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The Discovery of RP-2119: A Potent, Selective, and Orally Bioavailable Polθ ATPase Inhibitor.

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Title: The Discovery of RP-2119: A Potent, Selective, and Orally Bioavailable Polθ ATPase Inhibitor.
Authors: Mochirian P; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Papp R; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Mathieu MC; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Ferraro GB; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Dietrich E; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Liu B; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Bendahan D; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Perryman AL; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Surprenant S; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Fournier S; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Barzili BL; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Bonneau-Fortin A; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Yin SY; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Leclaire ME; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Patel C; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Poirier H; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Save S; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Mathieu Y; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Morin N; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Godbout C; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Burston HE; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Zahn KE; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Attia MA; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Pinter T; Paraza Pharma Inc., 2525 Ave. Marie Curie, Montréal, Québec H4S 1Z9, Canada., Barabé F; Paraza Pharma Inc., 2525 Ave. Marie Curie, Montréal, Québec H4S 1Z9, Canada., Parikh P; Piramal Pharma Ltd., Village Matoda, Taluka: Sanand, Ahmedabad 382213, Gujarat,India., Jagani C; Piramal Pharma Ltd., Village Matoda, Taluka: Sanand, Ahmedabad 382213, Gujarat,India., Kang G; NanoImaging Services, 4940 Carroll Canyon Rd UNIT 115, San Diego, California 92121, United States., Scapin G; NanoImaging Services, 4940 Carroll Canyon Rd UNIT 115, San Diego, California 92121, United States., Mamane Y; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Sfeir A; Molecular Biology Program, Sloan Kettering Institute, MSKCC, 430 E 67th Street, New York, New York 10065, United States., Mader P; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, Ontario M5G 1X5, Canada., Sicheri F; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, Ontario M5G 1X5, Canada., Zimmermann M; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Roulston A; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Morris SJ; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Black WC; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada., Gallant M; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada.
Source: Journal of medicinal chemistry [J Med Chem] 2025 Sep 25; Vol. 68 (18), pp. 19726-19745. Date of Electronic Publication: 2025 Sep 08.
Publication Type: 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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PubType: Academic Journal
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IllustrationInfo
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  Data: The Discovery of RP-2119: A Potent, Selective, and Orally Bioavailable Polθ ATPase Inhibitor.
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Piramal Pharma Ltd., Village Matoda, Taluka: Sanand, Ahmedabad 382213, Gujarat,India.<br /><searchLink fieldCode="AU" term="%22Jagani+C%22">Jagani C</searchLink>; Piramal Pharma Ltd., Village Matoda, Taluka: Sanand, Ahmedabad 382213, Gujarat,India.<br /><searchLink fieldCode="AU" term="%22Kang+G%22">Kang G</searchLink>; NanoImaging Services, 4940 Carroll Canyon Rd UNIT 115, San Diego, California 92121, United States.<br /><searchLink fieldCode="AU" term="%22Scapin+G%22">Scapin G</searchLink>; NanoImaging Services, 4940 Carroll Canyon Rd UNIT 115, San Diego, California 92121, United States.<br /><searchLink fieldCode="AU" term="%22Mamane+Y%22">Mamane Y</searchLink>; Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada.<br /><searchLink fieldCode="AU" term="%22Sfeir+A%22">Sfeir A</searchLink>; Molecular Biology Program, Sloan Kettering Institute, MSKCC, 430 E 67th Street, New York, New York 10065, United States.<br /><searchLink fieldCode="AU" term="%22Mader+P%22">Mader P</searchLink>; 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Repare Therapeutics, 7171 Frederick-Banting, Building 2, H4S 1Z9 Montréal, Québec, Canada.
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