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Page 1
BET bromodomain inhibitors regulate keratinocyte plasticity.
Schutzius G, Kolter C, Bergling S, Tortelli F, Fuchs F, Renner S, Guagnano V, Cotesta S, Rueeger H, Faller M, Bouchez L, Salathe A, Nigsch F, Richards SM, Louis M, Gruber V, Aebi A, Turner J, Grandjean F, Li J, Dimitri C, Thomas JR, Schirle M, Blank J, Drueckes P, Vaupel A, Tiedt R, Manley PW, Klopp J, Hemmig R, Zink F, Leroy N, Carbone W, Roma G, Keller CG, Dales N, Beyerbach A, Zimmerlin A, Bonenfant D, Terranova R, Berwick A, Sahambi S, Reynolds A, Jennings LL, Ruffner H, Tarsa P, Bouwmeester T, Driver V, Frederiksen M, Lohmann F, Kirkland S. Schutzius G, et al. Among authors: blank j. Nat Chem Biol. 2021 Mar;17(3):280-290. doi: 10.1038/s41589-020-00716-z. Epub 2021 Jan 18. Nat Chem Biol. 2021. PMID: 33462494
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
Discovery of 1-((6-Aminopyridin-3-yl)Methyl)-3-(4-Bromophenyl)Urea as a Potent, Irreversible Myeloperoxidase Inhibitor.
Marro ML, Patterson AW, Lee L, Deng L, Reynolds A, Ren X, Axford L, Patnaik A, Hollis-Symynkywicz M, Casson N, Custeau D, Ames L, Loi S, Zhang L, Honda T, Blank J, Harrison TJ, Papillon JPN, Hamann LG, Marcinkeviciene J, Regard JB. Marro ML, et al. Among authors: blank j. J Pharmacol Exp Ther. 2018 Oct;367(1):147-154. doi: 10.1124/jpet.118.248435. Epub 2018 Aug 3. J Pharmacol Exp Ther. 2018. PMID: 30076263
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
Evolution of Novartis' Small Molecule Screening Deck Design.
Schuffenhauer A, Schneider N, Hintermann S, Auld D, Blank J, Cotesta S, Engeloch C, Fechner N, Gaul C, Giovannoni J, Jansen J, Joslin J, Krastel P, Lounkine E, Manchester J, Monovich LG, Pelliccioli AP, Schwarze M, Shultz MD, Stiefl N, Baeschlin DK. Schuffenhauer A, et al. Among authors: blank j. J Med Chem. 2020 Dec 10;63(23):14425-14447. doi: 10.1021/acs.jmedchem.0c01332. Epub 2020 Nov 3. J Med Chem. 2020. PMID: 33140646 Review.
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
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist.
Betschart C, Faller M, Zink F, Hemmig R, Blank J, Vangrevelinghe E, Bourrel M, Glatthar R, Behnke D, Barker K, Heizmann A, Angst D, Nimsgern P, Jacquier S, Junt T, Zipfel G, Ruzzante G, Loetscher P, Limonta S, Hawtin S, Andre CB, Boulay T, Feifel R, Knoepfel T. Betschart C, et al. Among authors: blank j. ACS Med Chem Lett. 2022 Mar 10;13(4):658-664. doi: 10.1021/acsmedchemlett.1c00696. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450354 Free PMC article.
Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction.
Ding J, Li G, Liu H, Liu L, Lin Y, Gao J, Zhou G, Shen L, Zhao M, Yu Y, Guo W, Hommel U, Ottl J, Blank J, Aubin N, Wei Y, He H, Sage DR, Atadja PW, Li E, Jain RK, Tallarico JA, Canham SM, Chiang YL, Wang H. Ding J, et al. Among authors: blank j. ACS Chem Biol. 2023 Jan 20;18(1):34-40. doi: 10.1021/acschembio.2c00843. Epub 2023 Jan 3. ACS Chem Biol. 2023. PMID: 36594833
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.
393 results