5.

X-ray Structures and Feasibility Assessment of CLK2 Inhibitors for Phelan-McDermid Syndrome.

Kallen J, Bergsdorf C, Arnaud B, Bernhard M, Brichet M, Cobos-Correa A, Elhajouji A, Freuler F, Galimberti I, Guibourdenche C, Haenni S, Holzinger S, Hunziker J, Izaac A, Kaufmann M, Leder L, Martus HJ, von Matt P, Polyakov V, Roethlisberger P, Roma G, Stiefl N, Uteng M, Lerchner A.

ChemMedChem. 2018 Sep 19;13(18):1997-2007. doi: 10.1002/cmdc.201800344. Epub 2018 Aug 16.

PMID:
29985556
6.

Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo.

Guendisch U, Weiss J, Ecoeur F, Riker JC, Kaupmann K, Kallen J, Hintermann S, Orain D, Dawson J, Billich A, Guntermann C.

PLoS One. 2017 Nov 20;12(11):e0188391. doi: 10.1371/journal.pone.0188391. eCollection 2017.

7.

Effect of the acylation of TEAD4 on its interaction with co-activators YAP and TAZ.

Mesrouze Y, Meyerhofer M, Bokhovchuk F, Fontana P, Zimmermann C, Martin T, Delaunay C, Izaac A, Kallen J, Schmelzle T, Erdmann D, Chène P.

Protein Sci. 2017 Dec;26(12):2399-2409. doi: 10.1002/pro.3312. Epub 2017 Nov 11.

PMID:
28960584
8.

Structural States of RORγt: X-ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds.

Kallen J, Izaac A, Be C, Arista L, Orain D, Kaupmann K, Guntermann C, Hoegenauer K, Hintermann S.

ChemMedChem. 2017 Jul 6;12(13):1014-1021. doi: 10.1002/cmdc.201700278. Epub 2017 Jun 20.

PMID:
28590087
9.

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists.

Hintermann S, Guntermann C, Mattes H, Carcache DA, Wagner J, Vulpetti A, Billich A, Dawson J, Kaupmann K, Kallen J, Stringer R, Orain D.

ChemMedChem. 2016 Dec 16;11(24):2640-2648. doi: 10.1002/cmdc.201600500. Epub 2016 Nov 30.

PMID:
27902884
10.

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist.

Orain D, Tasdelen E, Haessig S, Koller M, Picard A, Dubois C, Lingenhoehl K, Desrayaud S, Floersheim P, Carcache D, Urwyler S, Kallen J, Mattes H.

ChemMedChem. 2017 Feb 3;12(3):197-201. doi: 10.1002/cmdc.201600467. Epub 2016 Nov 15.

PMID:
27863026
11.

Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2016 Nov 17;5. pii: e19317. doi: 10.7554/eLife.19317. No abstract available.

12.

Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9.

PMID:
27542305
13.

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.

J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5.

PMID:
26181851
14.

Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.

Gessier F, Kallen J, Jacoby E, Chène P, Stachyra-Valat T, Ruetz S, Jeay S, Holzer P, Masuya K, Furet P.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3621-5. doi: 10.1016/j.bmcl.2015.06.058. Epub 2015 Jun 23.

PMID:
26141769
15.

A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2015 May 12;4. pii: e06498. doi: 10.7554/eLife.06498. Erratum in: Elife. 2016 Nov 17;5:null.

16.

Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.

Vaupel A, Bold G, De Pover A, Stachyra-Valat T, Lisztwan JH, Kallen J, Masuya K, Furet P.

Bioorg Med Chem Lett. 2014 May 1;24(9):2110-4. doi: 10.1016/j.bmcl.2014.03.039. Epub 2014 Mar 22. Erratum in: Bioorg Med Chem Lett. 2015 Mar 15;25(6):1356. Hergovich-Lisztwan, Joanna [corrected to Lisztwan, Joanna Hergovich].

PMID:
24704029
17.

Identification and X-ray co-crystal structure of a small-molecule activator of LFA-1-ICAM-1 binding.

Hintersteiner M, Kallen J, Schmied M, Graf C, Jung T, Mudd G, Shave S, Gstach H, Auer M.

Angew Chem Int Ed Engl. 2014 Apr 22;53(17):4322-6. doi: 10.1002/anie.201310240. Epub 2014 Apr 1.

18.

