The Orexin receptors: Structural and anti-tumoral properties

Hypocretins (orexins): The ultimate translational neuropeptides

(2022) Laura H. Jacobson et al.   JOURNAL OF INTERNAL MEDICINE

Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist

(2022) Tatsuhiko Fujimoto et al.   ACS Medicinal Chemistry Letters

The Orexin-A/OX1R System Induces Cell Death in Pancreatic Cancer Cells Resistant to Gemcitabine and Nab-Paclitaxel Treatment

(2022) Thierry Voisin et al.   Frontiers in Oncology

The war against pancreatic cancer in 2020 — advances on all fronts

(2021) Tejeshwar Jain et al.   Nature Reviews Gastroenterology & Hepatology

Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

(2021) Chuan Hong et al.   Nature Communications

Diverse Functional Autoantibodies in Patients with COVID-19

(2021) Eric Y. Wang et al.   NATURE

Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery

(2021) Lauren M. Slosky et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Pancreatic adenocarcinoma: Beyond first line, where are we?

(2021) Sara Cherri et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Pancreatic Cancer

(2021) Wungki Park et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Patient-derived tumor models: a more suitable tool for pre-clinical studies in colorectal cancer

(2021) Giulia Rizzo et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

An overview of the orexinergic system in different animal species

(2021) Idris A. Azeez et al.   METABOLIC BRAIN DISEASE

Orexins/Hypocretins and Cancer: A Neuropeptide as Emerging Target

(2021) Couvineau Alain et al.   MOLECULES

Early detection of pancreatic cancer using DNA-based molecular approaches

(2021) Aatur D. Singhi et al.   Nature Reviews Gastroenterology & Hepatology

Molecular alterations in pancreatic tumors

(2021) Michela Visani et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Focus on the Complex Interconnection between Cancer, Narcolepsy and Other Neurodegenerative Diseases: A Possible Case of Orexin-Dependent Inverse Comorbidity

(2021) Maria P. Mogavero et al.   Cancers

Identifying Novel Actionable Targets in Colon Cancer

(2021) Maria Grazia Cerrito et al.   Biomedicines

Orexins: A promising target to digestive cancers, inflammation, obesity and metabolism dysfunctions

(2021) Alain Couvineau et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Daridorexant, a New Dual Orexin Receptor Antagonist to Treat Insomnia Disorder

(2020) Yves Dauvilliers et al.   ANNALS OF NEUROLOGY

Recently Approved and Upcoming Treatments for Narcolepsy

(2020) Michael J. Thorpy   CNS DRUGS

Lemborexant: First Approval

(2020) Lesley J. Scott   DRUGS

Orexin Antagonists: A Wake-Up Call for Medicinal Chemists?

(2020) D. Eric Walters   JOURNAL OF MEDICINAL CHEMISTRY

Role of Brown Adipose Tissue in Adiposity Associated With Narcolepsy Type 1

(2020) Maaike E. Straat et al.   Frontiers in Endocrinology

Evolution of Orexin Neuropeptide System: Structure and Function

(2020) Shingo Soya et al.   Frontiers in Neuroscience

Re‐examining the ‘Dissociation Model’ of G protein activation from the perspective of Gβγ signaling

(2020) Yin Kwan Chung et al.   FEBS Journal

The neurobiological underpinning of the circadian wake signal

(2020) Jamie M. Zeitzer   BIOCHEMICAL PHARMACOLOGY

Therapeutic resistance of pancreatic cancer: Roadmap to its reversal

(2020) Sen Yu et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Systemic administration of orexin A ameliorates established experimental autoimmune encephalomyelitis by diminishing neuroinflammation

(2019) Laurine Becquet et al.   Journal of Neuroinflammation

Orexins as Novel Therapeutic Targets in Inflammatory and Neurodegenerative Diseases

(2019) Alain Couvineau et al.   Frontiers in Endocrinology

A Review of Single-Nucleotide Polymorphisms in Orexigenic Neuropeptides Targeting G Protein-Coupled Receptors

(2018) Mark D. Ericson et al.   ACS Chemical Neuroscience

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Crystal Structures of Human Orexin 2 Receptor Bound to the Subtype-Selective Antagonist EMPA

