Radiometallated receptor-avid peptide conjugates for specific in vivo targeting of cancer cells.
New receptor-avid radiotracers are being developed for site-specific in vivo targeting of a myriad of receptors expressed on cancer cells. This review exemplifies strategies being used to design radiometallated peptide conjugates that maximize uptake in tumors and optimize their in vivo pharmacokinetic properties. Efforts to produce synthetic peptide analogues that target the following three receptor systems are highlighted: Gastrin releasing peptide (GRP), alpha-melanocyte stimulating hormone (alpha-MSH), and guanylate cyclase-C (GC-C) receptors.
Hoffman
T J
TJ
Department of Internal Medicine, University of Missouri and Research Service, Columbia, MO 65211, USA.
Quinn
T P
TP
Volkert
W A
WA
D000818:Animals; D006162:Guanylate Cyclase; D006801:Humans; D008545:Melanoma / Q000000981:diagnostic imaging / Q000628:therapy; D009369:Neoplasms / Q000737:chemistry / Q000000981:diagnostic imaging*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin / Q000032:analysis*; D011956:Receptors, Cell Surface / Q000032:analysis*; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled; D018000:Receptors, Peptide; D011979:Receptors, Pituitary Hormone / Q000032:analysis*
D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D011956:Receptors, Cell Surface; D018000:Receptors, Peptide; D011979:Receptors, Pituitary Hormone; C029446:MSH receptor; D006162:Guanylate Cyclase; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled