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, Bhavatarini, Paul, Thomas A, Shah, Parantu K, Kost-Alimova, Maria, Nottebaum, Lisa, Shi, Xi, Zhan, Yanai, Leo, Elisabetta, Mahadeshwar, Harshad S, Protopopov, Alexei, Futreal, Andrew, Tieu, Trang N, Peoples, Mike, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Petrocchi, Alessia, Verhelle, Dominique, Owen, Dafydd R, Draetta, Giulio, Jones, Philip, Palmer, Wylie S, Sharma, Shikhar, Andersen, Jannik N
Published in Cancer research (Chicago, Ill.) (15.09.2015)
Published in Cancer research (Chicago, Ill.) (15.09.2015)
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Journal Article
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor
Palmer, Wylie S, Poncet-Montange, Guillaume, Liu, Gang, Petrocchi, Alessia, Reyna, Naphtali, Subramanian, Govindan, Theroff, Jay, Yau, Anne, Kost-Alimova, Maria, Bardenhagen, Jennifer P, Leo, Elisabetta, Shepard, Hannah E, Tieu, Trang N, Shi, Xi, Zhan, Yanai, Zhao, Shuping, Barton, Michelle C, Draetta, Giulio, Toniatti, Carlo, Jones, Philip, Geck Do, Mary, Andersen, Jannik N
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
Summa, Vincenzo, Petrocchi, Alessia, Bonelli, Fabio, Crescenzi, Benedetta, Donghi, Monica, Ferrara, Marco, Fiore, Fabrizio, Gardelli, Cristina, Gonzalez Paz, Odalys, Hazuda, Daria J, Jones, Philip, Kinzel, Olaf, Laufer, Ralph, Monteagudo, Edith, Muraglia, Ester, Nizi, Emanuela, Orvieto, Federica, Pace, Paola, Pescatore, Giovanna, Scarpelli, Rita, Stillmock, Kara, Witmer, Marc V, Rowley, Michael
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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Journal Article
Identification of potent and selective MTH1 inhibitors
Petrocchi, Alessia, Leo, Elisabetta, Reyna, Naphtali J., Hamilton, Matthew M., Shi, Xi, Parker, Connor A., Mseeh, Faika, Bardenhagen, Jennifer P., Leonard, Paul, Cross, Jason B., Huang, Sha, Jiang, Yongying, Cardozo, Mario, Draetta, Giulio, Marszalek, Joseph R., Toniatti, Carlo, Jones, Philip, Lewis, Richard T.
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
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Journal Article
Gametocyte-specific and all-blood-stage transmission-blocking chemotypes discovered from high throughput screening on Plasmodium falciparum gametocytes
Paonessa, Giacomo, Siciliano, Giulia, Graziani, Rita, Lalli, Cristiana, Cecchetti, Ottavia, Alli, Cristina, La Valle, Roberto, Petrocchi, Alessia, Sferrazza, Alessio, Bisbocci, Monica, Falchi, Mario, Toniatti, Carlo, Bresciani, Alberto, Alano, Pietro
Published in Communications biology (06.06.2022)
Published in Communications biology (06.06.2022)
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Journal Article
A patent review of SHP2 allosteric inhibitors (2018-present)
Petrocchi, Alessia, Ciammaichella, Alina
Published in Expert opinion on therapeutic patents (03.05.2024)
Published in Expert opinion on therapeutic patents (03.05.2024)
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Journal Article
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors
Ponzi, Simona, Ferrigno, Federica, Bisbocci, Monica, Alli, Cristina, Ontoria, Jesus M., Petrocchi, Alessia, Toniatti, Carlo, Torrente, Esther
Published in Bioorganic & medicinal chemistry letters (01.03.2024)
Published in Bioorganic & medicinal chemistry letters (01.03.2024)
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Journal Article
