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Page 1
The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
Wylie AA, Schoepfer J, Jahnke W, Cowan-Jacob SW, Loo A, Furet P, Marzinzik AL, Pelle X, Donovan J, Zhu W, Buonamici S, Hassan AQ, Lombardo F, Iyer V, Palmer M, Berellini G, Dodd S, Thohan S, Bitter H, Branford S, Ross DM, Hughes TP, Petruzzelli L, Vanasse KG, Warmuth M, Hofmann F, Keen NJ, Sellers WR. Wylie AA, et al. Among authors: marzinzik al. Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22. Nature. 2017. PMID: 28329763
Library design for fragment based screening.
Schuffenhauer A, Ruedisser S, Marzinzik AL, Jahnke W, Blommers M, Selzer P, Jacoby E. Schuffenhauer A, et al. Among authors: marzinzik al. Curr Top Med Chem. 2005;5(8):751-62. doi: 10.2174/1568026054637700. Curr Top Med Chem. 2005. PMID: 16101415 Review.
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J. Fabbro D, et al. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I, Guerro-Lagasse S, Gutmann S, Hinh L, Jahnke W, Klopp J, Lai A, Lindvall MK, Ma S, Möbitz H, Pecchi S, Rummel G, Shoemaker K, Trappe J, Voliva C, Cowan-Jacob SW, Marzinzik AL. Karpov AS, et al. Among authors: marzinzik al. ACS Med Chem Lett. 2015 May 22;6(7):776-81. doi: 10.1021/acsmedchemlett.5b00102. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191365 Free PMC article.
Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding.
Marzinzik AL, Amstutz R, Bold G, Bourgier E, Cotesta S, Glickman JF, Götte M, Henry C, Lehmann S, Hartwieg JC, Ofner S, Pellé X, Roddy TP, Rondeau JM, Stauffer F, Stout SJ, Widmer A, Zimmermann J, Zoller T, Jahnke W. Marzinzik AL, et al. ChemMedChem. 2015 Nov;10(11):1884-91. doi: 10.1002/cmdc.201500338. Epub 2015 Sep 18. ChemMedChem. 2015. PMID: 26381451
A General Strategy for Targeting Drugs to Bone.
Jahnke W, Bold G, Marzinzik AL, Ofner S, Pellé X, Cotesta S, Bourgier E, Lehmann S, Henry C, Hemmig R, Stauffer F, Hartwieg JC, Green JR, Rondeau JM. Jahnke W, et al. Among authors: marzinzik al. Angew Chem Int Ed Engl. 2015 Nov 23;54(48):14575-9. doi: 10.1002/anie.201507064. Epub 2015 Oct 12. Angew Chem Int Ed Engl. 2015. PMID: 26457482
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: marzinzik al. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
28 results