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Brendan Frett

TitleAssistant Professor
InstitutionUniversity of Arkansas for Medical Sciences
DepartmentPharmaceutical Science, College of Pharmacy
DivisionPharmaceutical Science
Address200 South Cedar
Mail Slot # 522
Little Rock AR 72202
Phone501-526-0893
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    Collapse Overview 
    Collapse 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.


    Collapse Affiliation 
    Collapse member of
    American Thyroid Association (ATA)

    Collapse Biography 
    Collapse awards and honors
    2018Envoys' Seeds of Science Award, UAMS
    2019Medical Research Endowment Award, UAMS
    2021Rho Chi Pharmacy Honor Society, Honorary Faculty Member, UAMS
    2022Pharmaceutical Sciences Faculty of the Year Award, UAMS

    Collapse Teaching 

    Collapse Research 
    Collapse research activities and funding
    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

    Collapse Bibliographic 
    Collapse selected publications
    Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Faculty can login to make corrections and additions. Don't see publications published under other names? Login to add alternative names.
    List All   |   Timeline
    1. Tran P, Moccia M, Wang X, Brescia A, Federico G, Gunaganti N, Wang Z, Yang M, Wang M, Jabali B, Yan W, Frett B, Santoro M, Carlomagno F, Li HY. Discovery of N-(3-fluorophenyl)-2-(4-((7-(1-methyl-1H-pyrazol-4-yl)quinazolin-4-yl)amino)phenyl)acetamide as the first orally active selective aurora kinase B inhibitor. Eur J Med Chem. 2025 Sep 15; 294:117735. PMID: 40398151.
      View in: PubMed
    2. 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.
      View in: PubMed
    3. 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.
      View in: PubMed
    4. 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.
      View in: PubMed
    5. 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.
      View in: PubMed
    6. 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.
      View in: PubMed
    7. Acharya B, Miah S, Frett B. Targeting TGF-?: triumphs and challenges. Future Med Chem. 2022 04; 14(7):455-458. PMID: 35152715.
      View in: PubMed
    8. 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.
      View in: PubMed
    9. 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.
      View in: PubMed
    10. 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.
      View in: PubMed
    11. 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.
      View in: PubMed
    12. 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.
      View in: PubMed
    13. 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.
      View in: PubMed
    14. 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.
      View in: PubMed
    15. 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.
      View in: PubMed
    16. 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.
      View in: PubMed
    17. 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.
      View in: PubMed
    18. 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.
      View in: PubMed
    19. 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.
      View in: PubMed
    20. 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.
      View in: PubMed
    21. 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.
      View in: PubMed
    22. 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.
      View in: PubMed
    23. 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.
      View in: PubMed
    24. 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.
      View in: PubMed
    25. 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.
      View in: PubMed
    26. 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.
      View in: PubMed
    27. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 35885931.
      View in: PubMed
    28. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 38744018.
      View in: PubMed
    29. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 39198533.
      View in: PubMed
    30. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 29487300.
      View in: PubMed
    31. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 29921474.
      View in: PubMed
    32. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 26843785.
      View in: PubMed
    33. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 32031562.
      View in: PubMed
    34. Sonderman KA, Wolf LL, Armstrong LB, Taylor K, Jiang W, Weil BR, Koehlmoos TP, Ricca RL, Weldon CB, Haider AH, Rice-Townsend SE. Testicular atrophy following inguinal hernia repair in children. Pediatr Surg Int. 2018 May; 34(5):553-560. PMID: 32347222.
      View in: PubMed
    35. 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.
      View in: PubMed
    36. 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.
      View in: PubMed
    37. 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.
      View in: PubMed
    38. 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.
      View in: PubMed
    39. 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.
      View in: PubMed
    40. 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.
      View in: PubMed
    41. 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.
      View in: PubMed
    42. 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.
      View in: PubMed
    43. 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.
      View in: PubMed
    44. 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.
      View in: PubMed
    45. 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.
      View in: PubMed
    46. 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.
      View in: PubMed
    47. 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.
      View in: PubMed
    48. McGoogan KE, Haafiz AB, Gonz?lez Peralta RP. Herpes simplex virus hepatitis in infants: clinical outcomes and correlates of disease severity. J Pediatr. 2011 Oct; 159(4):608-11. PMID: 26126987.
      View in: PubMed
    49. McGoogan KE, Haafiz AB, Gonz?lez Peralta RP. Herpes simplex virus hepatitis in infants: clinical outcomes and correlates of disease severity. J Pediatr. 2011 Oct; 159(4):608-11. PMID: 22923851.
      View in: PubMed
    50. McGoogan KE, Haafiz AB, Gonz?lez Peralta RP. Herpes simplex virus hepatitis in infants: clinical outcomes and correlates of disease severity. J Pediatr. 2011 Oct; 159(4):608-11. PMID: 32823007.
      View in: PubMed
    51. McGoogan KE, Haafiz AB, Gonz?lez Peralta RP. Herpes simplex virus hepatitis in infants: clinical outcomes and correlates of disease severity. J Pediatr. 2011 Oct; 159(4):608-11. PMID: 32870163.
      View in: PubMed
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