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

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

Format: Article
Diterbitkan: MDPI AG 2024-08-01

Deskripsi

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)<sub>14</sub>] on their accumulation in the kidney, the biodistributions of [<sup>67</sup>Ga]Ga-<i>N</i>,<i>N</i>′-bis-[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-<i>N</i>,<i>N</i>′-diacetic acid-conjugated (<span style="font-variant: small-caps;">l</span>-Glu)<sub>14</sub> ([<sup>67</sup>Ga]Ga-HBED-CC-(<span style="font-variant: small-caps;">l</span>-Glu)<sub>14</sub>), [<sup>67</sup>Ga]Ga-HBED-CC-(<span style="font-variant: small-caps;">d</span>-Glu)<sub>14</sub>, [<sup>67</sup>Ga]Ga-HBED-CC-(<span style="font-variant: small-caps;">d</span><span style="font-variant: small-caps;">l</span>-Glu)<sub>14</sub>, and [<sup>67</sup>Ga]Ga-HBED-CC-(<span style="font-variant: small-caps;">d</span>-Glu-<span style="font-variant: small-caps;">l</span>-Glu)<sub>7</sub> were compared. Although the accumulation of these compounds in the bone was comparable, their kidney accumulation and retention were strikingly different, with [<sup>67</sup>Ga]Ga-HBED-CC-(<span style="font-variant: small-caps;">d</span>-Glu-<span style="font-variant: small-caps;">l</span>-Glu)<sub>7</sub> exhibiting the lowest level of kidney accumulation among these compounds. Repeated <span style="font-variant: small-caps;">d</span>- and <span style="font-variant: small-caps;">l</span>-peptides may be a useful method for reducing renal accumulation in some cases.