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Page 1
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: blank j. 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
A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.
Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F. Tiedt R, et al. Among authors: blank j. Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22. Cancer Res. 2011. PMID: 21697284
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Shultz MD, Kirby CA, Stams T, Chin DN, Blank J, Charlat O, Cheng H, Cheung A, Cong F, Feng Y, Fortin PD, Hood T, Tyagi V, Xu M, Zhang B, Shao W. Shultz MD, et al. Among authors: blank j. J Med Chem. 2012 Feb 9;55(3):1127-36. doi: 10.1021/jm2011222. Epub 2012 Feb 1. J Med Chem. 2012. PMID: 22260203
Structural determinants of MALT1 protease activity.
Wiesmann C, Leder L, Blank J, Bernardi A, Melkko S, Decock A, D'Arcy A, Villard F, Erbel P, Hughes N, Freuler F, Nikolay R, Alves J, Bornancin F, Renatus M. Wiesmann C, et al. Among authors: blank j. J Mol Biol. 2012 May 25;419(1-2):4-21. doi: 10.1016/j.jmb.2012.02.018. Epub 2012 Feb 23. J Mol Biol. 2012. PMID: 22366302 Free 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. Among authors: blank j. 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
Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P. Fairhurst RA, et al. Among authors: blank j. Medchemcomm. 2017 Jun 8;8(8):1604-1613. doi: 10.1039/c7md00213k. eCollection 2017 Aug 1. Medchemcomm. 2017. PMID: 30108871 Free PMC article.
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: blank j, blank ma. 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
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J, Schadt HS, Couttet P, Wolf A, Wang Y, Barzaghi-Rinaudo P, Murakami M, Kauffmann A, Knoepfel T, Buschmann N, Leblanc C, Mah R, Furet P, Blank J, Hofmann F, Sellers WR, Graus Porta D. Weiss A, et al. Among authors: blank j. Mol Cancer Ther. 2019 Dec;18(12):2194-2206. doi: 10.1158/1535-7163.MCT-18-1291. Epub 2019 Aug 13. Mol Cancer Ther. 2019. PMID: 31409633
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Knoepfel T, Nimsgern P, Jacquier S, Bourrel M, Vangrevelinghe E, Glatthar R, Behnke D, Alper PB, Michellys PY, Deane J, Junt T, Zipfel G, Limonta S, Hawtin S, Andre C, Boulay T, Loetscher P, Faller M, Blank J, Feifel R, Betschart C. Knoepfel T, et al. Among authors: blank j. J Med Chem. 2020 Aug 13;63(15):8276-8295. doi: 10.1021/acs.jmedchem.0c00130. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32786235
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: blank j. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
385 results