Brendan Frett
Title | Assistant Professor |
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Institution | University of Arkansas for Medical Sciences |
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Department | Pharmaceutical Science, College of Pharmacy |
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Division | Pharmaceutical Science |
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Address | 200 South Cedar Mail Slot # 522 Little Rock AR 72202
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Phone | 501-526-0893 |
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vCard | Download vCard |
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Overview Dr. Brendan Frett received his Ph.D. in Pharmaceutical Sciences with an emphasis in Drug Discovery and Development from the University of Arizona in 2014. He received postdoctoral training in Medicinal Chemistry as well as Pharmaceutics at the University of Arizona. Dr. Frett has successfully transferred academic-based discoveries to pharmaceutical companies for clinical development. He is interested in pursuing translational research projects, where research completed in his laboratory can directly help patients.
Affiliation American Thyroid Association (ATA)
Biography 2018 | Envoys' Seeds of Science Award, UAMS | 2019 | Medical Research Endowment Award, UAMS | 2021 | Rho Chi Pharmacy Honor Society, Honorary Faculty Member, UAMS | 2022 | Pharmaceutical Sciences Faculty of the Year Award, UAMS |
Teaching Research P20GM152281 (EOFF, ROBERT L)Mar 5, 2024 - Dec 31, 2028 NIH Center for Molecular Interactions in Cancer (CMIC) Role: Co-Investigator |
| R01CA197178 (LI, HONG-YU)Sep 30, 2015 - Aug 31, 2021 NIH Selective RET Kinase and Its Mutant Inhibitors for the Treatment of Medullary Thyroid Cancer Role: Co-Investigator |
| P20GM109005 (BOERMA, MARJAN)Jun 24, 2015 - May 31, 2025 NIH Center for Studies of Host Response to Cancer Therapy Role: Co-Investigator |
Bibliographic
Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications.
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Waldrip ZJ, Acharya B, Armstrong D, Hanafi M, Rainwater RR, Amole S, Fulmer M, Azevedo-Pouly AC, Burns A, Burdine L, Frett B, Burdine MS. Discovery of the DNA-PKcs inhibitor DA-143 which exhibits enhanced solubility relative to NU7441. Sci Rep. 2024 08 28; 14(1):19999. PMID: 39198533.
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Acharya B, Saha D, Garcia Garcia N, Armstrong D, Jabali B, Hanafi M, Frett B, Ryan KR. Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors. Bioorg Med Chem. 2024 May 15; 106:117749. PMID: 38744018.
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McCrury M, Swafford K, Shuttleworth SL, Mehdi SH, Acharya B, Saha D, Naceanceno K, Byrum SD, Storey AJ, Xu YZ, Doshier C, Patel V, Post GR, De Loose A, Rodriguez A, Shultz LD, Zhan F, Yoon D, Frett B, Kendrick S. Bifunctional Inhibitor Reveals NEK2 as a Therapeutic Target and Regulator of Oncogenic Pathways in Lymphoma. Mol Cancer Ther. 2024 Mar 04; 23(3):316-329. PMID: 37816504.
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Frett B, Stephens KE, Koss B, Melnyk S, Farrar J, Saha D, Roy Choudhury S. Enhancer-activated RET confers protection against oxidative stress to KMT2A-rearranged acute myeloid leukemia. Cancer Sci. 2024 Mar; 115(3):963-973. PMID: 38226414.
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Acharya B, Saha D, Armstrong D, Jabali B, Hanafi M, Herrera-Rueda A, Lakkaniga NR, Frett B. Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules. RSC Med Chem. 2024 Feb 21; 15(2):399-415. PMID: 38389874.
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Acharya B, Frett B. An updated patent review of rearranged during transfection (RET) kinase inhibitors (2016-present). Expert Opin Ther Pat. 2022 Oct; 32(10):1067-1077. PMID: 36198171.
