Philip Jones

发表

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

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

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.

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

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

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.

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

R. De Francesco, S. Altamura, M. Rowley, 2008, 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.

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.

Development of second generation epigenetic agents

Philip Jones, Philip D. Jones, 2012 .

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.

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.

Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.

Uwe Koch, Michael Rowley, U. Koch, 2009, Bioorganic & medicinal chemistry letters.

Histone Deacetylase Inhibitors

Philip Jones, Philip D. Jones, 2009 .

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.

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.

Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.

M. Rowley, Philip Jones, C. Steinkühler, 2009, 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.

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.

Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2.

G. Poncet-Montange, Gilbert R. Lee, J. Ladbury, 2015, The Biochemical journal.

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

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

Profiling PARP inhibitors

Philip Jones, 2012, Nature Biotechnology.

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

Philip Jones, Philip D. Jones, 2010 .

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.

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.

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.

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

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

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

M. Rowley, Philip Jones, C. Steinkühler, 2009, Bioorganic & medicinal chemistry letters.

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.

Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy.

Philip Jones, C. Ager, M. D. Di Francesco, 2019, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.

C. Toniatti, M. Rowley, Philip Jones, 2010, Bioorganic & medicinal chemistry letters.

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

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

Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Justin K. Huang, P. Mandal, Jason P. Burke, 2020, Cancer Research.

Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.

U. Koch, C. Toniatti, M. Rowley, 2009, Bioorganic & medicinal chemistry letters.

Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

C. Toniatti, M. Rowley, Philip Jones, 2010, Bioorganic & medicinal chemistry letters.

From natural products to small molecule ketone histone deacetylase inhibitors: development of new class specific agents.

Philip Jones, C. Steinkühler, Philip Jones, 2008, Current pharmaceutical design.

An inhibitor of oxidative phosphorylation exploits cancer vulnerability

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

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.

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

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

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.

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 .

Telomere dysfunction drives aberrant hematopoietic differentiation and myelodysplastic syndrome.

Michael C. Ryan, Nipun A. Mistry, L. Chin, 2015, Cancer cell.

Identification of potent and selective MTH1 inhibitors.

F. Mseeh, C. Toniatti, G. Draetta, 2005, Bioorganic & medicinal chemistry letters.

Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

C. Toniatti, M. Rowley, Philip Jones, 2010, Bioorganic & medicinal chemistry letters.

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

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

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.

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.

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.

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

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

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

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

Abstract 3277: IACS-9779, a development candidate that inhibits 2,3-dioxygenase (IDO) activity by blocking heme incorporation into IDO apoenzyme

F. Mseeh, T. Heffernan, Ningping Feng, 2019, Clinical Research (Excluding Clinical Trials).

Abstract PR01: IACS-010759 a novel inhibitor of oxidative phosphorylation advancing into first-in-human studies to exploit metabolic vulnerabilities

M. Protopopova, M. Konopleva, C. Bristow, 2017 .

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

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