title: RGD-based PET tracers for imaging receptor integrin αv β3 expression.
abstract: Positron emission tomography (PET) imaging of receptor integrin αv β3 expression may play a key role in the early detection of cancer and cardiovascular diseases, monitoring disease progression, evaluating therapeutic response, and aiding anti-angiogenic drugs discovery and development. The last decade has seen the development of new PET tracers for in vivo imaging of integrin αv β3 expression along with advances in PET chemistry. In this review, we will focus on the radiochemistry development of PET tracers based on arginine-glycine-aspartic acid (RGD) peptide, present an overview of general strategies for preparing RGD-based PET tracers, and review the recent advances in preparations of (18) F-labeled, (64) Cu-labeled, and (68) Ga-labeled RGD tracers, RGD-based PET multivalent probes, and RGD-based PET multimodality probes for imaging receptor integrin αv β3 expression.
authors.affiliation: PET Center, Children's Hospital of Michigan, Detroit Medical Center, Detroit, MI, 48201, USA; Wayne State University School of Medicine, Detroit, MI, 48201, USA.
authors.forename: Hancheng
authors.initials: H
authors.lastname: Cai
authors.forename: Peter S
authors.initials: PS
authors.lastname: Conti
mesh_terms: D000818:Animals; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D007553:Isotope Labeling; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D039302:Integrin alphaVbeta3; D009842:Oligopeptides; D019275:Radiopharmaceuticals; C047981:arginyl-glycyl-aspartic acid
keywords: PET imaging; RGD; integrin; radiochemistry