C
Carlo Toniatti
Researcher at Merck & Co.
Publications - 26
Citations - 1494
Carlo Toniatti is an academic researcher from Merck & Co.. The author has contributed to research in topics: Poly ADP ribose polymerase & PARP inhibitor. The author has an hindex of 14, co-authored 26 publications receiving 1327 citations. Previous affiliations of Carlo Toniatti include University of Texas MD Anderson Cancer Center.
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Journal ArticleDOI
The poly(ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial
Shahneen Sandhu,Shahneen Sandhu,William R. Schelman,George Wilding,Victor Moreno,Richard D. Baird,Susana Miranda,Lucy Hylands,Ruth Riisnaes,Martin Forster,Aurelius Omlin,Nathan Kreischer,Khin Thway,Heidrun Gevensleben,L. Sun,John W. Loughney,Manash Shankar Chatterjee,Carlo Toniatti,Carlo Toniatti,Christopher L. Carpenter,Robert Iannone,Stan B. Kaye,Johann S. de Bono,Robert M Wenham +23 more
TL;DR: Niraparib (MK4827) as mentioned in this paper is an oral potent, selective PARP-1/PARP-2 inhibitor that induces synthetic lethality in preclinical tumour models with loss of BRCA and PTEN function.
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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.
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Forced Mitotic Entry of S-Phase Cells as a Therapeutic Strategy Induced by Inhibition of WEE1
Marieke Aarts,Rachel Sharpe,Isaac Garcia-Murillas,Heidrun Gevensleben,Melissa S. Hurd,Stuart D. Shumway,Carlo Toniatti,Alan Ashworth,Nicholas C. Turner +8 more
TL;DR: It is shown that p53/p21 inactivation combined with high expression of mitotic cyclins and EZH2 predispose to mitotic entry during S-phase with cells reliant on WEE1 to prevent premature cyclin-dependent kinase (CDK)1 activation.
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MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation
Li Wang,Kathryn A. Mason,K. Kian Ang,Thomas A. Buchholz,David Valdecanas,Anjili Mathur,Carolyn A. Buser-Doepner,Carlo Toniatti,Luka Milas +8 more
TL;DR: MK-4827 shows high potential to improve the efficacy of radiotherapy and reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h, which potentially adds to the flexibility of design of future clinical trials.
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Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition
Amy D. Guertin,Melissa M. Martin,Brian S. Roberts,Melissa S. Hurd,Xianlu Qu,Nathan R. Miselis,Yaping Liu,Jing Li,Igor Feldman,Yair Benita,Andrew Bloecher,Carlo Toniatti,Stuart D. Shumway +12 more
TL;DR: This demonstration of DNA double strand breaks in the absence of a DNA damaging chemotherapeutic provides preclinical rationale for combining WEE1 and CHK1 inhibitors as a cancer treatment regimen.