Commentary: harnessing the first peptidic modulator of the estrogen receptor GPER

R Lappano, M Maggiolini, C Mallet… - Frontiers in …, 2024 - frontiersin.org
According to the pioneering work of Thomas et al., the G protein-coupled estrogen receptor
GPER, a class A (rhodopsin-like) GPCR, interacts with estradiol (Thomas et al., 2005). This …

mPRα mediates P4/Org OD02‐0 to improve the sensitivity of lung adenocarcinoma to EGFR‐TKIs via the EGFR‐SRC‐ERK1/2 pathway

X Lu, A Guan, X Chen, J Xiao, M Xie… - Molecular …, 2020 - Wiley Online Library
The discovery of epidermal growth factor receptor (EGFR) mutations has made EGFR
tyrosine kinase inhibitors (EGFR‐TKIs) a milestone in the treatment for advanced non–small …

[HTML][HTML] GPR171 expression enhances proliferation and metastasis of lung cancer cells

SH Dho, KP Lee, D Jeong, CJ Kim, KS Chung, JY Kim… - Oncotarget, 2016 - ncbi.nlm.nih.gov
G protein-coupled receptors (GPCRs) are among the most significant therapeutic targets
and some of them promote the growth and metastasis of cancer. Here, we show that an …

A Gprc5a tumor suppressor loss of expression signature is conserved, prevalent, and associated with survival in human lung adenocarcinomas

H Kadara, J Fujimoto, T Men, X Ye, D Lotan, JS Lee… - Neoplasia, 2010 - Elsevier
Increasing the understanding of the impact of changes in oncogenes and tumor suppressor
genes is essential for improving the management of lung cancer. Recently, we identified a …

GPER function in breast cancer: an overview

R Lappano, A Pisano, M Maggiolini - Frontiers in endocrinology, 2014 - frontiersin.org
The G-protein-coupled estrogen receptor-1 (GPER, formerly known as GPR30) has attracted
increasing interest, considering its ability to mediate estrogenic signaling in different cell …

PRMT1, a key modulator of Unliganded progesterone receptor signaling in breast Cancer

L Malbeteau, J Jacquemetton, C Languilaire… - International Journal of …, 2022 - mdpi.com
The progesterone receptor (PR) is a key player in major physiological and pathological
responses in women, and the signaling pathways triggered following hormone binding have …

Identification of PGRMC1 as a Candidate Oncogene for Head and Neck Cancers and Its Involvement in Metabolic Activities

Y Zhao, X Ruan - Frontiers in Bioengineering and Biotechnology, 2020 - frontiersin.org
Progesterone Receptor Membrane Component 1 (PGRMC1/Sigma-2 receptor) is located on
chromosome Xq21 and encodes a haem-containing protein that interacts with epidermal …

GPER1 influences cellular homeostasis and cytostatic drug resistance via influencing long chain ceramide synthesis in breast cancer cells

MS Wegner, L Gruber, N Schömel, S Trautmann… - The international journal …, 2019 - Elsevier
The G protein-coupled estrogen receptor 1 (GPER1) is involved in the regulation of
physiological processes such as cellular growth and proliferation, but also in …

Recent advances in the rationale design of GPER ligands

C Rosano, R Lappano, MF Santolla… - Current medicinal …, 2012 - ingentaconnect.com
G-Protein Coupled Receptor (GPCR) superfamily, which comprises approximately 900
members, is the largest family of protein targets with proven therapeutic value. Although at …

GPER and human pathologies

Y Jacquot, M Kampa, SH Lindsey - Frontiers in Endocrinology, 2021 - frontiersin.org
More than 40% of commercialized drugs exert their action through G protein-coupled
receptors (GPCRs), indicating that the modulation of these hepta-transmembrane proteins is …