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A small molecule inhibitor of HER3: a proof-of-concept study.
Colomba A, Fitzek M, George R, Weitsman G, Roberts S, Zanetti-Domingues L, Hirsch M, Rolfe DJ, Mehmood S, Madin A, Claus J, Kjaer S, Snijders AP, Ng T, Martin-Fernandez M, Smith DM, Parker PJ. Colomba A, et al. Among authors: fitzek m. Biochem J. 2020 Sep 18;477(17):3329-3347. doi: 10.1042/BCJ20200496. Biochem J. 2020. PMID: 32815546 Free PMC article.
A small-molecule PI3Kα activator for cardioprotection and neuroregeneration.
Gong GQ, Bilanges B, Allsop B, Masson GR, Roberton V, Askwith T, Oxenford S, Madsen RR, Conduit SE, Bellini D, Fitzek M, Collier M, Najam O, He Z, Wahab B, McLaughlin SH, Chan AWE, Feierberg I, Madin A, Morelli D, Bhamra A, Vinciauskaite V, Anderson KE, Surinova S, Pinotsis N, Lopez-Guadamillas E, Wilcox M, Hooper A, Patel C, Whitehead MA, Bunney TD, Stephens LR, Hawkins PT, Katan M, Yellon DM, Davidson SM, Smith DM, Phillips JB, Angell R, Williams RL, Vanhaesebroeck B. Gong GQ, et al. Among authors: fitzek m. Nature. 2023 Jun;618(7963):159-168. doi: 10.1038/s41586-023-05972-2. Epub 2023 May 24. Nature. 2023. PMID: 37225977 Free PMC article.
Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel.
Hancox U, Cosulich S, Hanson L, Trigwell C, Lenaghan C, Ellston R, Dry H, Crafter C, Barlaam B, Fitzek M, Smith PD, Ogilvie D, D'Cruz C, Castriotta L, Wedge SR, Ward L, Powell S, Lawson M, Davies BR, Harrington EA, Foster E, Cumberbatch M, Green S, Barry ST. Hancox U, et al. Among authors: fitzek m. Mol Cancer Ther. 2015 Jan;14(1):48-58. doi: 10.1158/1535-7163.MCT-14-0406. Epub 2014 Nov 14. Mol Cancer Ther. 2015. PMID: 25398829
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Giordanetto F, Green S, Inghardt T, Hennequin L, Hancox U, Lambert-van der Brempt C, Morgentin R, Pass S, Plé P, Saleh T, Ward L. Barlaam B, et al. Among authors: fitzek m. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3928-35. doi: 10.1016/j.bmcl.2014.06.040. Epub 2014 Jun 21. Bioorg Med Chem Lett. 2014. PMID: 24992874
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N. Barlaam B, et al. Among authors: fitzek m. J Med Chem. 2015 Jan 22;58(2):943-62. doi: 10.1021/jm501629p. Epub 2015 Jan 7. J Med Chem. 2015. PMID: 25514658
59 results