(2018) Ryoji Suno et al.   STRUCTURE

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma

(2018) Stéphanie Dayot et al.   Oncotarget

Hypocretin as a Hub for Arousal and Motivation

(2018) Susan M. Tyree et al.   Frontiers in Neurology

Ectopic expression of OX1R in ulcerative colitis mediates anti-inflammatory effect of orexin-A

(2018) N. Messal et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

The Anti-tumoral Properties of Orexin/Hypocretin Hypothalamic Neuropeptides: An Unexpected Therapeutic Role

(2018) Alain Couvineau et al.   Frontiers in Endocrinology

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An alerting structure: human orexin receptor 1

(2016) Daniel Wacker et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An alerting structure: human orexin receptor 1

(2016) Daniel Wacker et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Peripherally administered orexin improves survival of mice with endotoxin shock

(2016) Yasuhiro Ogawa et al.   eLife

Crucial role of the orexin-B C-terminus in the induction of OX1receptor-mediated apoptosis: analysis by alanine scanning, molecular modelling and site-directed mutagenesis

(2015) Pascal Nicole et al.   BRITISH JOURNAL OF PHARMACOLOGY

Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia

(2015) Anthony J. Roecker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists

(2015) Takashi Nagahara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structures for G-Protein-Coupled Receptor Tetramers in Complex with G Proteins

(2015) Arnau Cordomí et al.   TRENDS IN BIOCHEMICAL SCIENCES

Modeling of the OX1R–orexin-A complex suggests two alternative binding modes

(2015) Lasse Karhu et al.   BMC STRUCTURAL BIOLOGY

Projecting Cancer Incidence and Deaths to 2030: The Unexpected Burden of Thyroid, Liver, and Pancreas Cancers in the United States

(2014) L. Rahib et al.   CANCER RESEARCH

The orexin type 1 receptor is overexpressed in advanced prostate cancer with a neuroendocrine differentiation, and mediates apoptosis

(2014) David Alexandre et al.   EUROPEAN JOURNAL OF CANCER

Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant

(2014) Jie Yin et al.   NATURE

Toward an Understanding of Agonist Binding to Human Orexin-1 and Orexin-2 Receptors with G-Protein-Coupled Receptor Modeling and Site-Directed Mutagenesis

(2013) Alexander Heifetz et al.   BIOCHEMISTRY

Dual orexin receptor antagonists – promising agents in the treatment of sleep disorders

(2013) Artur Pałasz et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Expression of Type 2 Orexin Receptor in Human Endometrium and Its Epigenetic Silencing in Endometrial Cancer

(2013) P. Dehan et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Truncated Orexin Peptides: Structure–Activity Relationship Studies

(2013) Nadezhda A. German et al.   ACS Medicinal Chemistry Letters

Study of Human Orexin-1 and -2 G-Protein-Coupled Receptors with Novel and Published Antagonists by Modeling, Molecular Dynamics Simulations, and Site-Directed Mutagenesis

(2012) Alexander Heifetz et al.   BIOCHEMISTRY

Aberrant Expression of OX1 Receptors for Orexins in Colon Cancers and Liver Metastases: an Openable Gate to Apoptosis

(2011) T. Voisin et al.   CANCER RESEARCH

The Family B1 GPCR: Structural Aspects and Interaction with Accessory Proteins

(2011) Alain Couvineau et al.   CURRENT DRUG TARGETS

Orexins and their receptors from fish to mammals: A comparative approach

(2011) Kari K.Y. Wong et al.   GENERAL AND COMPARATIVE ENDOCRINOLOGY

Origin of Secretin Receptor Precedes the Advent of Tetrapoda: Evidence on the Separated Origins of Secretin and Orexin

(2011) Janice K. V. Tam et al.   PLoS One

Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia

(2010) Christopher D. Cox et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hypocretin/orexin in fish physiology with emphasis on zebrafish

(2009) P. Panula   Acta Physiologica

Orexins/hypocretins and orexin receptors in apoptosis: a mini-review

(2009) M. Laburthe et al.   Acta Physiologica

Discovery of a functional immunoreceptor tyrosine-based switch motif in a 7-transmembrane-spanning receptor: role in the orexin receptor OX1R-driven apoptosis

(2009) Aadil El Firar et al.   FASEB JOURNAL

A hallmark of immunoreceptor, the tyrosine-based inhibitory motif ITIM, is present in the G protein-coupled receptor OX1R for orexins and drives apoptosis: a novel mechanism

(2008) Thierry Voisin et al.   FASEB JOURNAL