Radiochemical Investigations of 99mTc−N3S-X-BBN[7−14]NH2: An in Vitro/in Vivo Structure−Activity Relationship Study Where X = 0-, 3-, 5-, 8-, and 11-Carbon Tethering Moieties

摘要: Bombesin (BBN), a 14 amino acid peptide, is an analogue of human gastrin releasing peptide (GRP) that binds to GRP receptors (GRPr) with high affinity and specificity. The GRPr overexpressed on variety cancer cells, including prostate, breast, lung, pancreatic cancers. specific aim this study was develop 99mTc-radiolabeled BBN analogues maintain specificity for the in vivo. A preselected synthetic sequence via solid-phase synthesis (SPPS) designed produce N3S−BBN (N3S = dimethylglycyl-l-seryl-l-cysteinylglycinamide) conjugates following general structure:  DMG-S-C-G-X-Q-W-A-V-G−H-L-M-(NH2), where spacer group, X 0 (no spacer), ω-NH2(CH2)2COOH, ω-NH2(CH2)4COOH, ω-NH2(CH2)7COOH, or ω-NH2-(CH2)10COOH. new constructs were purified by reversed phase-HPLC (RP-HPLC). Electrospray mass spectrometry (ES-MS) used characterize nonmetalated conjugates. Re(V)−BBN prepared reaction Re(V)gluconate wi...