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Page 1
A first-in-human phase 1/2 dose-escalation study of MAK683 (EED inhibitor) in patients with advanced malignancies.
Ribrag V, Iglesias L, De Braud F, Ma B, Yokota T, Zander T, Spreafico A, Subbiah V, Illert AL, Tan D, Santoro A, Munster PN, Suehiro Y, Wang Y, Ji DM, Chen S, Beltz K, Suenaga N, Ramkumar T, Luo F, Lai C, Wainberg ZA. Ribrag V, et al. Among authors: beltz k. Eur J Cancer. 2024 Nov 16;216:115122. doi: 10.1016/j.ejca.2024.115122. Online ahead of print. Eur J Cancer. 2024. PMID: 39793445
Discovery of NP3-253, a Potent Brain Penetrant Inhibitor of the NLRP3 Inflammasome.
Mackay A, Velcicky J, Gommermann N, Mattes H, Janser P, Wright M, Dubois C, Brenneisen S, Ilic S, Vangrevelinghe E, Stiefl N, Boettcher A, Schoenboerner M, Vogelsanger M, Muller-Bentz S, Kamke M, Rubert J, Kauffmann M, Desrayaud S, Trunzer M, Srinivas H, Hinniger A, von Burg N, Beltz K, Dekker C, Farady CJ. Mackay A, et al. Among authors: beltz k. J Med Chem. 2024 Dec 12;67(23):20780-20798. doi: 10.1021/acs.jmedchem.4c02350. Epub 2024 Nov 22. J Med Chem. 2024. PMID: 39574318
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
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.
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
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.
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.
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