A fracture prevention service reduces further fractures two years after incident minimal trauma fracture.

Van der Kallen J, Giles M, Cooper K, Gill K, Parker V, Tembo A, Major G, Ross L, Carter J.

Int J Rheum Dis. 2014 Feb;17(2):195-203. doi: 10.1111/1756-185X.12101. Epub 2013 May 28.

PMID:
24576275
19.

Safety and efficacy of catheter directed thrombolysis in children with deep venous thrombosis.

Darbari DS, Desai D, Arnaldez F, Desai K, Kallen J, Strouse J, Streiff MB, Hong K, Takemoto CM.

Br J Haematol. 2012 Nov;159(3):376-8. doi: 10.1111/bjh.12025. Epub 2012 Aug 31. No abstract available.

PMID:
22934795
20.

The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.

Furet P, Chène P, De Pover A, Valat TS, Lisztwan JH, Kallen J, Masuya K.

Bioorg Med Chem Lett. 2012 May 15;22(10):3498-502. doi: 10.1016/j.bmcl.2012.03.083. Epub 2012 Mar 30.

PMID:
22507962
21.

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, Urwyler S.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):996-9. doi: 10.1016/j.bmcl.2011.12.009. Epub 2011 Dec 8.

PMID:
22197388
22.

Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.

Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3358-61. doi: 10.1016/j.bmcl.2011.04.017. Epub 2011 Apr 8.

PMID:
21531559
23.

The x-ray crystal structure of the first RNA recognition motif and site-directed mutagenesis suggest a possible HuR redox sensing mechanism.

Benoit RM, Meisner NC, Kallen J, Graff P, Hemmig R, Cèbe R, Ostermeier C, Widmer H, Auer M.

J Mol Biol. 2010 Apr 16;397(5):1231-44. doi: 10.1016/j.jmb.2010.02.043. Epub 2010 Feb 26.

PMID:
20219472
24.

Knowledge-based virtual screening: application to the MDM4/p53 protein-protein interaction.

Jacoby E, Boettcher A, Mayr LM, Brown N, Jenkins JL, Kallen J, Engeloch C, Schopfer U, Furet P, Masuya K, Lisztwan J.

Methods Mol Biol. 2009;575:173-94. doi: 10.1007/978-1-60761-274-2_7.

PMID:
19727615
25.

Reduced Z-axis coverage multidetector CT angiography for suspected acute pulmonary embolism could decrease dose and maintain diagnostic accuracy.

Kallen JA, Coughlin BF, O'Loughlin MT, Stein B.

Emerg Radiol. 2010 Jan;17(1):31-5. doi: 10.1007/s10140-009-0818-6. Epub 2009 May 26.

PMID:
19468764
26.

Crystal Structures of Human MdmX (HdmX) in Complex with p53 Peptide Analogues Reveal Surprising Conformational Changes.

Kallen J, Goepfert A, Blechschmidt A, Izaac A, Geiser M, Tavares G, Ramage P, Furet P, Masuya K, Lisztwan J.

J Biol Chem. 2009 Mar 27;284(13):8812-21. doi: 10.1074/jbc.M809096200. Epub 2009 Jan 19.

27.

Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.

Kallen J, Lattmann R, Beerli R, Blechschmidt A, Blommers MJ, Geiser M, Ottl J, Schlaeppi JM, Strauss A, Fournier B.

J Biol Chem. 2007 Aug 10;282(32):23231-9. Epub 2007 Jun 6.

28.

Structure of human cyclophilin A in complex with the novel immunosuppressant sanglifehrin A at 1.6 A resolution.

Kallen J, Sedrani R, Zenke G, Wagner J.

J Biol Chem. 2005 Jun 10;280(23):21965-71. Epub 2005 Mar 16.

29.

1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.

Wattanasin S, Kallen J, Myers S, Guo Q, Sabio M, Ehrhardt C, Albert R, Hommel U, Weckbecker G, Welzenbach K, Weitz-Schmidt G.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1217-20.

PMID:
15686945
30.

Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.

Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Geiser M, Halleux C, Kallen J, Keller H, Ramage P.

J Med Chem. 2005 Jan 27;48(2):364-79.

PMID:
15658851
31.
33.

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.