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Swafford K, Acharya B, Xu YZ, Raney T, McCrury M, Saha D, Frett B, Kendrick S. Targeting a Novel G-Quadruplex in the CARD11 Oncogene Promoter with Naptho(2,1-b)furan-1-ethanol,2-nitro- Requires the Nitro Group. Genes (Basel). 2022 06 25; 13(7). PMID: 35885931.
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Acharya B, Saha D, Armstrong D, Lakkaniga NR, Frett B. FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms. RSC Med Chem. 2022 Jul 20; 13(7):798-816. PMID: 35923716.
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Acharya B, Miah S, Frett B. Targeting TGF-?: triumphs and challenges. Future Med Chem. 2022 04; 14(7):455-458. PMID: 35152715.
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Zhang L, Moccia M, Briggs DC, Bharate JB, Lakkaniga NR, Knowles P, Yan W, Tran P, Kharbanda A, Wang X, Leung YK, Frett B, Santoro M, McDonald NQ, Carlomagno F, Li HY. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J Med Chem. 2022 01 27; 65(2):1536-1551. PMID: 35081714.
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Saha D, Ryan KR, Lakkaniga NR, Acharya B, Garcia NG, Smith EL, Frett B. Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. J Med Chem. 2021 08 26; 64(16):11747-11773. PMID: 34402300.
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Zhang L, Lakkaniga NR, Bharate JB, Mcconnell N, Wang X, Kharbanda A, Leung YK, Frett B, Shah NP, Li HY. Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. Eur J Med Chem. 2021 Dec 05; 225:113776. PMID: 34479037.
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Kharbanda A, Tran P, Zhang L, Leung YK, Li HY, Frett B. Discovery of 4-aminoquinolines as highly selective TGF?R1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. Eur J Med Chem. 2021 Dec 05; 225:113763. PMID: 34419892.
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Moccia M, Yang D, Lakkaniga NR, Frett B, McConnell N, Zhang L, Brescia A, Federico G, Zhang L, Salerno P, Santoro M, Li HY, Carlomagno F. Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases. Sci Rep. 2021 08 09; 11(1):16103. PMID: 34373541.
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Kharbanda A, Zhang L, Saha D, Tran P, Xu K, Li MO, Leung YK, Frett B, Li HY. Discovery and biological evaluation of phthalazines as novel non-kinase TGF? pathway inhibitors. Eur J Med Chem. 2021 Nov 05; 223:113660. PMID: 34246853.
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Saha D, Ryan KR, Lakkaniga NR, Smith EL, Frett B. Pyrazoloadenine Inhibitors of the RET Lung Cancer Oncoprotein Discovered by a Fragment Optimization Approach. ChemMedChem. 2021 05 18; 16(10):1605-1608. PMID: 33559353.
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Yan W, Zhang L, Lv F, Moccia M, Carlomagno F, Landry C, Santoro M, Gosselet F, Frett B, Li HY. Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation. Eur J Med Chem. 2021 Apr 15; 216:113265. PMID: 33652352.
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Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, Lee Y, Nam DH, Kornblum HI, Wang M, Nakano I. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. J Clin Invest. 2020 11 02; 130(11):6187. PMID: 33044225.
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Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, Lee Y, Nam DH, Kornblum HI, Wang M, Nakano I. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. J Clin Invest. 2020 09 01; 130(9):5027. PMID: 32870163.
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Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY. Correction to Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2020 Sep 10; 63(17):10089. PMID: 32841014.
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Lakkaniga NR, Gunaganti N, Zhang L, Belachew B, Frett B, Leung YK, Li HY. Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation. Eur J Med Chem. 2020 Nov 15; 206:112691. PMID: 32823007.
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Lakkaniga NR, Zhang L, Belachew B, Gunaganti N, Frett B, Li HY. Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression. Eur J Med Chem. 2020 Oct 01; 203:112589. PMID: 32717530.
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Storey AJ, Naceanceno KS, Lan RS, Washam CL, Orr LM, Mackintosh SG, Tackett AJ, Edmondson RD, Wang Z, Li HY, Frett B, Kendrick S, Byrum SD. ProteoViz: a tool for the analysis and interactive visualization of phosphoproteomics data. Mol Omics. 2020 08 01; 16(4):316-326. PMID: 32347222.
