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Items: 24

1.

An inhibitor of oxidative phosphorylation exploits cancer vulnerability.

Molina JR, Sun Y, Protopopova M, Gera S, Bandi M, Bristow C, McAfoos T, Morlacchi P, Ackroyd J, Agip AA, Al-Atrash G, Asara J, Bardenhagen J, Carrillo CC, Carroll C, Chang E, Ciurea S, Cross JB, Czako B, Deem A, Daver N, de Groot JF, Dong JW, Feng N, Gao G, Gay J, Do MG, Greer J, Giuliani V, Han J, Han L, Henry VK, Hirst J, Huang S, Jiang Y, Kang Z, Khor T, Konoplev S, Lin YH, Liu G, Lodi A, Lofton T, Ma H, Mahendra M, Matre P, Mullinax R, Peoples M, Petrocchi A, Rodriguez-Canale J, Serreli R, Shi T, Smith M, Tabe Y, Theroff J, Tiziani S, Xu Q, Zhang Q, Muller F, DePinho RA, Toniatti C, Draetta GF, Heffernan TP, Konopleva M, Jones P, Di Francesco ME, Marszalek JR.

Nat Med. 2018 Jul;24(7):1036-1046. doi: 10.1038/s41591-018-0052-4. Epub 2018 Jun 11.

PMID:
29892070
2.

Physical Exercise Improves Total Antioxidant Capacity and Gene Expression in Rat Hippocampal Tissue.

Franzoni F, Federighi G, Fusi J, Agosta V, Cerri E, Banducci R, Petrocchi A, Bernardi R, Innocenti A, Pruneti C, Daniele S, Pellegrini S, Martini C, Scuri R, Galetta F.

Arch Ital Biol. 2017 Jul 1;155(1-2):1-10. doi: 10.12871/000398292017121.

PMID:
28715593
3.

Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.

Lim J, Kelley EH, Methot JL, Zhou H, Petrocchi A, Chen H, Hill SE, Hinton MC, Hruza A, Jung JO, Maclean JK, Mansueto M, Naumov GN, Philippar U, Raut S, Spacciapoli P, Sun D, Siliphaivanh P.

J Med Chem. 2016 Jul 14;59(13):6501-11. doi: 10.1021/acs.jmedchem.6b00708. Epub 2016 Jul 1.

PMID:
27329786
4.

Identification of potent and selective MTH1 inhibitors.

Petrocchi A, Leo E, Reyna NJ, Hamilton MM, Shi X, Parker CA, Mseeh F, Bardenhagen JP, Leonard P, Cross JB, Huang S, Jiang Y, Cardozo M, Draetta G, Marszalek JR, Toniatti C, Jones P, Lewis RT.

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1503-1507. doi: 10.1016/j.bmcl.2016.02.026. Epub 2016 Feb 11.

PMID:
26898335
5.

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.

Vangamudi B, Paul TA, Shah PK, Kost-Alimova M, Nottebaum L, Shi X, Zhan Y, Leo E, Mahadeshwar HS, Protopopov A, Futreal A, Tieu TN, Peoples M, Heffernan TP, Marszalek JR, Toniatti C, Petrocchi A, Verhelle D, Owen DR, Draetta G, Jones P, Palmer WS, Sharma S, Andersen JN.

Cancer Res. 2015 Sep 15;75(18):3865-3878. doi: 10.1158/0008-5472.CAN-14-3798. Epub 2015 Jul 2.

6.

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

Palmer WS, Poncet-Montange G, Liu G, Petrocchi A, Reyna N, Subramanian G, Theroff J, Yau A, Kost-Alimova M, Bardenhagen JP, Leo E, Shepard HE, Tieu TN, Shi X, Zhan Y, Zhao S, Barton MC, Draetta G, Toniatti C, Jones P, Geck Do M, Andersen JN.

J Med Chem. 2016 Feb 25;59(4):1440-54. doi: 10.1021/acs.jmedchem.5b00405. Epub 2015 Jul 6.

7.

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

Pettazzoni P, Viale A, Shah P, Carugo A, Ying H, Wang H, Genovese G, Seth S, Minelli R, Green T, Huang-Hobbs E, Corti D, Sanchez N, Nezi L, Marchesini M, Kapoor A, Yao W, Francesco ME, Petrocchi A, Deem AK, Scott K, Colla S, Mills GB, Fleming JB, Heffernan TP, Jones P, Toniatti C, DePinho RA, Draetta GF.

Cancer Res. 2015 Mar 15;75(6):1091-101. doi: 10.1158/0008-5472.CAN-14-1854. Epub 2015 Mar 3.

8.

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

Poncet-Montange G, Zhan Y, Bardenhagen JP, Petrocchi A, Leo E, Shi X, Lee GR 4th, Leonard PG, Geck Do MK, Cardozo MG, Andersen JN, Palmer WS, Jones P, Ladbury JE.

Biochem J. 2015 Mar 1;466(2):337-46. doi: 10.1042/BJ20140933.

