Affiliation: F. Hoffmann-La Roche Ltd
- Trace amine-associated receptors form structurally and functionally distinct subfamilies of novel G protein-coupled receptorsLothar Lindemann
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, CH 4070 Basel, Switzerland
Genomics 85:372-85. 2005..We propose a uniform nomenclature describing this novel GPCR family in all mammalian species as trace-amine-associated receptors (TAARs), which resolves the ambiguities and contradictions of the previous naming...
- A renaissance in trace amines inspired by a novel GPCR familyLothar Lindemann
F Hoffmann La Roche, Pharmaceuticals Division, Discovery Neuroscience, CH 4070 Basel, Switzerland
Trends Pharmacol Sci 26:274-81. 2005..Current research focuses on dissecting their molecular pharmacology and on the identification of endogenous ligands for the apparently TA-insensitive members of this receptor family...
- CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitorLothar Lindemann
F Hoffmann La Roche Ltd Pharmaceuticals Division, Discovery Neuroscience, Grenzacherstrasse 124, 4070 Basel, Switzerland
J Pharmacol Exp Ther 339:474-86. 2011..By enabling long-term treatment through a wide age range, CTEP allows the exploration of the full therapeutic potential of mGlu5 inhibitors for indications requiring chronic receptor inhibition...
- Chronic pharmacological mGlu5 inhibition corrects fragile X in adult miceAubin Michalon
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche, CH 4070 Basel, Switzerland
Neuron 74:49-56. 2012..It is of great interest how these findings may translate into ongoing clinical research testing mGlu5 inhibitors in FXS patients...
- G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a surveyNicole A Kratochwil
Pharma Research and Early Development, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland and Nutley, New Jersey 07110 1199, USA
Curr Top Med Chem 11:1902-24. 2011..Illustrative examples are taken from the GPCR family class C, metabotropic glutamate receptors 1 and 5 and sweet taste receptors, and from the GPCR class A, e.g. nicotinic acid and 5-hydroxytryptamine 5A receptor...
- An automated system for the analysis of G protein-coupled receptor transmembrane binding pockets: alignment, receptor-based pharmacophores, and their applicationNicole A Kratochwil
Pharmaceuticals Division, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
J Chem Inf Model 45:1324-36. 2005..The value of the 3D receptor model is demonstrated for a class C GPCR family, the metabotropic glutamate receptors...
- In vitro pharmacological selectivity profile of oseltamivir prodrug (Tamiflu) and active metaboliteLothar Lindemann
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche Ltd, Basel, Switzerland
Eur J Pharmacol 628:6-10. 2010..Neuropsychiatric adverse events observed in influenza patients are likely a phenomenon caused by the infection rather than by oseltamivir...
- Synapse dysfunction in autism: a molecular medicine approach to drug discovery in neurodevelopmental disordersWill Spooren
CNS Research and Early Clinical Development, F Hoffmann La Roche Ltd, 4070 Basel, Switzerland Electronic address
Trends Pharmacol Sci 33:669-84. 2012..Here, we review the opportunities and challenges in drug development for autism and provide insight into the neurobiology of ASDs...
- Trace amine-associated receptor 1 modulates dopaminergic activityLothar Lindemann
Pharmaceuticals Division, Central Nervous System Research, Department PRDNP5 CH, Bldg 70 331, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
J Pharmacol Exp Ther 324:948-56. 2008..Taken together, the data reveal TAAR1 as regulator of dopaminergic neurotransmission...