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Page 1
An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient.
Quancard J, Klein T, Fung SY, Renatus M, Hughes N, Israël L, Priatel JJ, Kang S, Blank MA, Viner RI, Blank J, Schlapbach A, Erbel P, Kizhakkedathu J, Villard F, Hersperger R, Turvey SE, Eder J, Bornancin F, Overall CM. Quancard J, et al. Among authors: schlapbach a. Nat Chem Biol. 2019 Mar;15(3):304-313. doi: 10.1038/s41589-018-0222-1. Epub 2019 Jan 28. Nat Chem Biol. 2019. PMID: 30692685
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.
Waelchli R, Bollbuck B, Bruns C, Buhl T, Eder J, Feifel R, Hersperger R, Janser P, Revesz L, Zerwes HG, Schlapbach A. Waelchli R, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. doi: 10.1016/j.bmcl.2005.09.035. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236504
The T-cell fingerprint of MALT1 paracaspase revealed by selective inhibition.
Bardet M, Unterreiner A, Malinverni C, Lafossas F, Vedrine C, Boesch D, Kolb Y, Kaiser D, Glück A, Schneider MA, Katopodis A, Renatus M, Simic O, Schlapbach A, Quancard J, Régnier CH, Bold G, Pissot-Soldermann C, Carballido JM, Kovarik J, Calzascia T, Bornancin F. Bardet M, et al. Among authors: schlapbach a. Immunol Cell Biol. 2018 Jan;96(1):81-99. doi: 10.1111/imcb.1018. Epub 2017 Dec 21. Immunol Cell Biol. 2018. PMID: 29359407
Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.
Velcicky J, Schlapbach A, Heng R, Revesz L, Pflieger D, Blum E, Hawtin S, Huppertz C, Feifel R, Hersperger R. Velcicky J, et al. Among authors: schlapbach a. ACS Med Chem Lett. 2018 Mar 20;9(4):392-396. doi: 10.1021/acsmedchemlett.8b00098. eCollection 2018 Apr 12. ACS Med Chem Lett. 2018. PMID: 29670707 Free PMC article.
N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.
Schlapbach A, Revesz L, Pissot Soldermann C, Zoller T, Régnier CH, Bornancin F, Radimerski T, Blank J, Schuffenhauer A, Renatus M, Erbel P, Melkko S, Heng R, Simic O, Endres R, Wartmann M, Quancard J. Schlapbach A, et al. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2153-2158. doi: 10.1016/j.bmcl.2018.05.017. Epub 2018 May 9. Bioorg Med Chem Lett. 2018. PMID: 29759726
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: schlapbach a. Arthritis Rheumatol. 2020 Jun;72(6):919-930. doi: 10.1002/art.41204. Epub 2020 Apr 26. Arthritis Rheumatol. 2020. PMID: 31943941
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: schlapbach a. Front Immunol. 2020 Apr 30;11:745. doi: 10.3389/fimmu.2020.00745. eCollection 2020. Front Immunol. 2020. PMID: 32425939 Free PMC article.
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: schlapbach a. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
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: schlapbach a. 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
Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.
Pissot Soldermann C, Simic O, Renatus M, Erbel P, Melkko S, Wartmann M, Bigaud M, Weiss A, McSheehy P, Endres R, Santos P, Blank J, Schuffenhauer A, Bold G, Buschmann N, Zoller T, Altmann E, Manley PW, Dix I, Buchdunger E, Scesa J, Quancard J, Schlapbach A, Bornancin F, Radimerski T, Régnier CH. Pissot Soldermann C, et al. Among authors: schlapbach a. J Med Chem. 2020 Dec 10;63(23):14576-14593. doi: 10.1021/acs.jmedchem.0c01245. Epub 2020 Nov 30. J Med Chem. 2020. PMID: 33252239
25 results