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Moccia M, Frett B, Zhang L, Lakkaniga NR, Briggs DC, Chauhan R, Brescia A, Federico G, Yan W, Santoro M, McDonald NQ, Li HY, Carlomagno F. Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology. J Med Chem. 2020 05 14; 63(9):4506-4516. PMID: 32298114.
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Lei J, Song GT, He LJ, Luo YF, Tang DY, Lin HK, Frett B, Li HY, Chen ZZ, Xu ZG. Correction: One-pot construction of functionalized aziridines and maleimides via a novel pseudo-Knoevenagel cascade reaction. Chem Commun (Camb). 2020 Feb 18; 56(14):2210. PMID: 32031562.
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Lei J, Song GT, He LJ, Luo YF, Tang DY, Lin HK, Frett B, Li HY, Chen ZZ, Xu ZG. One-pot construction of functionalized aziridines and maleimides via a novel pseudo-Knoevenagel cascade reaction. Chem Commun (Camb). 2020 Feb 18; 56(14):2194-2197. PMID: 31971170.
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Lakkaniga NR, Balasubramaniam M, Zhang S, Frett B, Li HY. Structural Characterization of the Aurora Kinase B "DFG-flip" Using Metadynamics. AAPS J. 2019 12 18; 22(1):14. PMID: 31853739.
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Saha D, Kharbanda A, Yan W, Lakkaniga NR, Frett B, Li HY. The Exploration of Chirality for Improved Druggability within the Human Kinome. J Med Chem. 2020 01 23; 63(2):441-469. PMID: 31550151.
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Gunaganti N, Kharbanda A, Lakkaniga NR, Zhang L, Cooper R, Li HY, Frett B. Catalyst free, C-3 functionalization of imidazo[1,2-a]pyridines to rapidly access new chemical space for drug discovery efforts. Chem Commun (Camb). 2018 Nov 15; 54(92):12954-12957. PMID: 30375586.
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Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY. Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 02 28; 62(4):1731-1760. PMID: 30188734.
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Frett B, McConnell N, Kharbanda A, Naresh G, Rounseville B, Warner C, Chang J, Debolske N, Li HY. Selective, C-3 Friedel-Crafts acylation to generate functionally diverse, acetylated Imidazo[1,2-a]pyridine derivatives. Tetrahedron. 2018 Aug 30; 74(35):4592-4600. PMID: 30344351.
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McConnell N, Frett B, Li H. Microwave-assisted green synthesis of anilines, phenols, and benzenediamines without transition metals, ligands, or organic solvents. Green Chem Lett Rev. 2018; 11(3):286-295. PMID: 30984284.
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He LJ, Yang DL, Li SQ, Zhang YJ, Tang Y, Lei J, Frett B, Lin HK, Li HY, Chen ZZ, Xu ZG. Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells. Bioorg Med Chem. 2018 08 07; 26(14):3899-3908. PMID: 29921474.
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Bharate JB, McConnell N, Naresh G, Zhang L, Lakkaniga NR, Ding L, Shah NP, Frett B, Li HY. Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. Sci Rep. 2018 02 27; 8(1):3722. PMID: 29487300.
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Lei J, Meng JP, Tang DY, Frett B, Chen ZZ, Xu ZG. Recent advances in the development of polycyclic skeletons via Ugi reaction cascades. Mol Divers. 2018 May; 22(2):503-516. PMID: 29340996.
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McConnell N, Xu Z, Kumarasamy V, Sun D, Frett B, Li HY. Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity. ChemistrySelect. 2017 12 11; 2(35):11821-11825. PMID: 30140731.
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Wang J, Cheng P, Pavlyukov MS, Yu H, Zhang Z, Kim SH, Minata M, Mohyeldin A, Xie W, Chen D, Goidts V, Frett B, Hu W, Li H, Shin YJ, Lee Y, Nam DH, Kornblum HI, Wang M, Nakano I. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2. J Clin Invest. 2017 Aug 01; 127(8):3075-3089. PMID: 28737508.
