Sigma Receptors as Endoplasmic Reticulum Stress “Gatekeepers” and their Modulators as Emerging New Weapons in the Fight Against Cancer

Are sigma modulators an effective opportunity for cancer treatment? A patent overview (1996-2016)

(2017) Simona Collina et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Are sigma receptor modulators a weapon against multiple sclerosis disease?

(2017) Simona Collina et al.   Future Medicinal Chemistry

Small-Molecule Sigma1 Modulator Induces Autophagic Degradation of PD-L1

(2017) Christina M. Maher et al.   MOLECULAR CANCER RESEARCH

Sigma Receptor (σR) Ligands with Antiproliferative and Anticancer Activity

(2017) et al.   MOLECULES

Mitotic progression following DNA damage enables pattern recognition within micronuclei

(2017) Shane M. Harding et al.   NATURE

The SigmaR1 chaperone drives breast and colorectal cancer cell migration by tuning SK3-dependent Ca2+ homeostasis

(2017) M Gueguinou et al.   ONCOGENE

Identification of the gene that codes for the σ2receptor

(2017) Assaf Alon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mitochondria‐associated membrane collapse is a common pathomechanism in SIGMAR1 ‐ and SOD1 ‐linked ALS

(2016) Seiji Watanabe et al.   EMBO Molecular Medicine

Impact of intracellular ion channels on cancer development and progression

(2016) Roberta Peruzzo et al.   EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS

Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents

(2016) Marta Rui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Reduction of TMEM97 increases NPC1 protein levels and restores cholesterol trafficking in Niemann-pick type C1 disease cells

(2016) Darius Ebrahimi-Fakhari et al.   HUMAN MOLECULAR GENETICS

Loss-of-function mutations in theSIGMAR1gene cause distal hereditary motor neuropathy by impairing ER-mitochondria tethering and Ca2+signalling

(2016) Elisa Gregianin et al.   HUMAN MOLECULAR GENETICS

Crystal structure of the human σ1 receptor

(2016) Hayden R. Schmidt et al.   NATURE

The Role of Endoplasmic Reticulum Stress in Human Pathology

(2015) Scott A. Oakes et al.   Annual Review of Pathology-Mechanisms of Disease

Sigma 1 Receptor antagonist potentiates the anti-cancer effect of p53 by regulating ER stress, ROS production, Bax levels, and caspase-3 activation

(2015) Mireille Happy et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The sigma-1 receptors are present in monomeric and oligomeric forms in living cells in the presence and absence of ligands

(2015) Ashish K. Mishra et al.   BIOCHEMICAL JOURNAL

Potential applications for sigma receptor ligands in cancer diagnosis and therapy

(2015) Aren van Waarde et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Dysfunction in endoplasmic reticulum-mitochondria crosstalk underlies SIGMAR1 loss of function mediated motor neuron degeneration

(2015) Nathalie Bernard-Marissal et al.   BRAIN

SIGMAR1 Regulates Membrane Electrical Activity in Response to Extracellular Matrix Stimulation to Drive Cancer Cell Invasiveness

(2015) D. Crottes et al.   CANCER RESEARCH

Sigma-2 Receptor Ligands: Neurobiological Effects

(2015) Lin Guo et al.   CURRENT MEDICINAL CHEMISTRY

Elements in support of the ‘non-identity’ of the PGRMC1 protein with the σ2 receptor

(2015) Carmen Abate et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Sigma 1 receptor regulates the oxidative stress response in primary retinal Müller glial cells via NRF2 signaling and system xc−, the Na+-independent glutamate–cystine exchanger

(2015) Jing Wang et al.   FREE RADICAL BIOLOGY AND MEDICINE

Role of sigma-1 receptors in neurodegenerative diseases

(2015) Linda Nguyen et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Role of the Sigma-1 receptor in Amyotrophic Lateral Sclerosis (ALS)

(2015) Timur A. Mavlyutov et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Sigma-1 receptor: The novel intracellular target of neuropsychotherapeutic drugs

(2015) Teruo Hayashi   JOURNAL OF PHARMACOLOGICAL SCIENCES

Proteostasis control by the unfolded protein response

(2015) Claudio Hetz et al.   NATURE CELL BIOLOGY

Sigma-1 receptor mediates cocaine-induced transcriptional regulation by recruiting chromatin-remodeling factors at the nuclear envelope

(2015) Shang-Yi A. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Sigma-2 Receptor and Progesterone Receptor Membrane Component 1 are Different Binding Sites Derived From Independent Genes

(2015) Uyen B. Chu et al.   EBioMedicine

The Oligomeric States of the Purified Sigma-1 Receptor Are Stabilized by Ligands

(2014) Katarzyna A. Gromek et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Overexpression of Sig1R is closely associated with tumor progression and poor outcome in patients with hilar cholangiocarcinoma

(2014) Dongyun Xu et al.   MEDICAL ONCOLOGY

A Comprehensive Ligand Based Mapping of the σ2 Receptor Binding Pocket

(2014) Derek Rhoades et al.   Medicinal Chemistry

Alzheimer's Therapeutics Targeting Amyloid Beta 1–42 Oligomers II: Sigma-2/PGRMC1 Receptors Mediate Abeta 42 Oligomer Binding and Synaptotoxicity

(2014) Nicholas J. Izzo et al.   PLoS One

Alzheimer's Therapeutics Targeting Amyloid Beta 1–42 Oligomers I: Abeta 42 Oligomer Binding to Specific Neuronal Receptors Is Displaced by Drug Candidates That Improve Cognitive Deficits

