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Radiolabeling and preliminary biodistribution study of 99m Tc-labeled antibody-mimetic scaffold protein repebody for initial clearance properties

Sajid Mushtaq, Jong Kook Rho, Jung Ae Kang, Joong-Jae Lee, Jung Young Kim, You Ree Nam, Seong-Jae Yun, Gyeong Hee Lee, Sang Hyun Park, Dong-Eun Lee, Hak-Sung Kim

Bioorg Med Chem Lett. 2017 Nov 15;27(22):5060-5064.

PMID: 29042166

Abstract:

Antibody-mimetic proteins are intensively being developed for biomedical applications including tumor imaging and therapy. Among them, repebody is a new class of protein that consists of highly diverse leucine-rich repeat (LRR) modules. Although all possible biomedical applications with repebody are ongoing, it's in vivo biodistribution and excretion pathway has not yet been explored. In this study, hexahistidine (His6)-tag bearing repebody (rEgH9) was labeled with [99mTc]-tricarbonyl, and biodistribution was performed following intravenous (I.V.) or intraperitoneal (I.P.) injection. Repebody protein was radiolabeled with high radiolabeling efficiency (>90%) and radiolabeled compound was more than 99% pure after purification. Biodistribution data indicates radiotracer has a rapid clearance from blood and excreted through the kidneys for intravenous (I.V.) injection, but comparatively slow clearance for an intraperitoneal (I.P.) injection. SPECT-CT images were found to be in agreement with biodistribution data, high activity was found inside kidneys. The observed result for rapid blood clearance and renal excretion of repebody (rEgH9) provide useful information for the further development of therapeutic strategy.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP58204425 Triamminetungsten(IV) tricarbonyl Triamminetungsten(IV) tricarbonyl 58204-42-5 Price
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