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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: pelle x. Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22. Nature. 2017. PMID: 28329763
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: pelle x. 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
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. Among authors: pelle x. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Jahnke W, Rondeau JM, Cotesta S, Marzinzik A, Pellé X, Geiser M, Strauss A, Götte M, Bitsch F, Hemmig R, Henry C, Lehmann S, Glickman JF, Roddy TP, Stout SJ, Green JR. Jahnke W, et al. Among authors: pelle x. Nat Chem Biol. 2010 Sep;6(9):660-6. doi: 10.1038/nchembio.421. Epub 2010 Aug 15. Nat Chem Biol. 2010. PMID: 20711197
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. Among authors: pelle x. 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: pelle x. 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
Identification of a PCSK9-LDLR disruptor peptide with in vivo function.
Brousseau ME, Clairmont KB, Spraggon G, Flyer AN, Golosov AA, Grosche P, Amin J, Andre J, Burdick D, Caplan S, Chen G, Chopra R, Ames L, Dubiel D, Fan L, Gattlen R, Kelly-Sullivan D, Koch AW, Lewis I, Li J, Liu E, Lubicka D, Marzinzik A, Nakajima K, Nettleton D, Ottl J, Pan M, Patel T, Perry L, Pickett S, Poirier J, Reid PC, Pelle X, Seepersaud M, Subramanian V, Vera V, Xu M, Yang L, Yang Q, Yu J, Zhu G, Monovich LG. Brousseau ME, et al. Among authors: pelle x. Cell Chem Biol. 2022 Feb 17;29(2):249-258.e5. doi: 10.1016/j.chembiol.2021.08.012. Epub 2021 Sep 20. Cell Chem Biol. 2022. PMID: 34547225 Free article.