Amber N. Frantz
Research Subjects
Amber N. Frantz has a total of 16 co-authors. Here are the top co-authors by number of shared publications:
Andrew D. Boyer
Voelcker Preclinical Pharmacology Core
1 shared publication- April L. Risinger
Department of Pharmacology and Mays Cancer Center, University of Texas Health Science Center, San Antonio, Texas, USA
1 shared publication - Doug E. Frantz
The Max and Minnie Tomerlin Voelcker Laboratory for Organic Chemistry, Department of Chemistry, The University of Texas at San Antonio, San Antonio, Texas 78249, United States
1 shared publication - Jennifer L. Bartels
Department of Radiology, University of Alabama at Birmingham, Birmingham, USA
1 shared publication Joseph W. Boerma
Voelcker Preclinical Pharmacology Core
1 shared publicationJycole E. M. Bush
Department of Pharmacology
1 shared publication
Latest Publications
- Open Access
- 16 July 2025
- Published by American Chemical Society (ACS) in ACS Medicinal Chemistry Letters
- Vol. 16 (8) , 1569-1574
Pharmacokinetic and Biodistribution Studies of [18F]-Taccalonolide: A Covalent Microtubule Stabilizer with Antitumor Efficacy
The taccalonolides are plant-derived microtubule stabilizers that covalently and specifically bind β-tubulin and provide antitumor efficacy in drug-resistant tumor models both in vitro and in vivo. Herein, we report the radiolabeling, in vitro uptake, and in vivo imaging of a 18F radiolabeled taccalonolide to investigate in vivo biodistribution, including accumulation in TNBC tumors. Biochemical and cellular studies demonstrate that fluorination does not alter biological activity and supports target engagement of the radiolabeled compound. In vivo studies in athymic nude mice bearing TNBC xenografts and healthy control animals show the highest uptake in the gallbladder and intestines with modest uptake in tumors. Unmodified free drug was detected in the gall bladder and intestines, suggesting hepatic transport of the compound prior to metabolism or irreversible target engagement. These results provide a strong rationale for the generation of novel derivatives and formulations to improve serum half-life and tumor targeting of the taccalonolides to ultimately provide new options for drug-resistant TNBC tumors.
- 16 July 2025
- Published by American Chemical Society (ACS) in ACS Medicinal Chemistry Letters
- Vol. 16 (8) , 1569-1574
Open AccessPharmacokinetic and Biodistribution Studies of [18F]-Taccalonolide: A Covalent Microtubule Stabilizer with Antitumor Efficacy
The taccalonolides are plant-derived microtubule stabilizers that covalently and specifically bind β-tubulin and provide antitumor efficacy in drug-resistant tumor models both in vitro and in vivo. Herein, we report the radiolabeling, in vitro uptake, and in vivo imaging of a 18F radiolabeled taccalonolide to investigate in vivo biodistribution, including accumulation in TNBC tumors. Biochemical and cellular studies demonstrate that fluorination does not alter biological activity and supports target engagement of the radiolabeled compound. In vivo studies in athymic nude mice bearing TNBC xenografts and healthy control animals show the highest uptake in the gallbladder and intestines with modest uptake in tumors. Unmodified free drug was detected in the gall bladder and intestines, suggesting hepatic transport of the compound prior to metabolism or irreversible target engagement. These results provide a strong rationale for the generation of novel derivatives and formulations to improve serum half-life and tumor targeting of the taccalonolides to ultimately provide new options for drug-resistant TNBC tumors.