(2014) Nicholas J. Izzo et al.   PLoS One

Addicted to secrete – novel concepts and targets in cancer therapy

(2014) Nicolas Dejeans et al.   TRENDS IN MOLECULAR MEDICINE

Stress, genomic adaptation, and the evolutionary trade-off

(2014) Steven D. Horne et al.   Frontiers in Genetics

Progesterone receptor membrane component 1/Sigma-2 receptor associates with MAP1LC3B and promotes autophagy

(2013) Shakeel UR Mir et al.   Autophagy

Transformation-Associated Changes in Sphingolipid Metabolism Sensitize Cells to Lysosomal Cell Death Induced by Inhibitors of Acid Sphingomyelinase

(2013) Nikolaj H.T. Petersen et al.   CANCER CELL

Progesterone Antagonism of Neurite Outgrowth Depends on Microglial Activation via Pgrmc1/S2R

(2013) N Bali et al.   ENDOCRINOLOGY

Sigma receptor modulators: a patent review

(2013) Simona Collina et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

The σ2 Receptor: A Novel Protein for the Imaging and Treatment of Cancer

(2013) Robert H. Mach et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Altered expression level of Sigma1 receptor gene in human colorectal cancer

(2013) Michał Skrzycki et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Neuroprotective effects of the Sigma-1 receptor (S1R) agonist PRE-084, in a mouse model of motor neuron disease not linked to SOD1 mutation

(2013) Marco Peviani et al.   NEUROBIOLOGY OF DISEASE

Sigma-1 Receptor Chaperone at the ER-Mitochondrion Interface Mediates the Mitochondrion-ER-Nucleus Signaling for Cellular Survival

(2013) Tomohisa Mori et al.   PLoS One

Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes

(2013) M Hafner Česen et al.   Cell Death & Disease

The sigma-1 receptor: a regulator of cancer cell electrical plasticity?

(2013) David Crottès et al.   Frontiers in Physiology

TMEM165 Deficiency Causes a Congenital Disorder of Glycosylation

(2012) François Foulquier et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression

(2012) Felix J. Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

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

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

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

The Sigma-1 Receptor Binds to the Nav1.5 Voltage-gated Na+Channel with 4-Fold Symmetry

(2012) Dilshan Balasuriya et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Time for TMEM?

(2012) Cathy M. Fuller   JOURNAL OF PHYSIOLOGY-LONDON

Identifying mechanism-of-action targets for drugs and probes

(2012) E. Gregori-Puigjane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The sigma-1 receptor: roles in neuronal plasticity and disease

(2012) Saïd Kourrich et al.   TRENDS IN NEUROSCIENCES

Translational Control in Cancer Etiology

(2012) D. Ruggero   Cold Spring Harbor Perspectives in Biology

The endoplasmic reticulum stress response in aging and age-related diseases

(2012) Marishka K. Brown et al.   Frontiers in Physiology

Ion channels and transporters in cancer. 3. Ion channels in the tumor cell-microenvironment cross talk

(2011) Annarosa Arcangeli   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Ion channels and transporters in cancer. 1. Ion channels and cell proliferation in cancer

(2011) Andrea Becchetti   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Endoplasmic reticulum stress and lipid dysregulation

(2011) Stephen M. Colgan et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

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

Sig1R Protein Regulates hERG Channel Expression through a Post-translational Mechanism in Leukemic Cells

(2011) David Crottès et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Unfolded Protein Response: From Stress Pathway to Homeostatic Regulation

(2011) P. Walter et al.   SCIENCE

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

Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors

(2010) Abdol R. Hajipour et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Demonstration of a Direct Interaction between σ-1 Receptors and Acid-Sensing Ion Channels

(2010) Stewart M. Carnally et al.   BIOPHYSICAL JOURNAL

Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells

(2010) Agostino Marrazzo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Progesterone inhibits apoptosis in part by PGRMC1-regulated gene expression

(2010) J.J. Peluso et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

(2010) John R Hornick et al.   Molecular Cancer

Progesterone Receptor Membrane Component 1 Inhibits the Activity of Drug-Metabolizing Cytochromes P450 and Binds to Cytochrome P450 Reductase

(2010) E. Szczesna-Skorupa et al.   MOLECULAR PHARMACOLOGY

Distribution of mRNAs encoding classical progestin receptor, progesterone membrane components 1 and 2, serpine mRNA binding protein 1, and progestin and ADIPOQ receptor family members 7 and 8 in rat forebrain

(2010) K.A. Intlekofer et al.   NEUROSCIENCE

Ion channels and the hallmarks of cancer

(2010) Natalia Prevarskaya et al.   TRENDS IN MOLECULAR MEDICINE

The sigma-1 receptor chaperone as an inter-organelle signaling modulator

(2010) Tsung-Ping Su et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

Identification of Cholesterol-Regulating Genes by Targeted RNAi Screening

(2009) Fabian Bartz et al.   Cell Metabolism

Voltage-gated Sodium Channel Activity Promotes Cysteine Cathepsin-dependent Invasiveness and Colony Growth of Human Cancer Cells

(2009) Ludovic Gillet et al.   JOURNAL OF BIOLOGICAL 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

The pharmacology of sigma-1 receptors

(2009) Tangui Maurice et al.   PHARMACOLOGY & THERAPEUTICS

Haploid Genetic Screens in Human Cells Identify Host Factors Used by Pathogens

(2009) J. E. Carette et al.   SCIENCE

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

Protein quality control in the early secretory pathway

(2008) Tiziana Anelli et al.   EMBO JOURNAL

STING is an endoplasmic reticulum adaptor that facilitates innate immune signalling

(2008) Hiroki Ishikawa et al.   NATURE

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