Atman
Shah
Synthesis and characterization of a small molecule model to assess bifunctional chelator design for copper-based radiopharmaceuticals Radiopharmaceuticals are a class of compounds that utilize radioactive isotopes for the imaging and treatment of various diseases, including certain cancers and neurological conditions like Alzheimer's disease. Central to the effectiveness of these compounds are bifunctional chelators (BFCs): molecules that serve the dual purpose of attaching to targeting modalities (antibodies, peptides, etc.) and
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Authors:
Atman Shah
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transporting the radioactive isotope of choice to the diseased region within the body. Radioisotopes of copper, such as Cu-64 and Cu-67, represent "theranostic" pairs that can be used for imaging and therapy, respectively. Copper BFC design, including in the FDA-approved radiopharmaceutical Cu-64(DOTATATE), often features a macrocyclic polyaminocarboxylate "core", yet significant concerns remain regarding in vivo efficacy due to metal loss and off-target delivery. This project explores the role of key BFC properties such as hydrophobicity in determining chelator stability within small molecule models of Cu-64(DOTATATE). Specifically, we will share progress towards the synthesis of a novel anthracene-based derivative and a variety of characterization techniques, and contextualize our results within the larger goal of stable radiopharmaceutical design. Avery Guo:
Source:
Brown / SPRINT|Undergraduate Teaching and Research Awards (UTRA)
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Atman Shah