Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging

Chidambaram Gunanathan; Adi Pais; Edna Furman-Haran; Dalia Seger; Erez Eyal; Sarbani Mukhopadhyay; Yehoshoa Ben-David; Gregory Leitus; Hagai Cohen; Ayelet Vilan; Hadassa Degani; David Milstein

doi:10.1021/bc700230m

Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging

Chidambaram Gunanathan, Adi Pais, Edna Furman-Haran, Dalia Seger, Erez Eyal, Sarbani Mukhopadhyay, Yehoshoa Ben-David, Gregory Leitus, Hagai Cohen, Ayelet Vilan, Hadassa Degani^*, David Milstein^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

26 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1361-1365
Number of pages	5
Journal	Bioconjugate Chemistry
Volume	18
Issue number	5
DOIs	https://doi.org/10.1021/bc700230m
Publication status	Published - 2007

All Science Journal Classification (ASJC) codes

Bioengineering
Biotechnology
Biomedical Engineering
Pharmacology
Pharmaceutical Science
Organic Chemistry

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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.",

author = "Chidambaram Gunanathan and Adi Pais and Edna Furman-Haran and Dalia Seger and Erez Eyal and Sarbani Mukhopadhyay and Yehoshoa Ben-David and Gregory Leitus and Hagai Cohen and Ayelet Vilan and Hadassa Degani and David Milstein",

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T1 - Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging

AU - Gunanathan, Chidambaram

AU - Pais, Adi

AU - Furman-Haran, Edna

AU - Seger, Dalia

AU - Eyal, Erez

AU - Mukhopadhyay, Sarbani

AU - Ben-David, Yehoshoa

AU - Leitus, Gregory

AU - Cohen, Hagai

AU - Vilan, Ayelet

AU - Degani, Hadassa

AU - Milstein, David

PY - 2007

Y1 - 2007

N2 - 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.

AB - 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.

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U2 - 10.1021/bc700230m

DO - 10.1021/bc700230m

M3 - Article

SN - 1043-1802

VL - 18

SP - 1361

EP - 1365

JO - Bioconjugate Chemistry

JF - Bioconjugate Chemistry

IS - 5

ER -

Water-soluble contrast agents targeted at the estrogen receptor for molecular magnetic resonance imaging

Abstract

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