P
Panagis Filippakopoulos
Researcher at Structural Genomics Consortium
Publications - 140
Citations - 15219
Panagis Filippakopoulos is an academic researcher from Structural Genomics Consortium. The author has contributed to research in topics: Bromodomain & Kinase. The author has an hindex of 52, co-authored 136 publications receiving 13021 citations. Previous affiliations of Panagis Filippakopoulos include University of Oxford & Ludwig Institute for Cancer Research.
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Journal ArticleDOI
Selective inhibition of BET bromodomains.
Panagis Filippakopoulos,Jun Qi,Sarah Picaud,Yao Shen,William B. Smith,Oleg Fedorov,Elizabeth M. Morse,T. Keates,Tyler T. Hickman,I. Felletar,Martin Philpott,Shonagh Munro,Michael R. McKeown,Yuchuan Wang,Amanda L. Christie,Nathan West,Michael J. Cameron,Brian E. Schwartz,Tom D. Heightman,Nicholas B. La Thangue,Christopher A. French,Olaf Wiest,Andrew L. Kung,Stefan Knapp,Stefan Knapp,James E. Bradner +25 more
TL;DR: A cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains is reported, establishing proof-of-concept for targeting protein–protein interactions of epigenetic ‘readers’, and providing a versatile chemical scaffold for the development of chemical probes more broadly throughout the b romodomain family.
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Histone recognition and large-scale structural analysis of the human bromodomain family.
Panagis Filippakopoulos,Sarah Picaud,Maria M. Mangos,T. Keates,Jean-Philippe Lambert,Dalia Barsyte-Lovejoy,I. Felletar,Rudolf Volkmer,Susanne Müller,Tony Pawson,Anne-Claude Gingras,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Stefan Knapp,Stefan Knapp,Stefan Knapp +15 more
TL;DR: Bromodomains are protein interaction modules that specifically recognize ε-N-lysine acetylation motifs, a key event in the reading process of epigenetic marks, and a structural mechanism for the simultaneous binding and recognition of diverse diacetyl-containing peptides by BRD4 is uncovered.
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Targeting bromodomains: epigenetic readers of lysine acetylation
TL;DR: Recent progress in the development of bromodomain inhibitors is highlighted, and their potential applications in drug discovery are highlighted.
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Large-Scale Structural Analysis of the Classical Human Protein Tyrosine Phosphatome
Alastair J. Barr,E. Ugochukwu,Wen Hwa Lee,Oliver N. King,Panagis Filippakopoulos,I. Alfano,Pavel Savitsky,N.A. Burgess-Brown,Susanne Müller,Stefan Knapp,Stefan Knapp +10 more
TL;DR: 22 human PTP crystal structures are presented that enable a comprehensive analysis of the classical PTP family and a “head-to-toe” dimerization model for RPTPγ/ζ is proposed that is distinct from the “inhibitory wedge” model and provides a molecular basis for inhibitory regulation.
Journal ArticleDOI
Bromodomains as therapeutic targets.
TL;DR: It is likely that BRDs will emerge alongside HATs and HDACs as interesting targets for drug development for the large number of diseases that are caused by aberrant acetylation of lysine residues.