Discovery of a Novel Series of Potent SHP2 Allosteric Inhibitors
Petrocchi, Alessia, Grillo, Alessandro, Ferrante, Luca, Randazzo, Pietro, Prandi, Adolfo, De Matteo, Marilenia, Iaccarino, Costanza, Bisbocci, Monica, Cellucci, Antonella, Alli, Cristina, Nibbio, Martina, Pucci, Vincenzo, Amaudrut, Jérôme, Montalbetti, Christian, Toniatti, Carlo, Di Fabio, Romano
Published in ACS medicinal chemistry letters (11.05.2023)
Published in ACS medicinal chemistry letters (11.05.2023)
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Journal Article
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme
Hamilton, Matthew M, Mseeh, Faika, McAfoos, Timothy J, Leonard, Paul G, Reyna, Naphtali J, Harris, Angela L, Xu, Alan, Han, Michelle, Soth, Michael J, Czako, Barbara, Theroff, Jay P, Mandal, Pijus K, Burke, Jason P, Virgin-Downey, Brett, Petrocchi, Alessia, Pfaffinger, Dana, Rogers, Norma E, Parker, Connor A, Yu, Simon S, Jiang, Yongying, Krapp, Stephan, Lammens, Alfred, Trevitt, Graham, Tremblay, Martin R, Mikule, Keith, Wilcoxen, Keith, Cross, Jason B, Jones, Philip, Marszalek, Joseph R, Lewis, Richard T
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Genetic events that limit the efficacy of MEK and RTK inhibitor therapies in a mouse model of KRAS-driven pancreatic cancer
Pettazzoni, Piergiorgio, Viale, Andrea, Shah, Parantu, Carugo, Alessandro, Ying, Haoqiang, Wang, Huamin, Genovese, Giannicola, Seth, Sahil, Minelli, Rosalba, Green, Tessa, Huang-Hobbs, Emmet, Corti, Denise, Sanchez, Nora, Nezi, Luigi, Marchesini, Matteo, Kapoor, Avnish, Yao, Wantong, Francesco, Maria E Di, Petrocchi, Alessia, Deem, Angela K, Scott, Kenneth, Colla, Simona, Mills, Gordon B, Fleming, Jason B, Heffernan, Timothy P, Jones, Philip, Toniatti, Carlo, DePinho, Ronald A, Draetta, Giulio F
Published in Cancer research (Chicago, Ill.) (15.03.2015)
Published in Cancer research (Chicago, Ill.) (15.03.2015)
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Journal Article
Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric Inhibitors
Torrente, Esther, Fodale, Valentina, Ciammaichella, Alina, Ferrigno, Federica, Ontoria, Jesus M., Ponzi, Simona, Rossetti, Ilaria, Sferrazza, Alessio, Amaudrut, Jérôme, Missineo, Antonino, Esposito, Simone, Palombo, Simone, Nibbio, Martina, Cerretani, Mauro, Bisbocci, Monica, Cellucci, Antonella, di Marco, Annalise, Alli, Cristina, Pucci, Vincenzo, Toniatti, Carlo, Petrocchi, Alessia
Published in ACS medicinal chemistry letters (09.02.2023)
Published in ACS medicinal chemistry letters (09.02.2023)
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Journal Article
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, Jongwon, Kelley, Elizabeth H, Methot, Joey L, Zhou, Hua, Petrocchi, Alessia, Chen, Hongmin, Hill, Susan E, Hinton, Marlene C, Hruza, Alan, Jung, Joon O, Maclean, John K. F, Mansueto, My, Naumov, George N, Philippar, Ulrike, Raut, Shruti, Spacciapoli, Peter, Sun, Dongyu, Siliphaivanh, Phieng
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Journal Article
Abstract 1975: Discovery of I-1000233, a potent, selective and brain permeable SHP2 allosteric inhibitor
Puca, Francesca, Fabbrini, Danilo, Ciammaichella, Alina, Missineo, Antonino, Bisbocci, Monica, Nibbio, Martina, Marco, Annalise Di, Apicella, Claudia, Colaceci, Fabrizio, Sasso, Romina, Natale, Daniela, Scalabrì, Francesco, Alli, Cristina, Pucci, Vincenzo, Montalbetti, Christian, Petrocchi, Alessia, Carugo, Alessandro, Toniatti, Carlo
