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A natural-product switch for a dynamic protein interface.
Scheepstra M, Nieto L, Hirsch AK, Fuchs S, Leysen S, Lam CV, in het Panhuis L, van Boeckel CA, Wienk H, Boelens R, Ottmann C, Milroy LG, Brunsveld L. Scheepstra M, et al. Angew Chem Int Ed Engl. 2014 Jun 16;53(25):6443-8. doi: 10.1002/anie.201403773. Epub 2014 May 12. Angew Chem Int Ed Engl. 2014. PMID: 24821627
Ligand Dependent Switch from RXR Homo- to RXR-NURR1 Heterodimerization.
Scheepstra M, Andrei SA, de Vries RMJM, Meijer FA, Ma JN, Burstein ES, Olsson R, Ottmann C, Milroy LG, Brunsveld L. Scheepstra M, et al. ACS Chem Neurosci. 2017 Sep 20;8(9):2065-2077. doi: 10.1021/acschemneuro.7b00216. Epub 2017 Jul 24. ACS Chem Neurosci. 2017. PMID: 28691794 Free PMC article.
Designed Spiroketal Protein Modulation.
Scheepstra M, Andrei SA, Unver MY, Hirsch AKH, Leysen S, Ottmann C, Brunsveld L, Milroy LG. Scheepstra M, et al. Angew Chem Int Ed Engl. 2017 May 8;56(20):5480-5484. doi: 10.1002/anie.201612504. Epub 2017 Apr 13. Angew Chem Int Ed Engl. 2017. PMID: 28407400 Free PMC article.
Identification of an allosteric binding site for RORγt inhibition.
Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L. Scheepstra M, et al. Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833. Nat Commun. 2015. PMID: 26640126 Free PMC article.
Bivalent Ligands for Protein Degradation in Drug Discovery.
Scheepstra M, Hekking KFW, van Hijfte L, Folmer RHA. Scheepstra M, et al. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176. doi: 10.1016/j.csbj.2019.01.006. eCollection 2019. Comput Struct Biotechnol J. 2019. PMID: 30788082 Free PMC article. Review.
Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.
Hekking KFW, Maroto S, van Kekem K, Haasjes FS, Slootweg JC, Oude Alink PGB, Dirks R, Sardana M, Bolster MG, Kuijpers B, Smith D, Doodeman R, Scheepstra M, Zech B, Mulvihill M, Renzetti LM, Babiss L, Centrella PA, Clark MA, Cuozzo JW, Guié MA, Sigel E, Habeshian S, Hupp CD, Liu J, Thomson HA, Zhang Y, Keefe AD, Müller G, Gremmen S. Hekking KFW, et al. Among authors: scheepstra m. J Med Chem. 2024 Feb 22;67(4):3039-3065. doi: 10.1021/acs.jmedchem.3c02206. Epub 2024 Feb 2. J Med Chem. 2024. PMID: 38306405