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Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.
Specker E, Matthes S, Wesolowski R, Schütz A, Grohmann M, Alenina N, Pleimes D, Mallow K, Neuenschwander M, Gogolin A, Weise M, Pfeifer J, Ziebart N, Heinemann U, von Kries JP, Nazaré M, Bader M. Specker E, et al. Among authors: heinemann u. J Med Chem. 2022 Aug 25;65(16):11126-11149. doi: 10.1021/acs.jmedchem.2c00598. Epub 2022 Aug 3. J Med Chem. 2022. PMID: 35921615
Usa1 functions as a scaffold of the HRD-ubiquitin ligase.
Horn SC, Hanna J, Hirsch C, Volkwein C, Schütz A, Heinemann U, Sommer T, Jarosch E. Horn SC, et al. Among authors: heinemann u. Mol Cell. 2009 Dec 11;36(5):782-93. doi: 10.1016/j.molcel.2009.10.015. Mol Cell. 2009. PMID: 20005842 Free article.
The Lin28 cold-shock domain remodels pre-let-7 microRNA.
Mayr F, Schütz A, Döge N, Heinemann U. Mayr F, et al. Among authors: heinemann u. Nucleic Acids Res. 2012 Aug;40(15):7492-506. doi: 10.1093/nar/gks355. Epub 2012 May 8. Nucleic Acids Res. 2012. PMID: 22570413 Free PMC article.
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Mostinski Y, Heynen GJJE, López-Alberca MP, Paul J, Miksche S, Radetzki S, Schaller D, Shanina E, Seyffarth C, Kolomeets Y, Ziebart N, de Schryver J, Oestreich S, Neuenschwander M, Roske Y, Heinemann U, Rademacher C, Volkamer A, von Kries JP, Birchmeier W, Nazaré M. Mostinski Y, et al. Among authors: heinemann u. J Med Chem. 2020 Dec 10;63(23):14780-14804. doi: 10.1021/acs.jmedchem.0c01265. Epub 2020 Nov 19. J Med Chem. 2020. PMID: 33210922
Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer.
Carter DM, Specker E, Małecki PH, Przygodda J, Dudaniec K, Weiss MS, Heinemann U, Nazaré M, Gohlke U. Carter DM, et al. Among authors: heinemann u. J Med Chem. 2021 Oct 14;64(19):14266-14282. doi: 10.1021/acs.jmedchem.1c00693. Epub 2021 Sep 23. J Med Chem. 2021. PMID: 34555281 Free article.
Tricellulin is a target of the ubiquitin ligase Itch.
Jennek S, Mittag S, Reiche J, Westphal JK, Seelk S, Dörfel MJ, Pfirrmann T, Friedrich K, Schütz A, Heinemann U, Huber O. Jennek S, et al. Among authors: heinemann u. Ann N Y Acad Sci. 2017 Jun;1397(1):157-168. doi: 10.1111/nyas.13349. Epub 2017 Apr 24. Ann N Y Acad Sci. 2017. PMID: 28436082
Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells.
Barone M, Müller M, Chiha S, Ren J, Albat D, Soicke A, Dohmen S, Klein M, Bruns J, van Dinther M, Opitz R, Lindemann P, Beerbaum M, Motzny K, Roske Y, Schmieder P, Volkmer R, Nazaré M, Heinemann U, Oschkinat H, Ten Dijke P, Schmalz HG, Kühne R. Barone M, et al. Among authors: heinemann u. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29684-29690. doi: 10.1073/pnas.2007213117. Epub 2020 Nov 12. Proc Natl Acad Sci U S A. 2020. PMID: 33184177 Free PMC article.
Crystal structure and site-directed mutagenesis of Bacillus macerans endo-1,3-1,4-beta-glucanase.
Hahn M, Olsen O, Politz O, Borriss R, Heinemann U. Hahn M, et al. Among authors: heinemann u. J Biol Chem. 1995 Feb 17;270(7):3081-8. doi: 10.1074/jbc.270.7.3081. J Biol Chem. 1995. PMID: 7852389 Free article.
Crystal structure analysis at 2.3-A resolution reveals a jelly-roll protein structure with a deep active site channel harboring the amino acid residues Trp101, Glu103, Asp105, and Glu107 as in the hybrid Bacillus beta-glucanase H(A16-M) (Keitel, T., Simon, O., Borriss, R., and …
Crystal structure analysis at 2.3-A resolution reveals a jelly-roll protein structure with a deep active site channel harboring the amino ac …
713 results