Sigma-2 Receptor Ligands and Their Perspectives in Cancer Diagnosis and Therapy

Assessment of Cellular Proliferation in Tumors by PET Using 18F-ISO-1

(2013) F. Dehdashti et al.   JOURNAL OF NUCLEAR MEDICINE

Inhibitory Effects of Sigma-2 Receptor Agonists on T Lymphocyte Activation

(2013) Miguel A. Iñiguez et al.   Frontiers in Pharmacology

7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands

(2012) Samuel D. Banister et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of a novel 99mTc cyclopentadienyl tricarbonyl complex ([(Cp-R)99mTc(CO)3]) for sigma-2 receptor tumor imaging

(2012) Xin Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Sigma-2 ligands induce tumour cell death by multiple signalling pathways

(2012) C Zeng et al.   BRITISH JOURNAL OF CANCER

2-Aminopyridine Derivatives as Potential σ2Receptor Antagonists

(2012) Carmen Abate et al.   ChemMedChem

Classes of Sigma2 (σ2) Receptor Ligands: Structure Affinity Relationship (SAfiR) Studies and Antiproliferative Activity

(2012) Carmen Abate et al.   CURRENT PHARMACEUTICAL DESIGN

Progesterone Regulation of Progesterone Receptor Membrane Component 1 (PGRMC1) Sumoylation and Transcriptional Activity in Spontaneously Immortalized Granulosa Cells

(2012) John J. Peluso et al.   ENDOCRINOLOGY

S2RPgrmc1: the cytochrome-related sigma-2 receptor that regulates lipid and drug metabolism and hormone signaling

(2012) Ikhlas S A Ahmed et al.   Expert Opinion on Drug Metabolism & Toxicology

Neutrophil Gelatinase-associated Lipocalin (NGAL) Expression Is Dependent on the Tumor-associated Sigma-2 Receptor S2RPgrmc1

(2012) Shakeel U. R. Mir et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lysosomal Membrane Permeabilization is an Early Event in Sigma-2 Receptor Ligand Mediated Cell Death in Pancreatic Cancer

(2012) John R Hornick et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Evidence for a genomic mechanism of action for progesterone receptor membrane component-1

(2012) John J. Peluso et al.   STEROIDS

Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand

(2011) Abdol R. Hajipour et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors

(2011) Kuo-Hsien Fan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Use of Multifunctional Sigma-2 Receptor Ligand Conjugates to Trigger Cancer-Selective Cell Death Signaling

(2011) D. Spitzer et al.   CANCER RESEARCH

Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands

(2011) Mine Yarim et al.   Chemical Biology & Drug Design

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands

(2011) Christophe Mésangeau et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Arylamides hybrids of two high-affinity σ2 receptor ligands as tools for the development of PET radiotracers

(2011) Carmen Abate et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Elevated progesterone receptor membrane component 1/sigma-2 receptor levels in lung tumors and plasma from lung cancer patients

(2011) Shakeel U.R. Mir et al.   INTERNATIONAL JOURNAL OF CANCER

Synthesis and Biological Characterization of 3-Substituted-1H-indoles as Ligands of GluN2B-ContainingN-Methyl-d-aspartate Receptors

(2011) Rosaria Gitto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorescent Derivatives of σ Receptor Ligand 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a Tool for Uptake and Cellular Localization Studies in Pancreatic Tumor Cells

(2011) Carmen Abate et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sigma-2 Receptor as Potential Indicator of Stem Cell Differentiation

(2011) Jodi L. Haller et al.   MOLECULAR IMAGING AND BIOLOGY

SV119-gold nanocage conjugates: a new platform for targeting cancer cellsvia sigma-2 receptors

(2011) Yucai Wang et al.   Nanoscale

Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site

(2011) Jinbin Xu et al.   Nature Communications

Radiosynthesis and biological evaluation of a promising σ2-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

(2010) Zhude Tu et al.   APPLIED RADIATION AND ISOTOPES

A 3D-pharmacophore model for σ2 receptors based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives

(2010) Erik Laurini et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Sigma Receptors in Oncology: Therapeutic and Diagnostic Applications of Sigma Ligands

(2010) Aren van Waarde et al.   CURRENT PHARMACEUTICAL DESIGN

Early development of sigma-receptor ligands

(2010) Sanju Narayanan et al.   Future Medicinal Chemistry

Pgrmc1 (Progesterone Receptor Membrane Component 1) Associates with Epidermal Growth Factor Receptor and Regulates Erlotinib Sensitivity

(2010) Ikhlas S. Ahmed et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Progesterone Receptor Membrane Component 1 (Pgrmc1): A Heme-1 Domain Protein That Promotes Tumorigenesis and Is Inhibited by a Small Molecule

(2010) I. S. Ahmed et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Sigma receptors and their ligands in cancer biology: overview and new perspectives for cancer therapy

(2010) Véronique Megalizzi et al.   MEDICINAL RESEARCH REVIEWS

The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine

(2010) John R Hornick et al.   Molecular Cancer

F281, synthetic agonist of the sigma-2 receptor, induces Ca2+ efflux from the endoplasmic reticulum and mitochondria in SK-N-SH cells

(2009) Giuseppe Cassano et al.   CELL CALCIUM

Exploring the Importance of Piperazine N-Atoms for σ2Receptor Affinity and Activity in a Series of Analogs of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28)†

(2009) Francesco Berardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sigma-2 receptor ligands potentiate conventional chemotherapies and improve survival in models of pancreatic adenocarcinoma

(2009) Hiroyuki Kashiwagi et al.   Journal of Translational Medicine

New N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs as σ2 receptor ligands: Synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents

(2008) Wenhua Chu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Conversion of a Highly Selective Sigma-1 Receptor–Ligand to Sigma-2 Receptor Preferring Ligands with Anticocaine Activity

(2008) Christophe Mésangeau et al.   JOURNAL OF MEDICINAL CHEMISTRY

PGRMC1 (progesterone receptor membrane component 1): A targetable protein with multiple functions in steroid signaling, P450 activation and drug binding

(2008) Hannah J. Rohe et al.   PHARMACOLOGY & THERAPEUTICS

Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization

(2007) Nicola Antonio Colabufo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS