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Items: 15

1.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

McNally R, Li Q, Li K, Dekker C, Vangrevelinghe E, Jones M, Chène P, Machauer R, Radimerski T, Eck MJ.

ACS Chem Biol. 2019 Mar 11. doi: 10.1021/acschembio.8b00722. [Epub ahead of print]

PMID:
30763067
2.

The β-secretase (BACE) inhibitor NB-360 in preclinical models: From amyloid-β reduction to downstream disease-relevant effects.

Neumann U, Machauer R, Shimshek DR.

Br J Pharmacol. 2019 Jan 18. doi: 10.1111/bph.14582. [Epub ahead of print] Review.

PMID:
30657591
3.

The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.

Neumann U, Ufer M, Jacobson LH, Rouzade-Dominguez ML, Huledal G, Kolly C, Lüönd RM, Machauer R, Veenstra SJ, Hurth K, Rueeger H, Tintelnot-Blomley M, Staufenbiel M, Shimshek DR, Perrot L, Frieauff W, Dubost V, Schiller H, Vogg B, Beltz K, Avrameas A, Kretz S, Pezous N, Rondeau JM, Beckmann N, Hartmann A, Vormfelde S, David OJ, Galli B, Ramos R, Graf A, Lopez Lopez C.

EMBO Mol Med. 2018 Nov;10(11). pii: e9316. doi: 10.15252/emmm.201809316.

4.

Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.

Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3.

PMID:
29764741
5.

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C.

ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9.

6.

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C.

ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11.

7.

Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice.

Shimshek DR, Jacobson LH, Kolly C, Zamurovic N, Balavenkatraman KK, Morawiec L, Kreutzer R, Schelle J, Jucker M, Bertschi B, Theil D, Heier A, Bigot K, Beltz K, Machauer R, Brzak I, Perrot L, Neumann U.

Sci Rep. 2016 Feb 25;6:21917. doi: 10.1038/srep21917.

8.

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.

Neumann U, Rueeger H, Machauer R, Veenstra SJ, Lueoend RM, Tintelnot-Blomley M, Laue G, Beltz K, Vogg B, Schmid P, Frieauff W, Shimshek DR, Staufenbiel M, Jacobson LH.

Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8.

9.

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.

Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5300-6. doi: 10.1016/j.bmcl.2013.07.071. Epub 2013 Aug 9.

PMID:
23981898
10.

Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.

Rueeger H, Lueoend R, Rogel O, Rondeau JM, Möbitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U.

J Med Chem. 2012 Apr 12;55(7):3364-86. doi: 10.1021/jm300069y. Epub 2012 Mar 21.

PMID:
22380629
11.

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

Lerchner A, Machauer R, Betschart C, Veenstra S, Rueeger H, McCarthy C, Tintelnot-Blomley M, Jaton AL, Rabe S, Desrayaud S, Enz A, Staufenbiel M, Paganetti P, Rondeau JM, Neumann U.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22.

PMID:
19963375
12.

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Machauer R, Laumen K, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Jaton AL, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055. Epub 2009 Jan 22.

PMID:
19195887
13.

Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.

Machauer R, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Neumann U, Paganetti P.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1361-5. doi: 10.1016/j.bmcl.2009.01.036. Epub 2009 Jan 19. Erratum in: Bioorg Med Chem Lett. 2009 Apr 15;19(8):2366.

PMID:
19195886

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