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Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function.
Coleman OD, Macdonald J, Thomson B, Ward JA, Stubbs CJ, McAllister TE, Clark S, Amin S, Cao Y, Abboud MI, Zhang Y, Sanganee H, Huber KVM, Claridge TDW, Kawamura A. Coleman OD, et al. Among authors: stubbs cj. Chem Sci. 2023 Apr 17;14(26):7136-7146. doi: 10.1039/d2sc05944d. eCollection 2023 Jul 5. Chem Sci. 2023. PMID: 37416723 Free PMC article.
Specific inhibition of CK2α from an anchor outside the active site.
Brear P, De Fusco C, Hadje Georgiou K, Francis-Newton NJ, Stubbs CJ, Sore HF, Venkitaraman AR, Abell C, Spring DR, Hyvönen M. Brear P, et al. Among authors: stubbs cj. Chem Sci. 2016 Nov 1;7(11):6839-6845. doi: 10.1039/c6sc02335e. Epub 2016 Jul 12. Chem Sci. 2016. PMID: 28451126 Free PMC article.
Combining structural and coevolution information to unveil allosteric sites.
La Sala G, Pfleger C, Käck H, Wissler L, Nevin P, Böhm K, Janet JP, Schimpl M, Stubbs CJ, De Vivo M, Tyrchan C, Hogner A, Gohlke H, Frolov AI. La Sala G, et al. Among authors: stubbs cj. Chem Sci. 2023 Jun 8;14(25):7057-7067. doi: 10.1039/d2sc06272k. eCollection 2023 Jun 28. Chem Sci. 2023. PMID: 37389247 Free PMC article.
KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe.
Bery N, Legg S, Debreczeni J, Breed J, Embrey K, Stubbs C, Kolasinska-Zwierz P, Barrett N, Marwood R, Watson J, Tart J, Overman R, Miller A, Phillips C, Minter R, Rabbitts TH. Bery N, et al. Nat Commun. 2019 Jun 13;10(1):2607. doi: 10.1038/s41467-019-10419-2. Nat Commun. 2019. PMID: 31197133 Free PMC article.
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
De Fusco C, Schimpl M, Börjesson U, Cheung T, Collie I, Evans L, Narasimhan P, Stubbs C, Vazquez-Chantada M, Wagner DJ, Grondine M, Sanders MG, Tentarelli S, Underwood E, Argyrou A, Smith JM, Lynch JT, Chiarparin E, Robb G, Bagal SK, Scott JS. De Fusco C, et al. J Med Chem. 2021 May 27;64(10):6814-6826. doi: 10.1021/acs.jmedchem.1c00067. Epub 2021 Apr 26. J Med Chem. 2021. PMID: 33900758 Free article.
Discovery of a selective c-MET inhibitor with a novel binding mode.
Collie GW, Barlind L, Bazzaz S, Börjesson U, Dale IL, Disch JS, Habeshian S, Jetson R, Khurana P, Madin A, Michaelides IN, Peng L, Snijder A, Stubbs CJ. Collie GW, et al. Among authors: stubbs cj. Bioorg Med Chem Lett. 2022 Nov 1;75:128948. doi: 10.1016/j.bmcl.2022.128948. Epub 2022 Aug 17. Bioorg Med Chem Lett. 2022. PMID: 35987508 Free article.
48 results