Optimization of the Pharmacokinetic Profile of [^99mTc]Tc-N₄-Bombesin Derivatives by Modification of the Pharmacophoric Gln-Trp Sequence.

ABSTRACT: Current radiolabeled gastrin-releasing peptide receptor (GRPR) ligands usually suffer from high accumulation in GRPR-positive organs (pancreas, stomach), limiting tumor-to-background contrast in the abdomen. In novel N₄-bombesin derivatives this was addressed by substitutions at the Gln⁷-Trp⁸ site within the MJ9 peptide (H-Pip⁵-phe⁶-Gln⁷-Trp⁸-Ala⁹-Val¹⁰-Gly¹¹-His¹²-Sta¹³-Leu¹⁴-NH₂) either by homoserine (Hse⁷), β-(3-benzothienyl) alanine (Bta⁸) or α-methyl tryptophan (α-Me-Trp⁸), with the aim of optimizing pharmacokinetics. We prepared and characterized the peptide conjugates 6-c

SUBMITTER: Gunther T 

PROVIDER: S-EPMC9500665 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature