Rucaparib

Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

[1]Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.|[2]Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.|[3]Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.|[4]Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246.|[5]J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84.|[6]Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13(595):eabe8226.Aging. 2021 Jan 20;13(3):4242-4257.|Am J Cancer Res. 2020 Aug 1;10(8):2649-2676.|Am J Cancer Res. 2024 Jan 15;14(1):378-389.|bioRxiv. 2023 Feb 6.|bioRxiv. 2023 Feb 7.|bioRxiv. 2024 Jul 10:2024.07.09.602803.|bioRxiv. 2024 September 19.|BMC Cancer. 2022 Mar 23;22(1):312.|Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. |DNA Repair (Amst). 2019 Jan;73:64-70.|Eur J Nucl Med Mol Imaging. 2024 Jul 18.|FASEB J. 2022 Jul;36(7):e22418.|Front Oncol. 2021 Jul 9;11:681441.|Gene. 2020 Oct 30;759:145000.|Genes Dis. 2023 Apr 12.|Int J Mol Sci. 2020 Feb 11;21(4):1185.|JCI Insight. 2023 Nov 8;8(21):e165268.|Mol Cancer Ther. 2024 Jun 19.|Nat Methods. 2023 Sep;20(9):1388-1399.|Neurooncol Adv. 2023 Feb 10;5(1):vdad010.|Patent. US20180263995A1.|Patent. US20180362972A1.|Research Square Preprint. 2024 Nov 06.|Research Square Print. September 20th, 2022.|Research Square Print. September 22nd, 2022.|Sci Adv. 2022 Feb 18;8(7):eabl9794.|Sci Immunol. 2024 Mar 15;9(93):eadj7238.|Sci Transl Med. 2021 May 26;13(595):eabe8226.|Talanta. 2018 Apr 1;180:127-132.|Theranostics. 2020 Jul 25;10(21):9477-9494. |Analyst. 2018 May 29;143(11):2501-2507.|Biochem Biophys Res Commun. 28 September 2021.|J Mol Med (Berl). 2019 Aug;97(8):1183-1193.|Nat Cell Biol. 2024 Jul 12.|Patent. US20200078369A1|Patent. US20200129476A1|Sens Actuators B Chem. 2018 Nov 10; 273:1047-1053. |Sens Actuators B Chem. 2018, 259: 565-572.|J Med Chem. 2023 Mar 6.|J Mol Med (Berl). 2019 Aug;97(8):1183-1193.