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News from DMCCB - Targeted Protein Degradation

Chimia, 2018-12, Vol.72 (12), p.903

Jaeschke, Georg

2018

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Contribution of mGluR5 to pathophysiology in a mouse model of human chromosome 16p11.2 microdeletion

Nature neuroscience, 2015-02, Vol.18 (2), p.182-184

2015

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Chemical, Analytical and Pharmacokinetic Characterisation of RO7304898, an API Consisting of Two Rapidly Interconverting Diastereoisomers

Pharmaceutical research, 2022-04, Vol.39 (4), p.653-667

2022

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mGluR5 Modulation of Behavioral and Epileptic Phenotypes in a Mouse Model of Tuberous Sclerosis Complex

Neuropsychopharmacology (New York, N.Y.), 2018-05, Vol.43 (6), p.1457-1465

2018

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Chronic Metabotropic Glutamate Receptor 5 Inhibition Corrects Local Alterations of Brain Activity and Improves Cognitive Performance in Fragile X Mice

Biological psychiatry (1969), 2014-02, Vol.75 (3), p.189-197

2014

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Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities

ChemMedChem, 2007-08, Vol.2 (8), p.1100-1115

2007

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CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor

The Journal of pharmacology and experimental therapeutics, 2011-11, Vol.339 (2), p.474

2011

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Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity

The Journal of pharmacology and experimental therapeutics, 2005-11, Vol.315 (2), p.711

2005

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Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2‑Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl‑1H‑imidazol-4-ylethynyl]pyridine (Basimglurant, RO4917523), a Promising Novel Medicine for Psychiatric Diseases

Journal of medicinal chemistry, 2015-02, Vol.58 (3), p.1358-1371

2015

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Enantioselective total synthesis of callipeltoside A: two approaches to the macrolactone fragment

Tetrahedron, 2008-05, Vol.64 (21), p.4671-4699

2008

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Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP

Journal of neurochemistry, 2006-07, Vol.98 (2), p.601-615

2006

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Enantioselective Total Synthesis of Callipeltoside A

Journal of the American Chemical Society, 2002-05, Vol.124 (20), p.5654-5655

2002

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Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors

European journal of pharmacology, 2006-01, Vol.529 (1), p.95-104

2006

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Metabotropic glutamate receptor 5 as drug target for Fragile X syndrome

Current opinion in pharmacology, 2015-02, Vol.20, p.124-134

2015

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Differential effects of diazepam and MPEP on habituation and neuro-behavioural processes in inbred mice

Behavioral and brain functions, 2012-06, Vol.8 (1), p.30-30

2012

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Chronic Pharmacological mGlu5 Inhibition Corrects Fragile X in Adult Mice

Neuron (Cambridge, Mass.), 2012-04, Vol.74 (1), p.49-56

2012

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Resolution of racemic carboxylic acid derivatives by Ti-TADDOLate mediated esterification reactions—A general method for the preparation of enantiopure compounds

Tetrahedron, 1997-06, Vol.53 (22), p.7539-7556

1997

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Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib

Journal of medicinal chemistry, 2022-10, Vol.65 (19), p.13052-13073

2022

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Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression

The Journal of pharmacology and experimental therapeutics, 2015-04, Vol.353 (1), p.213

2015

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Results and evaluation of a first‐in‐human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methods

British journal of clinical pharmacology, 2018-03, Vol.84 (3), p.445-455

2018

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Blocking metabotropic glutamate receptor subtype 5 relieves maladaptive chronic stress consequences

Brain, behavior, and immunity, 2017-01, Vol.59, p.79-92

2017

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Contribution of mGluR5 to hippocampal pathophysiology in a mouse model of human chromosome 16p11.2 microdeletion

Nature neuroscience, 2015-01, Vol.18 (2), p.182-184

2015

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Yeast Synthetic Biology Platform Generates Novel Chemical Structures as Scaffolds for Drug Discovery

ACS synthetic biology, 2014-05, Vol.3 (5), p.314-323

2014

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mGlu5 receptor antagonists and their therapeutic potential

Expert opinion on therapeutic patents, 2008-02, Vol.18 (2), p.123-142

2008

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Stress-induced hyperthermia: Effects of acute and repeated dosing of MPEP

European journal of pharmacology, 2007-07, Vol.568 (1), p.199-202

2007

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News from DMCCB - Targeted Protein Degradation

Contribution of mGluR5 to pathophysiology in a mouse model of human chromosome 16p11.2 microdeletion

Chemical, Analytical and Pharmacokinetic Characterisation of RO7304898, an API Consisting of Two Rapidly Interconverting Diastereoisomers

mGluR5 Modulation of Behavioral and Epileptic Phenotypes in a Mouse Model of Tuberous Sclerosis Complex

Chronic Metabotropic Glutamate Receptor 5 Inhibition Corrects Local Alterations of Brain Activity and Improves Cognitive Performance in Fragile X Mice

Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities

CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor

Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity

Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2‑Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl‑1H‑imidazol-4-ylethynyl]pyridine (Basimglurant, RO4917523), a Promising Novel Medicine for Psychiatric Diseases

Enantioselective total synthesis of callipeltoside A: two approaches to the macrolactone fragment

Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP

Enantioselective Total Synthesis of Callipeltoside A

Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors

Metabotropic glutamate receptor 5 as drug target for Fragile X syndrome

Differential effects of diazepam and MPEP on habituation and neuro-behavioural processes in inbred mice

Chronic Pharmacological mGlu5 Inhibition Corrects Fragile X in Adult Mice

Resolution of racemic carboxylic acid derivatives by Ti-TADDOLate mediated esterification reactions—A general method for the preparation of enantiopure compounds

Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib

Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression

Results and evaluation of a first‐in‐human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methods

Blocking metabotropic glutamate receptor subtype 5 relieves maladaptive chronic stress consequences

Contribution of mGluR5 to hippocampal pathophysiology in a mouse model of human chromosome 16p11.2 microdeletion

Yeast Synthetic Biology Platform Generates Novel Chemical Structures as Scaffolds for Drug Discovery

mGlu5 receptor antagonists and their therapeutic potential

Stress-induced hyperthermia: Effects of acute and repeated dosing of MPEP

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