[Lys(DOTA)4]BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.
We substituted a truncated neuropeptide Y (NPY) analog, [Pro(30), Tyr(32), Leu(34)]NPY(28-36)NH(2) also called BVD15, at various positions with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7-10-tetraacetic acid) and evaluated the effect of the coupling position with the binding affinity for NPY Y(1) receptors (NPY1R). Our data suggest that [Lys(DOTA)(4)]BVD15 (K(i)=63+/-25 nM vs. K(i)=39+/-34 nM for BVD15) is a potent NPY analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.
Guérin
Brigitte
B
Department of Nuclear Medicine and Radiobiology, Centre d'Imagerie Moléculaire de Sherbrooke, Université de Sherbrooke, Québec, Canada. brigitte.guerin2@USherbrooke.ca
Dumulon-Perreault
Véronique
V
Tremblay
Marie-Claude
MC
Ait-Mohand
Samia
S
Fournier
Patrick
P
Dubuc
Céléna
C
Authier
Simon
S
Bénard
François
F
D001943:Breast Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism*; D002460:Cell Line; D045744:Cell Line, Tumor; D015195:Drug Design; D005260:Female; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000378:metabolism*; D006801:Humans; D009478:Neuropeptide Y / Q000031:analogs & derivatives* / Q000378:metabolism*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D017476:Receptors, Neuropeptide Y / Q000032:analysis / Q000378:metabolism*
C523778:DOTA4 compound; D006573:Heterocyclic Compounds, 1-Ring; D009478:Neuropeptide Y; D019275:Radiopharmaceuticals; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor