title: A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P.
abstract: The macrocyclic bone-seeking agent, DO2A2P, bears a cyclen core and two pairs of peripheral phosphonate and carboxylate groups. The geometric disposition of the peripheral functionalities gives arise to a pair of geometric isomers: cis-DO2A2P and trans-DO2A2P. In order to compare the biological behavior of the isomer pair, cis-DO2A2P was synthesized. Both isomers were successfully radiolabeled with (177)Lu, which might potentiate their applications in both radiotherapy and imaging of bone diseases. Through a set of biological assays including the hydroxyapatite binding, in vitro stability, and in vivo distribution, we demonstrated that the geometric pair of DO2A2P had virtually identical biological properties.
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
authors.forename: Guiyang
authors.initials: G
authors.lastname: Hao
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA; Institute of Crystal Materials, Shandong University, Jinan, Shandong, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
authors.forename: Gedaa
authors.initials: G
authors.lastname: Hassan
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
authors.forename: Orhan K
authors.initials: OK
authors.lastname: Öz
authors.affiliation: Advanced Imaging Research Center, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
authors.forename: Zoltan
authors.initials: Z
authors.lastname: Kovacs
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA; Advanced Imaging Research Center, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. Electronic address: xiankai.sun@utsouthwestern.edu.
authors.forename: Xiankai
authors.initials: X
authors.lastname: Sun
mesh_terms: D000818:Animals; D003287:Contrast Media / Q000737:chemistry; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D007536:Isomerism; D007553:Isotope Labeling; D008187:Lutetium / Q000737:chemistry; D051379:Mice; D063065:Organophosphonates / Q000737:chemistry*; D011868:Radioisotopes; D015899:Tomography, Emission-Computed, Single-Photon; D051598:Whole Body Imaging
chemical_list: D003287:Contrast Media; D006573:Heterocyclic Compounds, 1-Ring; D063065:Organophosphonates; D011868:Radioisotopes; C000601193:cis-DO2A2P; C000601192:trans-DO2A2P; D008187:Lutetium
keywords: Bisphosphonate; Bone-seeking agent; Geometric isomer; Lutetium-177; Macrocyclics