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Xi JB, Fang YF, Frett B, Zhu ML, Zhu T, Kong YN, Guan FJ, Zhao Y, Zhang XW, Li HY, Ma ML, Hu W. Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in?vitro and in?vivo antitumor activities. Eur J Med Chem. 2017 Jan 27; 126:1083-1106. PMID: 28039836.
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Frett B, Carlomagno F, Moccia ML, Brescia A, Federico G, De Falco V, Admire B, Chen Z, Qi W, Santoro M, Li HY. Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology. Angew Chem Int Ed Engl. 2015 Jul 20; 54(30):8717-21. PMID: 26126987.
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Wang Y, Frett B, McConnell N, Li HY. Metal-free, efficient hydrazination of imidazo[1,2-a]pyridine with diethyl azodicarboxylate in neutral media. Org Biomol Chem. 2015 Mar 14; 13(10):2958-64. PMID: 25611884.
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Frett B, McConnell N, Smith CC, Wang Y, Shah NP, Li HY. Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors. Eur J Med Chem. 2015 Apr 13; 94:123-31. PMID: 25765758.
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Frett B, Moccia M, Carlomagno F, Santoro M, Li HY. Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation. Eur J Med Chem. 2014 Oct 30; 86:714-23. PMID: 25232968.
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Frett B, McConnell N, Wang Y, Xu Z, Ambrose A, Li HY. Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies. Medchemcomm. 2014 Oct 01; 5(10):1507-1514. PMID: 26843921.
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Li F, Frett B, Li HY. Selective Reduction of Halogenated Nitroarenes with Hydrazine Hydrate in the Presence of Pd/C. Synlett. 2014 Jun; 25(10):1403-1408. PMID: 26843785.
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Wang Y, Frett B, Li HY. Efficient access to 2,3-diarylimidazo[1,2-a]pyridines via a one-pot, ligand-free, palladium-catalyzed three-component reaction under microwave irradiation. Org Lett. 2014 Jun 06; 16(11):3016-9. PMID: 24854606.
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Frett B, Brown RV, Ma M, Hu W, Han H, Li HY. Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition. J Med Chem. 2014 Jul 24; 57(14):5835-44. PMID: 24517277.
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Frett B, Wang Y, Li HY. Targeting the K-Ras/PDEd protein-protein interaction: the solution for Ras-driven cancers or just another therapeutic mirage? ChemMedChem. 2013 Oct; 8(10):1620-2. PMID: 23939923.
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Roberts SA, Saha B, Frett B, Li HY. (Z)-N-tert-Butyl-2-(4-meth-oxy-anilino)-N'-(4-meth-oxy-phen-yl)-2-phenyl-acetimidamide. Acta Crystallogr Sect E Struct Rep Online. 2013 Jun 01; 69(Pt 6):o902. PMID: 23795077.
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Wang Y, Kaiser CE, Frett B, Li HY. Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators. J Med Chem. 2013 Jul 11; 56(13):5219-30. PMID: 23566315.
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Gunawan S, Ayaz M, De Moliner F, Frett B, Kaiser C, Patrick N, Xu Z, Hulme C. Synthesis of Tetrazolo-Fused Benzodiazepines and Benzodiazepinones by a Two-Step Protocol Using an Ugi-Azide Reaction for Initial Diversity Generation. Tetrahedron. 2012 Jul 08; 68(27-28):5606-5611. PMID: 22923851.
This graph shows the total number of publications by year, by first, middle/unknown, or last author.
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Year | Publications |
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2012 | 1 | 2013 | 3 | 2014 | 5 | 2015 | 3 | 2016 | 1 | 2017 | 2 | 2018 | 7 | 2019 | 2 | 2020 | 9 | 2021 | 7 | 2022 | 5 | 2023 | 1 | 2024 | 4 |
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