M. Fitzek

发表

Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.

J. Nissink, G. Walker, R. Ducray, 2011, Bioorganic & medicinal chemistry letters.

A small molecule inhibitor of HER3: a proof-of-concept study

Laura C. Zanetti-Domingues, Laura C Zanetti-Domingues, David M. Smith, 2020, Biochemical Journal.

Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.

S. Green, B. Barlaam, S. Cosulich, 2015, Bioorganic & medicinal chemistry letters.

Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition

D. M. Smith, David M. Smith, N. Selmi, 2020, Cell Death Discovery.

Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.

S. Emery, C. Forder, D. Buttar, 2008, Bioorganic & medicinal chemistry letters.

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.

S. Green, B. Barlaam, S. Degorce, 2014, Bioorganic & medicinal chemistry letters.

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.

S. Green, Rebecca P A Ellston, B. Barlaam, 2017, Bioorganic & medicinal chemistry letters.

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.

S. Green, B. Barlaam, S. Degorce, 2016, Bioorganic & medicinal chemistry letters.

Abstract 3264: AZD8186: a potent selective inhibitor of PI3Kβ targeting PTEN-deficient tumours dependent on dysregulated PI3Kβ signalling.

S. Barry, S. Green, Rebecca P A Ellston, 2013 .

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.

S. Green, B. Barlaam, S. Degorce, 2015, Journal of medicinal chemistry.

Inhibition of PI3Kβ Signaling with AZD8186 Inhibits Growth of PTEN-Deficient Breast and Prostate Tumors Alone and in Combination with Docetaxel

S. Barry, Paul D. Smith, E. Harrington, 2014, Molecular Cancer Therapeutics.

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.

S. Green, Rebecca P A Ellston, B. Barlaam, 2015, Bioorganic & medicinal chemistry letters.

A phenotypic screen of Marfan syndrome iPSC-derived vascular smooth muscle cells uncovers GSK3β as a new target

David M. Smith, S. Sinha, Anne Child, 2022, bioRxiv.

Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.

S. Green, B. Barlaam, S. Cosulich, 2017, Bioorganic & medicinal chemistry letters.

Pluripotent Stem Cell-Derived Hepatocytes Phenotypic Screening Reveals Small Molecules Targeting the CDK2/4-C/EBPα/DGAT2 Pathway Preventing ER-Stress Induced Lipid Accumulation

Preeti Iyer, O. Engkvist, David M. Smith, 2020, International journal of molecular sciences.

A small molecule PI3Kα activator for cardioprotection and neuroregeneration

Ralitsa R. Madsen, Roger L. Williams, P. Hawkins, 2023, Nature.

Abstract 2830: Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment ofPIK3CA-dependent cancers

S. Green, R. Morgentin, S. Cosulich, 2015 .

Inhibition of PI3Kβ Signaling with AZD8186 Inhibits Growth of PTEN-Deficient Breast and Prostate Tumors Alone and in Combination with Docetaxel

S. Barry, Paul D. Smith, E. Harrington, 2014, Molecular Cancer Therapeutics.