A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER).
نویسندگان
چکیده
We report the rational design, based on docking simulations, and synthesis of the first fluorescent and selective probe of GPER for bioimaging purposes and functional dissecting studies. It has been conceived as a Bodipy derivative and obtained by accessible and direct synthesis. Its optical properties have been measured in different solvents, showing insensitivity to their polarity. Its binding to GPER was achieved by competition assays with [3H]E2 and [5,6-3H] nicotinic acid in ER-negative and GPER-positive SkBr3 breast cancer cells. SkBr3 cells, transfected with a GPER expression vector containing a FLAG tag, were used to confirm that the fluorophore binds to GPER in a specific manner.
منابع مشابه
A comparative study of estrogen receptor beta expression in melanoma and benign melanocytic lesions
Background: Malignant melanoma is the most aggressive form of skin cancer. In contrast to other tumors, the role of estrogen in the initiation and progression of melanoma remains unclear. The aim of this study was to evaluate estrogen receptor beta protein expression in human melanoma tissues and in the benign melanocytic lesions. Method: Twenty-one patients, 11 with cutaneous melanoma and 10 w...
متن کاملFunction of G-Protein-Coupled Estrogen Receptor-1 in Reproductive System Tumors
The G-protein-coupled estrogen receptor-1 (GPER-1), also known as GPR30, is a novel estrogen receptor mediating estrogen receptor signaling in multiple cell types. The progress of estrogen-related cancer is promoted by GPER-1 activation through mitogen-activated protein kinases (MAPK), phosphoinositide 3-kinase (PI3K), and phospholipase C (PLC) signaling pathways. However, this promoting effect...
متن کاملAn amine/imine functionalized microporous MOF as a new fluorescent probe exhibiting selective sensing of Fe3+ and Al3+ over mixed metal ions
Nowadays metal-organic frameworks with multiple luminescent centers are very fascinating as multifunctional luminescent material because of their luminescence properties, which could be systematically tuned by deliberate use of organic ligands and metal ions. In this research, we explored a microporous mixed-ligand MOF for highly selective and sensitive detection of metal ions. A two-fold inter...
متن کاملComparative Study of Simultaneously and Interval Injection Estradiol and Tamoxifen on Estrogen Receptor α Expression in the Ca 1 Region of Hippocampal Pyramidal Neurons in Ovariectomized Rat
Purpose: The aim of our study is the assesment of estrogen receptor a expression in pyramidal neurons in rat CA 1hippocampus that has been ovariectomized. By using the estrogen antagonist, Tamoxifen level of expression of estrogen receptor a in these cells. Materials and Methods: To study the effect of 17- b estradiol and tamoxifen on estrogen receptors a, expression in hippocampus rats of Wist...
متن کاملStroke increases g protein-coupled estrogen receptor expression in the brain of male but not female mice.
The novel estrogen receptor, G protein-coupled estrogen receptor (GPER, previously named GPR30), is widely distributed throughout the male and female brain and, thus, could potentially play a role in estrogen-mediated neuroprotective effects in diseases such as stroke. We hypothesized that GPER distribution and expression in the brain of male, intact female, and ovariectomized (OVX) mice is inc...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Organic & biomolecular chemistry
دوره 13 42 شماره
صفحات -
تاریخ انتشار 2015