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Page 1
Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors.
Velcicky J, Janser P, Gommermann N, Brenneisen S, Ilic S, Vangrevelinghe E, Stiefl N, Boettcher A, Arnold C, Malinverni C, Dawson J, Murgasova R, Desrayaud S, Beltz K, Hinniger A, Dekker C, Farady CJ, Mackay A. Velcicky J, et al. Among authors: beltz k. J Med Chem. 2024 Jan 25;67(2):1544-1562. doi: 10.1021/acs.jmedchem.3c02098. Epub 2024 Jan 4. J Med Chem. 2024. PMID: 38175811
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Machauer R, Lueoend R, Hurth K, Veenstra SJ, Rueeger H, Voegtle M, Tintelnot-Blomley M, Rondeau JM, Jacobson LH, Laue G, Beltz K, Neumann U. Machauer R, et al. Among authors: beltz k. J Med Chem. 2021 Oct 28;64(20):15262-15279. doi: 10.1021/acs.jmedchem.1c01300. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34648711
Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.
Quancard J, Simic O, Pissot Soldermann C, Aichholz R, Blatter M, Renatus M, Erbel P, Melkko S, Endres R, Sorge M, Kieffer L, Wagner T, Beltz K, Mcsheehy P, Wartmann M, Régnier CH, Calzascia T, Radimerski T, Bigaud M, Weiss A, Bornancin F, Schlapbach A. Quancard J, et al. Among authors: beltz k. J Med Chem. 2020 Dec 10;63(23):14594-14608. doi: 10.1021/acs.jmedchem.0c01246. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216547
Requirement of Mucosa-Associated Lymphoid Tissue Lymphoma Translocation Protein 1 Protease Activity for Fcγ Receptor-Induced Arthritis, but Not Fcγ Receptor-Mediated Platelet Elimination, in Mice.
Martin K, Touil R, Cvijetic G, Israel L, Kolb Y, Sarret S, Valeaux S, Degl'Innocenti E, Le Meur T, Caesar N, Bardet M, Beerli C, Zerwes HG, Kovarik J, Beltz K, Schlapbach A, Quancard J, Régnier CH, Bigaud M, Junt T, Wieczorek G, Isnardi I, Littlewood-Evans A, Bornancin F, Calzascia T. Martin K, et al. Among authors: beltz k. Arthritis Rheumatol. 2020 Jun;72(6):919-930. doi: 10.1002/art.41204. Epub 2020 Apr 26. Arthritis Rheumatol. 2020. PMID: 31943941
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. Shimshek DR, et al. Among authors: beltz k. Sci Rep. 2016 Feb 25;6:21917. doi: 10.1038/srep21917. Sci Rep. 2016. PMID: 26912421 Free PMC article.
Pharmacological Inhibition of MALT1 Protease Leads to a Progressive IPEX-Like Pathology.
Martin K, Junker U, Tritto E, Sutter E, Rubic-Schneider T, Morgan H, Niwa S, Li J, Schlapbach A, Walker D, Bigaud M, Beerli C, Littlewood-Evans A, Rudolph B, Laisney M, Ledieu D, Beltz K, Quancard J, Bornancin F, Zamurovic Ribrioux N, Calzascia T. Martin K, et al. Among authors: beltz k. Front Immunol. 2020 Apr 30;11:745. doi: 10.3389/fimmu.2020.00745. eCollection 2020. Front Immunol. 2020. PMID: 32425939 Free PMC article.
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. Neumann U, et al. Among authors: beltz k. EMBO Mol Med. 2018 Nov;10(11):e9316. doi: 10.15252/emmm.201809316. EMBO Mol Med. 2018. PMID: 30224383 Free PMC article. Clinical Trial.
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. Neumann U, et al. Among authors: beltz k. Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8. Mol Neurodegener. 2015. PMID: 26336937 Free PMC article.
An adenosine nucleoside inhibitor of dengue virus.
Yin Z, Chen YL, Schul W, Wang QY, Gu F, Duraiswamy J, Kondreddi RR, Niyomrattanakit P, Lakshminarayana SB, Goh A, Xu HY, Liu W, Liu B, Lim JY, Ng CY, Qing M, Lim CC, Yip A, Wang G, Chan WL, Tan HP, Lin K, Zhang B, Zou G, Bernard KA, Garrett C, Beltz K, Dong M, Weaver M, He H, Pichota A, Dartois V, Keller TH, Shi PY. Yin Z, et al. Among authors: beltz k. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20435-9. doi: 10.1073/pnas.0907010106. Epub 2009 Nov 16. Proc Natl Acad Sci U S A. 2009. PMID: 19918064 Free PMC article.
16 results