Molecules (Aug 2024)

Differences in the Renal Accumulation of Radiogallium-Labeled (Glu)<sub>14</sub> Peptides Containing Different Optical Isomers of Glutamic Acid

  • Kazuma Ogawa,
  • Kota Nishizawa,
  • Kenji Mishiro,
  • Masayuki Munekane,
  • Takeshi Fuchigami,
  • Hiroaki Echigo,
  • Hiroshi Wakabayashi,
  • Seigo Kinuya

DOI
https://doi.org/10.3390/molecules29173993
Journal volume & issue
Vol. 29, no. 17
p. 3993

Abstract

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Acidic amino acid peptides have a high affinity for bone. Previously, we demonstrated that radiogallium complex-conjugated oligo-acidic amino acids possess promising properties as bone-seeking radiopharmaceuticals. Here, to elucidate the effect of stereoisomers of Glu in Glu-containing peptides [(Glu)14] on their accumulation in the kidney, the biodistributions of [67Ga]Ga-N,N′-bis-[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N′-diacetic acid-conjugated (l-Glu)14 ([67Ga]Ga-HBED-CC-(l-Glu)14), [67Ga]Ga-HBED-CC-(d-Glu)14, [67Ga]Ga-HBED-CC-(dl-Glu)14, and [67Ga]Ga-HBED-CC-(d-Glu-l-Glu)7 were compared. Although the accumulation of these compounds in the bone was comparable, their kidney accumulation and retention were strikingly different, with [67Ga]Ga-HBED-CC-(d-Glu-l-Glu)7 exhibiting the lowest level of kidney accumulation among these compounds. Repeated d- and l-peptides may be a useful method for reducing renal accumulation in some cases.

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