Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging.
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.
Gunanathan
Chidambaram
C
Department of Organic Chemistry, Weizmann Institute of Science, Rehovot 76100, Israel.
Pais
Adi
A
Furman-Haran
Edna
E
Seger
Dalia
D
Eyal
Erez
E
Mukhopadhyay
Sarbani
S
Ben-David
Yehoshoa
Y
Leitus
Gregory
G
Cohen
Hagai
H
Vilan
Ayelet
A
Degani
Hadassa
H
Milstein
David
D
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*