Brendan Frett
Assistant Professor
Also affiliated: University of Arizona (2012–2020); Syntrix Biosystems (United States) (2017–2020); Nimbis Services (United States) (2013); University of Arizona Cancer Center (2014)
Faculty Researcher
Pharmaceutical Science, College of Pharmacy
Research Areas
Biomedical Subjects
Links
Biography and Research Information
OverviewAI-generated summary
Dr. Brendan Frett's research focuses on the discovery and development of small-molecule inhibitors targeting kinases involved in cancer and other diseases. His work leverages structure-based drug design and medicinal chemistry to create novel compounds with potential for clinical translation. Dr. Frett has investigated inhibitors for various kinases, including RET, TRK, and FLT3, which are implicated in different types of cancer such as acute myeloid leukemia and lymphomas.
His laboratory synthesizes and evaluates these compounds, examining their structure-activity relationships and their effects on cancer cells and tumor models. Dr. Frett's research has led to the identification of bifunctional inhibitors and compounds with specific binding poses, aiming to overcome resistance mechanisms and improve therapeutic efficacy. He has a strong interest in translational research, seeking to move laboratory discoveries into clinical development to directly benefit patients.
Dr. Frett's scholarly output includes over 135 publications with 1,408 citations, and an h-index of 24, designating him as a highly cited researcher. He collaborates extensively with colleagues at the University of Arkansas for Medical Sciences, including Baku Acharya, Samantha Kendrick, Ying-Zhi Xu, and Mason McCrury, with whom he shares a significant number of publications.
Research 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.
Metrics
- h-index: 24
- Publications: 135
- Citations: 1,468
Selected Publications
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Epigenetic dysregulation and therapeutic targeting of <scp>RET</scp> receptor tyrosine kinase in high‐risk <scp> <i>KMT2A</i> </scp> ‐rearranged acute myeloid leukaemia (2025)
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Discovery of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRK/PTK6 inhibitors (2025)
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Discovery of Novel 1h-Pyrazolo[3,4-D]Pyrimidine Derivatives as Brk/Ptk6 Inhibitors (2025)
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Transforming growth factor β receptor 1 and mitogen-activated protein 4 kinase 4 dual inhibitor, TK-850, reduces renal fibrosis in unilateral ureteral–obstructed mice (2025)
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An updated patent review of rearranged during transfection (RET) kinase inhibitors (2022-present) (2025)
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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 (2025)
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Epigenetic Dysregulation and Therapeutic Targeting of RET Receptor Tyrosine Kinase in High-Risk KMT2A-Rearranged Pediatric Acute Myeloid Leukemia (2025)
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Discovery of the DNA-PKcs inhibitor DA-143 which exhibits enhanced solubility relative to NU7441 (2024)
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Attenuation of renal injury by administration of TK-850, a dual inhibitor of TGFβR1/MAP4K4 (2024)
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Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors (2024)
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557 Dual TGFβR1/MAP4K4 inhibitor reduces kidney injury in a mouse model of renal fibrosis. (2024)
Grants & Funding
As listed on this researcher's institutional profile.
- Center for Studies of Host Response to Cancer Therapy NIH Co-Investigator
- Selective RET Kinase and Its Mutant Inhibitors for the Treatment of Medullary Thyroid Cancer NIH Co-Investigator
- Center for Molecular Interactions in Cancer (CMIC) NIH Co-Investigator
Collaboration Network
Top Collaborators
- Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development
- FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms
- Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules
- Bifunctional Inhibitor Reveals NEK2 as a Therapeutic Target and Regulator of Oncogenic Pathways in Lymphoma
- Targeting a Novel G-Quadruplex in the CARD11 Oncogene Promoter with Naptho(2,1-b)furan-1-ethanol,2-nitro- Requires the Nitro Group
Showing 5 of 10 shared publications
- Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development
- FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms
- Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules
- Bifunctional Inhibitor Reveals NEK2 as a Therapeutic Target and Regulator of Oncogenic Pathways in Lymphoma
- Enhancer‐activated <scp>RET</scp> confers protection against oxidative stress to <scp>KMT2A</scp>‐rearranged acute myeloid leukemia
Showing 5 of 9 shared publications
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- 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
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
Showing 5 of 7 shared publications
- Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development
- FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms
- 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
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
Showing 5 of 7 shared publications
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- 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
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors
Showing 5 of 6 shared publications
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
- 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
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors
- Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
- Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors
- Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology
- 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
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors
- Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology
- FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms
- Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules
- Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors
- Discovery of the DNA-PKcs inhibitor DA-143 which exhibits enhanced solubility relative to NU7441
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
- Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
- Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development
- Pyrazoloadenine Inhibitors of the RET Lung Cancer Oncoprotein Discovered by a Fragment Optimization Approach
- Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors
- 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
- Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
- 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
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