1393933-89-5Relevant articles and documents
Synthesis and characterization of αvβ3- targeting peptidomimetic chelate conjugates for PET and SPECT imaging
Kim, Young-Seung,Nwe, Kido,Milenic, Diane E.,Brechbiel, Martin W.,Satz, Stanley,Baidoo, Kwamena E.
supporting information; experimental part, p. 5517 - 5522 (2012/09/25)
There is growing interest in small peptidomimetic αvβ 3 integrin antagonists that are readily synthesized and characterized and can be easily handled using physiological conditions. Peptidomimetic 4-[2-(3,4,5,6-tetrahydropyrimidine-2-ylamino)ethyloxy]benzoyl-2-[N-(3-amino- neopenta-1-carbamyl)]-aminoethylsulfonyl-amino-β-alanine (IAC) was successfully conjugated to 1-(1-carboxy-3-carbo-t-butoxypropyl)-4,7-(carbo-tert- butoxymethyl)-1,4,7-triazacyclononane (NODA-GA(tBu)3) and 1-(1-carboxy-3-carbotertbutoxymethyl)-1,4,7,10-tetraazacyclododecane (DOTA-GA(tBu)4) and radiolabeled with 111In, 67Ga and 203Pb. Results of a radioimmunoassay demonstrated binding to purified αvβ3 integrin when 1-4 equiv of integrin were added to the reaction. Based on this promising result, investigations are moving forward to evaluate the NODA-GA-IAC and DOTA-GA-IAC conjugates for targeting tumor associated angiogenesis and α vβ3 integrin positive tumors to define their PET and SPECT imaging qualities as well as their potential for delivery of therapeutic radionuclides.