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
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Journal Article
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor
Harper, Steven, McCauley, John A, Rudd, Michael T, Ferrara, Marco, DiFilippo, Marcello, Crescenzi, Benedetta, Koch, Uwe, Petrocchi, Alessia, Holloway, M. Katharine, Butcher, John W, Romano, Joseph J, Bush, Kimberly J, Gilbert, Kevin F, McIntyre, Charles J, Nguyen, Kevin T, Nizi, Emanuela, Carroll, Steven S, Ludmerer, Steven W, Burlein, Christine, DiMuzio, Jillian M, Graham, Donald J, McHale, Carolyn M, Stahlhut, Mark W, Olsen, David B, Monteagudo, Edith, Cianetti, Simona, Giuliano, Claudio, Pucci, Vincenzo, Trainor, Nicole, Fandozzi, Christine M, Rowley, Michael, Coleman, Paul J, Vacca, Joseph P, Summa, Vincenzo, Liverton, Nigel J
Published in ACS medicinal chemistry letters (12.04.2012)
Published in ACS medicinal chemistry letters (12.04.2012)
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Journal Article
Abstract LB-071: Discovery of an imidazopyridine series of potent human IDO1 inhibitors with robust target engagement in a preclinical tumor model
Petrocchi, Alessia, Reyna, Naphtali J., Mseeh, Faika, Parker, Connor A., Yu, Simon, Xu, Quanyun, Feng, Ningping, Leonard, Paul, Rogers, Norma, Cross, Jason B., Harris, Angela L., Jiang, Yongying, Khor, Tin Oo, Mahendra, Mikhila G., Pang, Jihai, Wu, Qi, Zuniga, Andy M., McAfoos, Timothy, Hamilton, Matthew M., Marszalek, Joe R., Mikule, Keith, Vancutsem, Paul, Wilcoxen, Keith, Tremblay, Martin, Jones, Philip, Lewis, Richard T.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2
Poncet-Montange, Guillaume, Zhan, Yanai, Bardenhagen, Jennifer P, Petrocchi, Alessia, Leo, Elisabetta, Shi, Xi, Lee, 4th, Gilbert R, Leonard, Paul G, Geck Do, Mary K, Cardozo, Mario G, Andersen, Jannik N, Palmer, Wylie S, Jones, Philip, Ladbury, John E
Published in Biochemical journal (01.03.2015)
Published in Biochemical journal (01.03.2015)
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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, Alessia, Jones, Philip, Rowley, Michael, Fiore, Fabrizio, Summa, Vincenzo
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Journal Article
4,5-Dihydroxypyrimidine Carboxamides and N-Alkyl-5-hydroxypyrimidinone Carboxamides Are Potent, Selective HIV Integrase Inhibitors with Good Pharmacokinetic Profiles in Preclinical Species
Summa, Vincenzo, Petrocchi, Alessia, Matassa, Victor G, Gardelli, Cristina, Muraglia, Ester, Rowley, Michael, Paz, Odalys Gonzalez, Laufer, Ralph, Monteagudo, Edith, Pace, Paola
Published in Journal of medicinal chemistry (16.11.2006)
Published in Journal of medicinal chemistry (16.11.2006)
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Journal Article
Abstract B48: Identification of potent, cell active MTH1 inhibitors and their use in target validation studies
Leo, Elisabetta, Petrocchi, Alessia, Bardenhagen, Jennifer, Alimova, Maria, Shi, Xi, Parker, Connor, Reyna, Naphtali, Hamilton, Matthew, Felix, Edward, Mazan, Andrzej, Dillon, Christian, Mseeh, Faika, Marszalek, Joseph R., Toniatti, Carlo, Draetta, Giulio, Jones, Phil, Lewis, Richard T.
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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