title: Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging.
abstract: Novel estrogen-conjugated pyridine-containing Gd(III) and Eu(III) contrast agents (EPTA-Gd/Eu) were designed and effectively synthesized. Convenient to administration and MRI experiments, both EPTA-Gd and EPTA-Eu are soluble in water. The EPTA-Gd selectively binds with a micromolar affinity to the estrogen receptor and induces proliferation of human breast cancer cells. The EPTA-Gd is not lethal and does not cause any adverse effects when administrated intravenously. It enhances T1 and T2 nuclear relaxation rates of water and serves as a selective contrast agent for localizing the estrogen receptor by MRI.
authors.affiliation: Department of Organic Chemistry, Weizmann Institute of Science, Rehovot 76100, Israel.
authors.forename: Chidambaram
authors.initials: C
authors.lastname: Gunanathan
authors.forename: Adi
authors.initials: A
authors.lastname: Pais
authors.forename: Edna
authors.initials: E
authors.lastname: Furman-Haran
authors.forename: Dalia
authors.initials: D
authors.lastname: Seger
authors.forename: Erez
authors.initials: E
authors.lastname: Eyal
authors.forename: Sarbani
authors.initials: S
authors.lastname: Mukhopadhyay
authors.forename: Yehoshoa
authors.initials: Y
authors.lastname: Ben-David
authors.forename: Gregory
authors.initials: G
authors.lastname: Leitus
authors.forename: Hagai
authors.initials: H
authors.lastname: Cohen
authors.forename: Ayelet
authors.initials: A
authors.lastname: Vilan
authors.forename: Hadassa
authors.initials: H
authors.lastname: Degani
authors.forename: David
authors.initials: D
authors.lastname: Milstein
mesh_terms: D001943:Breast Neoplasms / Q000473:pathology; D003287:Contrast Media / Q000737:chemistry*; D019786:Gadolinium DTPA / Q000008:administration & dosage / Q000138:chemical synthesis*; D006801:Humans; D007089:Image Enhancement / Q000379:methods*; D007275:Injections, Intravenous; D008279:Magnetic Resonance Imaging / Q000379:methods*; D011960:Receptors, Estrogen / Q000032:analysis*; D012995:Solubility; D013997:Time Factors; D014867:Water / Q000737:chemistry*