9.

Enhancing the chemical mixture methodology in emergency preparedness and consequence assessment analysis.

Yu XY, Glantz CS, Yao J, He H, Petrocchi AJ, Craig DK, Ciolek JT, Booth AE.

Toxicology. 2013 Nov 16;313(2-3):174-84. doi: 10.1016/j.tox.2012.10.011. Epub 2012 Nov 23.

PMID:
23182768
10.

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.

Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ.

ACS Med Chem Lett. 2012 Mar 2;3(4):332-6. doi: 10.1021/ml300017p. eCollection 2012 Apr 12.

11.

Discovery of pyrrolidine-based ╬▓-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.

Stachel SJ, Steele TG, Petrocchi A, Haugabook SJ, McGaughey G, Katharine Holloway M, Allison T, Munshi S, Zuck P, Colussi D, Tugasheva K, Wolfe A, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):240-4. doi: 10.1016/j.bmcl.2011.11.024. Epub 2011 Nov 12.

PMID:
22130130
12.

The development and application of the chemical mixture methodology in analysis of potential health impacts from airborne release in emergencies.

Yu XY, Petrocchi AJ, Craig DK, Glantz CS, Trott DM, Ciolek J, Lu PY, Bond JA, Tuccinardi TE Jr, Bouslaugh P.

J Appl Toxicol. 2010 Aug;30(6):513-24. doi: 10.1002/jat.1558. Review.

PMID:
20635331
13.

Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.

Harper S, Ferrara M, Crescenzi B, Pompei M, Palumbi MC, DiMuzio JM, Donghi M, Fiore F, Koch U, Liverton NJ, Pesci S, Petrocchi A, Rowley M, Summa V, Gardelli C.

J Med Chem. 2009 Aug 13;52(15):4820-37. doi: 10.1021/jm900372w.

PMID:
19624135
14.

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.

Petrocchi A, Jones P, Rowley M, Fiore F, Summa V.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4245-9. doi: 10.1016/j.bmcl.2009.05.098. Epub 2009 May 29.

PMID:
19523819
15.

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

Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M.

J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z.

PMID:
18763751
16.

Studies of metabolism and disposition of potent human immunodeficiency virus (HIV) integrase inhibitors using 19F-NMR spectroscopy.

Monteagudo E, Pesci S, Taliani M, Fiore F, Petrocchi A, Nizi E, Rowley M, Laufer R, Summa V.

Xenobiotica. 2007 Sep;37(9):1000-12.

PMID:
17896326
17.

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

Pace P, Di Francesco ME, Gardelli C, Harper S, Muraglia E, Nizi E, Orvieto F, Petrocchi A, Poma M, Rowley M, Scarpelli R, Laufer R, Gonzalez Paz O, Monteagudo E, Bonelli F, Hazuda D, Stillmock KA, Summa V.

J Med Chem. 2007 May 3;50(9):2225-39. Epub 2007 Apr 12.

PMID:
17428043
18.

4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.

Summa V, Petrocchi A, Matassa VG, Gardelli C, Muraglia E, Rowley M, Paz OG, Laufer R, Monteagudo E, Pace P.

J Med Chem. 2006 Nov 16;49(23):6646-9.

PMID:
17154493
19.

From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.

Petrocchi A, Koch U, Matassa VG, Pacini B, Stillmock KA, Summa V.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):350-3. Epub 2006 Oct 25.

PMID:
17107799
20.

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

Jones P, Altamura S, Chakravarty PK, Cecchetti O, De Francesco R, Gallinari P, Ingenito R, Meinke PT, Petrocchi A, Rowley M, Scarpelli R, Serafini S, Steink├╝hler C.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5948-52. Epub 2006 Sep 20.

PMID:
16987657
21.

HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.

Summa V, Petrocchi A, Matassa VG, Taliani M, Laufer R, De Francesco R, Altamura S, Pace P.

J Med Chem. 2004 Oct 21;47(22):5336-9.

PMID:
15481971
22.

Discovery of alpha,gamma-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase.

Summa V, Petrocchi A, Pace P, Matassa VG, De Francesco R, Altamura S, Tomei L, Koch U, Neuner P.

J Med Chem. 2004 Jan 1;47(1):14-7.

PMID:
14695815
23.

Derivation of temporary emergency exposure limits (TEELs).

Craig DK, Davis JS, Hansen DJ, Petrocchi AJ, Powell TJ, Tuccinardi TE Jr.

J Appl Toxicol. 2000 Jan-Feb;20(1):11-20.

PMID:
10641012
24.

Recommended default methodology for analysis of airborne exposures to mixtures of chemicals in emergencies.

Craig DK, Baskett RL, Davis JS, Dukes L, Hansen DJ, Petrocchi AJ, Powell TJ, Sutherland PJ, Tuccinardi TE Jr.

Appl Occup Environ Hyg. 1999 Sep;14(9):609-17. Review.

PMID:
10510523

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