Philip D. Jones

发表

An inhibitor of oxidative phosphorylation exploits cancer vulnerability

M. Protopopova, R. DePinho, M. Konopleva, 2018, Nature Medicine.

Inhibition of dual leucine zipper kinase prevents chemotherapy-induced peripheral neuropathy and cognitive impairments

S. Kesler, Bo Peng, F. Mseeh, 2021, Pain.

Dual Leucine Zipper Kinase Is Constitutively Active in the Adult Mouse Brain and Has Both Stress-Induced and Homeostatic Functions

Philip Jones, M. Soth, W. Ray, 2020, International journal of molecular sciences.

Homeostatic versus pathological functions of Dual Leucine Zipper Kinase in the adult mouse brain

R. Al-ouran, Philip Jones, M. Soth, 2018, bioRxiv.

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.

R. De Francesco, S. Altamura, M. Rowley, 2008, Bioorganic & medicinal chemistry letters.

Inhibition of class I histone deacetylase with an apicidin derivative prevents cardiac hypertrophy and failure.

M. Todaro, G. Ciliberto, M. Latronico, 2008, Cardiovascular research.

Substrate binding to histone deacetylases as shown by the crystal structure of the HDAC8–substrate complex

R. De Francesco, A. Vannini, A. Carfi, 2007, EMBO reports.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

D. Hazuda, M. Rowley, V. Summa, 2008, Journal of medicinal chemistry.

Optimization of a series of potent and selective ketone histone deacetylase inhibitors.

M. Rowley, Philip Jones, C. Steinkühler, 2008, Bioorganic & medicinal chemistry letters.

Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain*

M. Bottomley, R. De Francesco, A. Carfi, 2008, Journal of Biological Chemistry.

N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.

M. Rowley, V. Summa, A. Petrocchi, 2009, Bioorganic & medicinal chemistry letters.

Inhibition of class I histone deacetylase with an apicidin derivative prevents cardiac hypertrophy and failure.

M. Todaro, G. Ciliberto, M. Latronico, 2008, Cardiovascular research.

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

M. Rowley, Philip Jones, C. Steinkühler, 2009, Journal of medicinal chemistry.

PISA, a novel pharmacodynamic assay for assessing poly(ADP-ribose) polymerase (PARP) activity in situ.

S. Browne, L. Lubbers, I. Reynolds, 2010, Journal of pharmacological and toxicological methods.

Development of Poly(ADP-Ribose)Polymerase (PARP) Inhibitors in Oncology

Philip Jones, Philip D. Jones, 2010 .

Metabolic reprogramming toward oxidative phosphorylation identifies a therapeutic target for mantle cell lymphoma

Michael L. Wang, Shaojun Zhang, Guangchun Han, 2019, Science Translational Medicine.

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.

Parantu K. Shah, A. Protopopov, B. Vangamudi, 2015, Cancer research.

Smoothened antagonists: a promising new class of antitumor agents

S. Pazzaglia, Philip Jones, P. Gallinari, 2009, Expert opinion on drug discovery.

Smoothenedantagonists: apromisingnewclassof antitumoragents

S. Pazzaglia, Philip Jones, P. Gallinari, 2009 .

In Vivo Functional Platform Targeting Patient-Derived Xenografts Identifies WDR5-Myc Association as a Critical Determinant of Pancreatic Cancer.

Parantu K. Shah, Nora S. Sanchez, L. Chin, 2016, Cell reports.

Development of second generation epigenetic agents

Philip Jones, Philip D. Jones, 2012 .

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.

M. Rowley, Philip Jones, C. Steinkühler, 2011, Bioorganic & medicinal chemistry letters.

Identification of potent and selective MTH1 inhibitors.

F. Mseeh, C. Toniatti, G. Draetta, 2005, Bioorganic & Medicinal Chemistry Letters.

2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.

M. Bottomley, M. Rowley, A. Carfi, 2008, Bioorganic & medicinal chemistry letters.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.

R. De Francesco, S. Altamura, M. Rowley, 2008, Journal of medicinal chemistry.

A series of novel, potent, and selective histone deacetylase inhibitors.

Michael Rowley, R. De Francesco, S. Altamura, 2006, Bioorganic & medicinal chemistry letters.

Histone Deacetylase Inhibitors

Philip Jones, Philip D. Jones, 2009 .

2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.

S. Altamura, M. Rowley, Philip Jones, 2008, Bioorganic & medicinal chemistry letters.

Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.

S. Altamura, M. Rowley, R. Laufer, 2009, Journal of medicinal chemistry.

Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.

M. Rowley, R. Laufer, Philip Jones, 2008, Bioorganic & medicinal chemistry letters.

Genetic events that limit the efficacy of MEK and RTK inhibitor therapies in a mouse model of KRAS-driven pancreatic cancer.

Parantu K. Shah, Nora S. Sanchez, G. Mills, 2015, Cancer research.

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

M. Rowley, C. Giuliano, Philip Jones, 2011, Bioorganic & medicinal chemistry letters.

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.

J. I. Hernando, S. Altamura, M. Rowley, 2011, Bioorganic & medicinal chemistry letters.

Phase I trial of IACS-010759 (IACS), a potent, selective inhibitor of complex I of the mitochondrial electron transport chain, in patients (pts) with advanced solid tumors.

F. Meric-Bernstam, F. Janku, A. Naing, 2019, Journal of Clinical Oncology.

Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors

Chien-Liang Liu, Morag Park, Hirohito Yamaguchi, 2016, Nature Medicine.

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.

C. Toniatti, S. Altamura, M. Rowley, 2009, Journal of medicinal chemistry.

Functional Genomics Reveals Synthetic Lethality between Phosphogluconate Dehydrogenase and Oxidative Phosphorylation.

R. DePinho, M. Warmoes, F. Mseeh, 2019, Cell reports.

Abstract A65: IACS-10759: A novel OXPHOS inhibitor that selectively kills tumors with metabolic vulnerabilities

Edward F. Chang, L. Chin, M. Protopopova, 2016 .

Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.

C. Toniatti, M. Rowley, K. Wilcoxen, 2015, Journal of medicinal chemistry.

Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery

B. Vangamudi, M. Kost-Alimova, M. Barton, 2015, Epigenetics & Chromatin.