M
Marketa Zvelebil
Researcher at Institute of Cancer Research
Publications - 94
Citations - 10713
Marketa Zvelebil is an academic researcher from Institute of Cancer Research. The author has contributed to research in topics: Kinase & Breast cancer. The author has an hindex of 47, co-authored 94 publications receiving 10152 citations. Previous affiliations of Marketa Zvelebil include Birkbeck, University of London & Queen's University Belfast.
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Journal ArticleDOI
The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer†
Adrian Folkes,Khatereh Ahmadi,Wendy K. Alderton,Sonia Alix,Stewart J. Baker,Gary Box,Irina Chuckowree,Paul A. Clarke,Paul Depledge,Suzanne A. Eccles,Lori Friedman,Angela Hayes,Timothy Hancox,Arumugam Kugendradas,Letitia Lensun,Pauline Moore,Olivero Alan G,Jodie Pang,Sonal Patel,Giles Pergl-Wilson,Florence I. Raynaud,Anthony Robson,Nahid Saghir,Laurent Salphati,Sukhjit Sohal,Mark H. Ultsch,Melanie Valenti,Heidi J.A. Wallweber,Nan Chi Wan,Christian Wiesmann,Paul Workman,Alexander Zhyvoloup,Marketa Zvelebil,Stephen J. Shuttleworth +33 more
TL;DR: Thieno[3,2-d]pyrimidine derivatives prepared and evaluated as inhibitors of PI3 kinase p110alpha resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor ofPI3K and is currently being evaluated in human clinical trials for the treatment of cancer.
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Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction.
Matthias P. Wymann,Ginette Bulgarelli-Leva,Marketa Zvelebil,Luciano Pirola,Bart Vanhaesebroeck,Michael D. Waterfield,George Panayotou +6 more
TL;DR: The identification of the site of interaction of wortmannin on the catalytic subunit of PI 3-kinase, p110alpha is reported, providing the basis for the design of novel and specific inhibitors of an enzyme family, including PI kinases and ATM-related genes, that play a central role in many physiological processes.
Journal ArticleDOI
Distinct specificity in the recognition of phosphoinositides by the pleckstrin homology domains of dynamin and Bruton's tyrosine kinase.
Kamran Salim,M J Bottomley,E Querfurth,Marketa Zvelebil,Ivan Gout,R Scaife,Robert L. Margolis,R Gigg,C. I. E. Smith,Paul C. Driscoll,Mike Waterfield,George Panayotou +11 more
TL;DR: A biosensor‐based assay was used here to probe interactions between PH domains and unilamellar liposomes containing different phospholipids and to demonstrate specificity for distinct phosphoinositides.
Journal ArticleDOI
Prediction of protein secondary structure and active sites using the alignment of homologous sequences.
TL;DR: From the sequence conservation and the predicted secondary structure, many active site regions of enzymes can be located and the entire algorithm is fully automatic and is applicable to all structural classes of globular proteins.
Journal ArticleDOI
Phosphoinositide 3-kinase signalling – which way to target?
TL;DR: Mechanistic data and mouse phenotypic analyses are summarised, and the possible success of therapeutic inhibition of distinct PI3K isoforms is discussed.