P
Philip Jones
Researcher at Merck & Co.
Publications - 77
Citations - 3452
Philip Jones is an academic researcher from Merck & Co.. The author has contributed to research in topics: Histone deacetylase & Poly ADP ribose polymerase. The author has an hindex of 25, co-authored 77 publications receiving 3205 citations. Previous affiliations of Philip Jones include United States Military Academy & Organon International.
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Journal ArticleDOI
Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
Vincenzo Summa,Alessia Petrocchi,Fabio Bonelli,Benedetta Crescenzi,Monica Donghi,Marco Ferrara,Fabrizio Fiore,Cristina Gardelli,Odalys Gonzalez Paz,Daria J. Hazuda,Philip Jones,Olaf Kinzel,Ralph Laufer,Edith Monteagudo,Ester Muraglia,Emanuela Nizi,Federica Orvieto,Paola Pace,Giovanna Pescatore,Rita Scarpelli,Kara A. Stillmock,Marc V. Witmer,Michael Rowley +22 more
TL;DR: The discovery of Raltegravir is reported, the first HIV-integrase inhibitor approved by FDA for the treatment of HIV infection, which derives from the evolution of 5,6-dihydroxypyrimidine-4-carboxamides and N-methyl- 4-hydroxypyridinone-car boxamides, which exhibited potent inhibition of the HIV-Integrase catalyzed strand transfer process.
Journal ArticleDOI
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
Armin Lahm,Chantal Paolini,Michele Pallaoro,Maria Chiara Nardi,Philip Jones,Petra Neddermann,Sonia Sambucini,Matthew J. Bottomley,P. Lo Surdo,Andrea Carfi,Uwe Koch,R. De Francesco,Christian Steinkühler,Paola Gallinari +13 more
TL;DR: Evidence is presented supporting the view that vertebrate class IIa HDACs may have evolved to maintain low basal activities on acetyl-lysines and to efficiently process restricted sets of specific, still undiscovered natural substrates.
Journal ArticleDOI
Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain
Matthew J. Bottomley,Paola Lo Surdo,Paolo Di Giovine,Agostino Cirillo,Rita Scarpelli,Federica Ferrigno,Philip Jones,Petra Neddermann,Raffaele De Francesco,Christian Steinkühler,Paola Gallinari,Andrea Carfi +11 more
TL;DR: The structures presented provide the molecular basis for the intrinsically low enzymatic activity of class IIa HDACs toward acetylated lysines and reveal active site features that may guide the design of class-specific inhibitors.
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Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Philip Jones,Sergio Altamura,Julia K. Boueres,Federica Ferrigno,Massimiliano Fonsi,Claudia Giomini,Stefania Lamartina,Edith Monteagudo,Jesus Maria Ontoria Ontoria,Maria Vittoria Orsale,Maria Cecilia Palumbi,Silvia Pesci,Giuseppe Roscilli,Rita Scarpelli,Carsten Schultz-Fademrecht,Carlo Toniatti,Michael Rowley +16 more
TL;DR: Compound 56, a novel series of 2-phenyl-2H-indazole-7-carboxamides as poly(ADP-ribose)polymerase (PARP) 1 and 2 inhibitors, displays good pharmacokinetic properties and is currently in phase I clinical trials.
Journal ArticleDOI
Substrate binding to histone deacetylases as shown by the crystal structure of the HDAC8-substrate complex.
Alessandro Vannini,Cinzia Volpari,Paola Gallinari,Philip Jones,Marco Mattu,Andrea Carfi,Raffaele De Francesco,Christian Steinkühler,Stefania Di Marco +8 more
TL;DR: The structure clarifies the role of active‐ site residues in the deacetylation reaction and substrate recognition and shows the unexpected role of a conserved residue at the active‐site rim, Asp 101, in positioning the substrate by directly interacting with the peptidic backbone and imposing a constrained cis‐conformation.