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Discovery of potent SARS-CoV-2 nsp3 macrodomain inhibitors uncovers lack of translation to cellular antiviral response.
Lee AA, Amick I, Aschenbrenner JC, Barr HM, Benjamin J, Brandis A, Cohen G, Diaz-Tapia R, Duberstein S, Dixon J, Cousins D, Fairhead M, Fearon D, Frick J, Gayvert J, Godoy AS, Griffin EJ, Huber K, Koekemoer L, Lahav N, Marples PG, McGovern BL, Mehlman T, Robinson MC, Singh U, Szommer T, Tomlinson CWE, Vargo T, von Delft F, Wang S, White K, Williams E, Winokan M. Lee AA, et al. Among authors: huber k. bioRxiv [Preprint]. 2024 Aug 21:2024.08.19.608619. doi: 10.1101/2024.08.19.608619. bioRxiv. 2024. PMID: 39229055 Free PMC article. Preprint.
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.
Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N. Resnick E, et al. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22. J Am Chem Soc. 2019. PMID: 31060360 Free PMC article.
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
Balıkçı E, Marques AMC, Bauer LG, Seupel R, Bennett J, Raux B, Buchan K, Simelis K, Singh U, Rogers C, Ward J, Cheng C, Szommer T, Schützenhofer K, Elkins JM, Sloman DL, Ahel I, Fedorov O, Brennan PE, Huber KVM. Balıkçı E, et al. Among authors: huber kvm. J Med Chem. 2024 May 9;67(9):7245-7259. doi: 10.1021/acs.jmedchem.4c00072. Epub 2024 Apr 18. J Med Chem. 2024. PMID: 38635563 Free PMC article.
Deliberately Losing Control of C-H Activation Processes in the Design of Small-Molecule-Fragment Arrays Targeting Peroxisomal Metabolism.
Khan Tareque R, Hassell-Hart S, Krojer T, Bradley A, Velupillai S, Talon R, Fairhead M, Day IJ, Bala K, Felix R, Kemmitt PD, Brennan P, von Delft F, Díaz Sáez L, Huber K, Spencer J. Khan Tareque R, et al. Among authors: huber k. ChemMedChem. 2020 Dec 15;15(24):2513-2520. doi: 10.1002/cmdc.202000543. Epub 2020 Sep 28. ChemMedChem. 2020. PMID: 32812371
Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.
Kidd SL, Fowler E, Reinhardt T, Compton T, Mateu N, Newman H, Bellini D, Talon R, McLoughlin J, Krojer T, Aimon A, Bradley A, Fairhead M, Brear P, Díaz-Sáez L, McAuley K, Sore HF, Madin A, O'Donovan DH, Huber KVM, Hyvönen M, von Delft F, Dowson CG, Spring DR. Kidd SL, et al. Among authors: huber kvm. Chem Sci. 2020 May 14;11(39):10792-10801. doi: 10.1039/d0sc01232g. Chem Sci. 2020. PMID: 34094333 Free PMC article.
Effects of myo-inositol supplementation in the diet on myo-inositol concentrations in the intestine, blood, eggs, and excreta of laying hens.
Sommerfeld V, Hanauska A, Huber K, Bennewitz J, Camarinha-Silva A, Feger M, Föller M, Oster M, Ponsuksili S, Schmucker S, Seifert J, Stefanski V, Wimmers K, Rodehutscord M. Sommerfeld V, et al. Among authors: huber k. Poult Sci. 2024 Nov 10;104(1):104545. doi: 10.1016/j.psj.2024.104545. Online ahead of print. Poult Sci. 2024. PMID: 39579515 Free article.
Covalent Inhibitors of KEAP1 with Exquisite Selectivity.
Fejes I, Markacz P, Tatai J, Rudas M, Dunkel P, Gyuris M, Nyerges M, Provost N, Duvivier V, Delerive P, Martiny V, Bristiel A, Vidal B, Richardson W, Rothweiler EM, Tranberg-Jensen J, Manning CE, Sweeney MN, Chalk R, Huber KVM, Bullock AN, Herner A, Seedorf K, Vinson C, Weber C, Kotschy A. Fejes I, et al. Among authors: huber kvm. J Med Chem. 2024 Nov 21. doi: 10.1021/acs.jmedchem.4c02019. Online ahead of print. J Med Chem. 2024. PMID: 39572012
2,091 results