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Journal of Neuroscience Research, ISSN 0360-4012, 06/2016, Volume 94, Issue 6, pp. 568 - 578
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 02/2019, Volume 164, pp. 499 - 516
Allosteric modulators of G-protein-coupled receptors have lately gained significant traction in drug discovery. Recent studies have shown that allosteric... 
Anti-obesity | Serotonin | Negative allosteric modulator | Food intake | Positive allosteric modulator | 5-HT2C receptor | 5-HT2B receptor | DESIGN | CHEMISTRY, MEDICINAL | AGONISTS | DISCOVERY | (2-PHENYLCYCLOPROPYL)METHYLAMINES | POTENT | INHIBITORS
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 02/2019, pp. 499 - 516
Allosteric modulators of G-protein-coupled receptors have lately gained significant traction in drug discovery. Recent studies have shown that allosteric... 
receptor | Anti-obesity | Negative allosteric modulator | Serotonin | Food intake | Positive allosteric modulator | 5-HT
Journal Article
Neuropharmacology, ISSN 0028-3908, 07/2014, Volume 82, pp. 161 - 173
Previous work has suggested that activation of mGlu5 receptor augments NMDA receptor function and thereby may constitute a rational approach addressing... 
Schizophrenia | Positive allosteric modulator | Neurotoxicity | Metabotropic glutamate receptor | Antipsychotic activity | METABOTROPIC GLUTAMATE-RECEPTOR | PROTEIN-KINASE-C | NEGATIVE SYMPTOMS | FRAGILE-X | NEUROSCIENCES | PREFRONTAL CORTEX | NEURONAL DAMAGE | PHARMACOLOGY & PHARMACY | LONG-TERM POTENTIATION | BINDING-SITES | ACUTE STRESS | METHYL-D-ASPARTATE | Antipsychotic Agents - toxicity | Neurons - pathology | Cricetulus | Rats, Wistar | Benzamides - pharmacokinetics | Allosteric Regulation | Humans | Male | Excitatory Amino Acid Agents - pharmacokinetics | Mice, 129 Strain | Necrosis - pathology | Excitatory Amino Acid Agents - chemistry | Oxadiazoles - toxicity | Receptor, Metabotropic Glutamate 5 - genetics | Necrosis - physiopathology | Neurotoxicity Syndromes - pathology | Neurons - physiology | Female | Cell Death - drug effects | Neurons - drug effects | Oxadiazoles - chemistry | Oxadiazoles - pharmacokinetics | Benzamides - chemistry | CHO Cells | Benzamides - toxicity | Brain - physiopathology | Cells, Cultured | Antipsychotic Agents - pharmacokinetics | Receptor, Metabotropic Glutamate 5 - metabolism | Rats, Sprague-Dawley | Mice, Knockout | Brain - drug effects | Excitatory Amino Acid Agents - toxicity | Animals | Antipsychotic Agents - chemistry | Cell Death - physiology | Neurotoxicity Syndromes - physiopathology | Brain - pathology | Methyl aspartate | Antipsychotic drugs | Glutamate | Index Medicus
Journal Article
JOURNAL OF BIOLOGICAL CHEMISTRY, ISSN 0021-9258, 08/2019, Volume 294, Issue 32, pp. 12132 - 12145
Nicotinic acetylcholine receptor (nAChR) ligands that lack agonist activity but enhance activation in the presence of an agonist are called positive allosteric... 
nicotinic acetylcholine receptors (nAChR) | ACTIVATION | DOMAIN | MECHANISM | drug design | DOCKING | DESENSITIZATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | ALPHA-5 | allosteric regulation | SOFTWARE | molecular docking | receptor desensitization | positive allosteric modulator | AGONIST | SUBUNIT | Index Medicus
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 04/2013, Volume 168, Issue 8, pp. 2000 - 2010
Background and Purpose Strong implications in major neurological diseases make the neuronal α4β2 nicotinic ACh receptor (nAChR) a highly interesting drug... 
nicotinic ACh receptor | patch‐clamp | α4β2 | positive allosteric modulator | NS9283 | patch-clamp | Drug Synergism | Patch-Clamp Techniques | Receptors, Nicotinic - metabolism | Acetylcholine - pharmacology | Oxadiazoles - pharmacology | Humans | HEK293 Cells | Pyridines - pharmacology | Nicotinic Agonists - pharmacology | Beta | Research Papers
Journal Article
Nature Reviews Immunology, ISSN 1474-1733, 2011, Volume 11, Issue 12, pp. 837 - 851
All animals, including humans, live in symbiotic association with microorganisms. The immune system accommodates host colonization by the microbiota, maintains... 
