title: Use of Morpholino Oligomers for Pretargeting.
abstract: Differing from the conventional direct-targeting strategy in which a probe or payload is directly loaded onto a targeting molecule that binds to the native target, pretargeting is an improved targeting strategy. It converts the native target to an artificial target specific for a secondary targeting molecule loaded with the probe or payload (effector). The effector is small and does not accumulate in normal tissues, which accelerates the targeting process and generates high target to nontarget ratios. DNA/cDNA analogs can serve as the recognition pair, i.e., the artificial target and the secondary targeting effector. Morpholino oligomers are so far the most investigated and the most successful DNA/cDNA analog recognition pairs for pretargeting. Herein, we describe the pretargeting principles, the pretargeting strategy using Morpholino oligomers, and the preclinical success so far achieved.
authors.affiliation: Department of Radiology, University of Massachusetts Medical School, 55 Lake Avenue North, Worcester, MA, 01655, USA. guozheng.liu@umassmed.edu.
authors.forename: Guozheng
authors.initials: G
authors.lastname: Liu
mesh_terms: D000818:Animals; D018390:Gene Targeting / Q000379:methods; D018014:Gene Transfer Techniques; D018796:Immunoconjugates; D007553:Isotope Labeling; D051379:Mice; D060172:Morpholinos / Q000008:administration & dosage / Q000737:chemistry / Q000235:genetics* / Q000493:pharmacokinetics; D000072098:Single Photon Emission Computed Tomography Computed Tomography; D014018:Tissue Distribution
chemical_list: D018796:Immunoconjugates; D060172:Morpholinos
keywords: Antibody; Antibody modification; In Vitro and In Vivo targeting evaluation; Morpholino oligomers; Preclinical study; Pretargeting; Radiolabeling of Morpholino oligomers; Semiempirical pretargeting model