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M. Fitzek · SciRah

Researcher profile · Semantic Scholar

M. Fitzek

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M. Fitzek — researcher profile on SciRah

h-index: 9
Works: 26
Citations: 463

Most-cited papers

A small molecule PI3Kα activator for cardioprotection and neuroregeneration
G. Q. Gong, B. Bilanges, Ben Allsop, G. Masson +37 more
2023Nature110 citations Open access
Semantic Scholar
Inhibition of PI3Kβ Signaling with AZD8186 Inhibits Growth of PTEN-Deficient Breast and Prostate Tumors Alone and in Combination with Docetaxel
Urs J Hancox, S. Cosulich, Lyndsey Hanson, C. Trigwell +20 more
2014Molecular Cancer Therapeutics83 citations Open access
Semantic Scholar
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.
B. Barlaam, S. Cosulich, S. Degorce, M. Fitzek +14 more
2015Journal of Medicinal Chemistry79 citations Open access
Semantic Scholar
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
R. Ducray, Iain Simpson, F. Jung, J. M. Nissink +5 more
2011Bioorganic & Medicinal Chemistry Letters44 citations Open access
Semantic Scholar
Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
B. Barlaam, S. Cosulich, Bénédicte Delouvrié, Rebecca P A Ellston +20 more
2015Bioorganic & Medicinal Chemistry Letters41 citations
Semantic Scholar
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.
B. Barlaam, S. Cosulich, S. Degorce, M. Fitzek +11 more
2014Bioorganic & Medicinal Chemistry Letters19 citations Open access
Semantic Scholar
Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition
Hugo Brito, Vanda Marques, M. B. Afonso, Dean G. Brown +9 more
2020Cell Death Discovery17 citations Open access
Semantic Scholar
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.
B. Barlaam, S. Cosulich, M. Fitzek, S. Green +8 more
2015Bioorganic & Medicinal Chemistry Letters11 citations Open access
Semantic Scholar
A small molecule inhibitor of HER3: a proof-of-concept study
A. Colomba, M. Fitzek, R. George, G. Weitsman +13 more
2020Biochemical Journal10 citations Open access
Semantic Scholar
Pluripotent Stem Cell-Derived Hepatocytes Phenotypic Screening Reveals Small Molecules Targeting the CDK2/4-C/EBPα/DGAT2 Pathway Preventing ER-Stress Induced Lipid Accumulation
Maddalena Parafati, S. Bae, R. J. Kirby, M. Fitzek +4 more
2020International Journal of Molecular Sciences8 citations Open access
Semantic Scholar
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.
B. Barlaam, S. Cosulich, M. Fitzek, Hervé Germain +13 more
2017Bioorganic & Medicinal Chemistry Letters8 citations Open access
Semantic Scholar
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
B. Barlaam, S. Cosulich, S. Degorce, M. Fitzek +11 more
2016Bioorganic & Medicinal Chemistry Letters7 citations Open access
Semantic Scholar
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.
D. Buttar, Mike Edge, Steve C Emery, M. Fitzek +9 more
2008Bioorganic & Medicinal Chemistry Letters7 citations Open access
Semantic Scholar
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
B. Barlaam, S. Cosulich, S. Degorce, Rebecca P A Ellston +10 more
2017Bioorganic & Medicinal Chemistry Letters5 citations Open access
Semantic Scholar
Overcoming Obstacles in the Implementation of Factorial Design for Assay Optimization
Robert J. Shaw, M. Fitzek, E. Mouchet, Graeme Walker +1 more
2015Assay and drug development technologies5 citations
Semantic Scholar
Fragment-Based Screening Identifies New Quinazolinone-Based Inositol Hexakisphosphate Kinase (IP6K) Inhibitors.
Tyler Heitmann, Gangling Liao, P. de León, Glen E. Ernst +8 more
2023ACS Medicinal Chemistry Letters4 citations Open access
Semantic Scholar
Abstract 3264: AZD8186: a potent selective inhibitor of PI3Kβ targeting PTEN-deficient tumours dependent on dysregulated PI3Kβ signalling.
Urs J Hancox, S. Cosulich, H. Dry, L. Hanson +12 more
20133 citations
Semantic Scholar
PI 3 Kβ / δ inhibitors for the treatment of PTEN-deficient tumours
B. Barlaam, S. Cosulich, S. Degorce, Rebecca P A Ellston +11 more
20171 citations
Semantic Scholar
Osimertinib (AZD9291), an irreversible 3rd generation TKI, induces tumor growth inhibition in NSCLC pre-clinical models harboring the most prevalent EGFR Ex20Ins (in vitro and in vivo)
R. Ward, S. Ashton, Ambra Bianco, N. Colclough +13 more
20161 citations
Semantic Scholar
Abstract 2830: Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment ofPIK3CA-dependent cancers
Barlaam Bernard Christophe, S. Cosulich, Bénédicte Delouvrié, M. Fitzek +15 more
20151 citations
Semantic Scholar
SCREENING FOR SMALL MOLECULE REGULATORS OF THE CREATINE TRANSPORTER (SLC6A8)
S. Zervou, H. A. Lake, M. Fitzek, M. Collier +5 more
20200 citations
Semantic Scholar
Abstract 4813: Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR)
R. Ward, Ambra Bianco, N. Colclough, D. Cross +15 more
2019Experimental and Molecular Therapeutics0 citations
Semantic Scholar
Discovery and validation of new modulators of necroptosis using phenotypic high throughput screening of a large compound library
H. M. de Sousa Brito, Vanda Marques, M. B. Afonso, Dean G. Brown +4 more
20180 citations
Semantic Scholar
272 8-(1-Anilino)ethyl)-2-morpholino-4-oxo-4H-chromene-6-carboxamides as PI3Kbeta/delta inhibitors: structure–activity relationships and identification of AZD8186, a clinical candidate for the treatment of PTEN deficient tumours
B. Barlaam, S. Cosulich, S. Degorce, M. Fitzek +14 more
20140 citations
Semantic Scholar
Abstract B238: Novel imidazo[1,2-a]pyridines as inhibitors of the IGF-1R tyrosine kinase.
R. Ducray, Iain Simpson, C. Jones, J. Curwen +7 more
20110 citations
Semantic Scholar
Structure of the Tie2 kinase domain in complex with a thiazolopyrimidine inhibitor
C. Brassington, J. Breed, D. Buttar, M. Fitzek +12 more
20090 citations
Semantic Scholar

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