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Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor.

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Title: Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor.
Authors: Vallée F; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Casás-Selves M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Bubenik M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Duplessis M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Sow B; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Suarez C; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Sangiorgi B; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Li L; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Hyer M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Papp R; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Leclaire ME; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Perryman AL; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Liu B; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Surprenant S; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Mochirian P; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Pau V; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Maderova Z; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Mader P; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Yin SY; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Goodfellow E; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Roulston A; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Stocco R; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Godbout C; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Baruah P; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Bonneau-Fortin A; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Schonhoft JD; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States., Nejad P; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States., Norman D; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada., Truong VL; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada., Crane S; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada., Attia MA; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Mao D; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Sicheri F; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.; Departments of Biochemistry and Molecular Genetics, University of Toronto, Toronto, ON M5S 1A8, Canada., Marshall CG; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States., Zimmermann M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Bendahan D; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Gallant M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Black WC; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Source: Journal of medicinal chemistry [J Med Chem] 2025 Jun 12; Vol. 68 (11), pp. 10631-10647. Date of Electronic Publication: 2025 May 16.
Publication Type: Clinical Trial, Phase I; Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
FullText Text:
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DbLabel: MEDLINE Ultimate
An: 40378279
AccessLevel: 2
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
IllustrationInfo
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  Data: Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor.
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Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Nejad+P%22">Nejad P</searchLink>; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Norman+D%22">Norman D</searchLink>; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada.<br /><searchLink fieldCode="AU" term="%22Truong+VL%22">Truong VL</searchLink>; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada.<br /><searchLink fieldCode="AU" term="%22Crane+S%22">Crane S</searchLink>; Sygnature Discovery, 2350 rue Cohen Suite 201, Ville St-Laurent, QC H4R 2N6, Canada.<br /><searchLink fieldCode="AU" term="%22Attia+MA%22">Attia MA</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Mao+D%22">Mao D</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.<br /><searchLink fieldCode="AU" term="%22Sicheri+F%22">Sicheri F</searchLink>; 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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2025 Jun 12; Vol. 68 (11), pp. 10631-10647. <i>Date of Electronic Publication: </i>2025 May 16.
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