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Page 1
Structures, functions and adaptations of the human LINE-1 ORF2 protein.
Baldwin ET, van Eeuwen T, Hoyos D, Zalevsky A, Tchesnokov EP, Sánchez R, Miller BD, Di Stefano LH, Ruiz FX, Hancock M, Işik E, Mendez-Dorantes C, Walpole T, Nichols C, Wan P, Riento K, Halls-Kass R, Augustin M, Lammens A, Jestel A, Upla P, Xibinaku K, Congreve S, Hennink M, Rogala KB, Schneider AM, Fairman JE, Christensen SM, Desrosiers B, Bisacchi GS, Saunders OL, Hafeez N, Miao W, Kapeller R, Zaller DM, Sali A, Weichenrieder O, Burns KH, Götte M, Rout MP, Arnold E, Greenbaum BD, Romero DL, LaCava J, Taylor MS. Baldwin ET, et al. Among authors: jestel a. Nature. 2024 Feb;626(7997):194-206. doi: 10.1038/s41586-023-06947-z. Epub 2023 Dec 14. Nature. 2024. PMID: 38096902 Free PMC article.
Mediator kinase inhibition further activates super-enhancer-associated genes in AML.
Pelish HE, Liau BB, Nitulescu II, Tangpeerachaikul A, Poss ZC, Da Silva DH, Caruso BT, Arefolov A, Fadeyi O, Christie AL, Du K, Banka D, Schneider EV, Jestel A, Zou G, Si C, Ebmeier CC, Bronson RT, Krivtsov AV, Myers AG, Kohl NE, Kung AL, Armstrong SA, Lemieux ME, Taatjes DJ, Shair MD. Pelish HE, et al. Among authors: jestel a. Nature. 2015 Oct 8;526(7572):273-276. doi: 10.1038/nature14904. Epub 2015 Sep 28. Nature. 2015. PMID: 26416749 Free PMC article.
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG. Crawford JJ, et al. Among authors: jestel a. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, MacFaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C. Dossetter AG, et al. Among authors: jestel a. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5563-8. doi: 10.1016/j.bmcl.2012.07.012. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858142
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M. Dossetter AG, et al. Among authors: jestel a. J Med Chem. 2012 Jul 26;55(14):6363-74. doi: 10.1021/jm3007257. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22742641
High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.
Fradera X, Kazemier B, Carswell E, Cooke A, Oubrie A, Hamilton W, Dempster M, Krapp S, Nagel S, Jestel A. Fradera X, et al. Among authors: jestel a. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Apr 1;68(Pt 4):404-8. doi: 10.1107/S1744309112009037. Epub 2012 Mar 27. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012. PMID: 22505407 Free PMC article.
Phosphorylation of the human full-length protein kinase Ciota.
Macek B, Benda C, Jestel A, Maskos K, Mann M, Messerschmidt A. Macek B, et al. Among authors: jestel a. J Proteome Res. 2008 Jul;7(7):2928-35. doi: 10.1021/pr800052z. Epub 2008 May 20. J Proteome Res. 2008. PMID: 18489133
Macrocyclic statine-based inhibitors of BACE-1.
Barazza A, Götz M, Cadamuro SA, Goettig P, Willem M, Steuber H, Kohler T, Jestel A, Reinemer P, Renner C, Bode W, Moroder L. Barazza A, et al. Among authors: jestel a. Chembiochem. 2007 Nov 23;8(17):2078-91. doi: 10.1002/cbic.200700383. Chembiochem. 2007. PMID: 17963207
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