Linton SD, Aja T, Allegrini PR, Deckwerth TL, Diaz JL, Hengerer B, Herrmann J, Jahangiri KG, Kallen J, Karanewsky DS, Meduna SP, Nalley K, Robinson ED, Roggo S, Rovelli G, Sauter A, Sayers RO, Schmitz A, Smidt R, Ternansky RJ, Tomaselli KJ, Ullman BR, Wiessner C, Wu JC.

Bioorg Med Chem Lett. 2004 May 17;14(10):2685-91.

PMID:
15109679
34.

Crystal structure of the human RORalpha Ligand binding domain in complex with cholesterol sulfate at 2.2 A.

Kallen J, Schlaeppi JM, Bitsch F, Delhon I, Fournier B.

J Biol Chem. 2004 Apr 2;279(14):14033-8. Epub 2004 Jan 13.

35.

Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.

Bitsch F, Aichholz R, Kallen J, Geisse S, Fournier B, Schlaeppi JM.

Anal Biochem. 2003 Dec 1;323(1):139-49.

PMID:
14622968
36.

Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.

Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Halleux C, Kallen J, Keller H, Schlaeppi JM, Stark W.

J Med Chem. 2003 Jul 3;46(14):2945-57.

PMID:
12825935
37.

Sanglifehrin-cyclophilin interaction: degradation work, synthetic macrocyclic analogues, X-ray crystal structure, and binding data.

Sedrani R, Kallen J, Martin Cabrejas LM, Papageorgiou CD, Senia F, Rohrbach S, Wagner D, Thai B, Jutzi Eme AM, France J, Oberer L, Rihs G, Zenke G, Wagner J.

J Am Chem Soc. 2003 Apr 2;125(13):3849-59.

PMID:
12656618
38.

X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha.

Kallen JA, Schlaeppi JM, Bitsch F, Geisse S, Geiser M, Delhon I, Fournier B.

Structure. 2002 Dec;10(12):1697-707.

39.

Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site.

Weitz-Schmidt G, Welzenbach K, Brinkmann V, Kamata T, Kallen J, Bruns C, Cottens S, Takada Y, Hommel U.

Nat Med. 2001 Jun;7(6):687-92.

PMID:
11385505
40.

Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain.

Kallen J, Welzenbach K, Ramage P, Geyl D, Kriwacki R, Legge G, Cottens S, Weitz-Schmidt G, Hommel U.

J Mol Biol. 1999 Sep 10;292(1):1-9.

PMID:
10493852
42.

Macrolide Analogues of the Novel Immunosuppressant Sanglifehrin: New Application of the Ring-Closing Metathesis Reaction.

Martin Cabrejas LM, Rohrbach S, Wagner D, Kallen J, Zenke G, Wagner J.

Angew Chem Int Ed Engl. 1999 Aug;38(16):2443-2446.

PMID:
10458816
43.

X-ray structure and conformational dynamics of the HIV-1 protease in complex with the inhibitor SDZ283-910: agreement of time-resolved spectroscopy and molecular dynamics simulations.

Ringhofer S, Kallen J, Dutzler R, Billich A, Visser AJ, Scholz D, Steinhauser O, Schreiber H, Auer M, Kungl AJ.

J Mol Biol. 1999 Mar 5;286(4):1147-59.

PMID:
10047488
44.
45.
46.

X-ray structures and analysis of 11 cyclosporin derivatives complexed with cyclophilin A.

Kallen J, Mikol V, Taylor P, Walkinshaw MD.

J Mol Biol. 1998 Oct 23;283(2):435-49.

PMID:
9769216
47.

Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.

Wagner J, Kallen J, Ehrhardt C, Evenou JP, Wagner D.

J Med Chem. 1998 Sep 10;41(19):3664-74.

PMID:
9733491
48.

Chemical modification of rapamycin: the discovery of SDZ RAD.

Sedrani R, Cottens S, Kallen J, Schuler W.

Transplant Proc. 1998 Aug;30(5):2192-4. No abstract available.

PMID:
9723437
49.

Demonstration of a cell-specific isomerization of invertebrate neuropeptides.

Soyez D, Laverdure AM, Kallen J, Van Herp F.

Neuroscience. 1998 Feb;82(3):935-42.

PMID:
9483547
50.

Conformational control of cyclosporin through substitution of the N-5 position. A new class of cyclosporin antagonists.

Papageorgiou C, Kallen J, France J, French R.

Bioorg Med Chem. 1997 Jan;5(1):187-92.

PMID:
9043670

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