DROSOPHILA IMMUNE-RESPONSE | L-ALANINE AMIDASE | GRAM-POSITIVE BACTERIA | IMD-PATHWAY | PATTERN-RECOGNITION | STRUCTURAL BASIS | NEGATIVE BACTERIA | GUT MICROBIOTA | IMMUNOLOGY | PGRP-LC | INNATE IMMUNITY | Peptidoglycan - metabolism | Invertebrates - microbiology | Humans | Vertebrates - immunology | Symbiosis - immunology | Vertebrates - microbiology | Embryo, Nonmammalian - immunology | Structure-Activity Relationship | Antimicrobial Cationic Peptides - metabolism | Peptidoglycan - immunology | Host-Pathogen Interactions - immunology | Animal Structures - microbiology | Inflammation - metabolism | Conserved Sequence | Carrier Proteins - chemistry | Carrier Proteins - immunology | Carrier Proteins - physiology | Protein Structure, Tertiary | Homeostasis - immunology | Models, Molecular | Host-Parasite Interactions - immunology | Inflammation - immunology | Embryo, Nonmammalian - microbiology | Eukaryota - immunology | Immunity, Innate | Animals | Intestines - microbiology | Models, Biological | Invertebrates - immunology | Protein Conformation | Metagenome - immunology | Cellular proteins | Cell receptors | Transcription factors | Colon cancer | Physiological aspects | Genetic aspects | Research | Risk factors | peptidoglycan recognition proteins | Pathogens | Microorganisms | Commensals | Homeostasis | Inflammation | Pattern recognition | Colonization | Immune system | Life Sciences | Cellular Biology | Development Biology
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1714 - 1718
This letter describes progress towards an M-4 PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-c[... 
CHEMISTRY, MEDICINAL | SERIES | SAR | CHEMISTRY, ORGANIC | RECEPTOR | DISCOVERY | CHALLENGES | Muscarinic acetylcholine receptor | Structure-activity relationship (SAR) | M-4 | Positive allosteric modulator (PAM) | OPTIMIZATION | Pharmacokinetics
Journal Article
PLOS ONE, ISSN 1932-6203, 01/2016, Volume 11, Issue 1, p. e0146517
Purpose The determination of the molecular mechanism underlying retinal pathogenesis and visual dysfunction during innate inflammation, and the treatment... 
OCULAR INFLAMMATION | MECHANISM | PATHWAY | II TYPE-1 RECEPTOR | MULTIDISCIPLINARY SCIENCES | RHODOPSIN | DEGRADATION | DIABETIC MACULAR EDEMA | ENDOTOXIN-INDUCED UVEITIS | SUPPRESSION | SIROLIMUS | Neuroprotective Agents - therapeutic use | Retina - drug effects | Sirolimus - therapeutic use | Signal Transduction | Uveitis - drug therapy | Mice, Inbred C57BL | Male | NF-kappa B - metabolism | Retina - immunology | Sirolimus - pharmacology | Retinitis - immunology | Animals | Neuroprotective Agents - pharmacology | Retinitis - drug therapy | Inflammation - drug therapy | Uveitis - immunology | Mice | Post-transcription | Diabetic retinopathy | Disease | Pathogenesis | Photopigments | Retina | Immunoblotting | Positive feedback | Proteins | Cell activation | Physiology | Inhibition | Electroretinography | NF-κB protein | Rhodopsin | Cytokines | Rapamycin | Gene expression | Concanavalin A | Protein synthesis | Monocyte chemoattractant protein | Phagocytosis | Monocyte chemoattractant protein 1 | TOR protein | Neuroprotection | Laboratories | Interleukin | Adhesion tests | Clinical trials | Biology | Activation | Feedback loops | Rod outer segment membranes | Kinases | Autophagy | Visual perception | Interleukin 6 | Rodents | Uveitis | Edema | Stat3 protein | Inflammation | Adhesion | Medicine | White blood cells | Signaling | Lymphocytes B | Medical prognosis | Retinitis | Diabetes
Journal Article