With Jan Stichel at Annette Beck - Sickinger's lab, Leipzig University, Germany and David Weaver, head of the high - throughput screening facilities at Vanderbilt University, I will be screening Vanderbilt's library of small molecules for potential
allosteric modulators of the human Y4 receptor.
The project aims to discover new agonist, antagonist and
allosteric modulators of these receptors mostly orphans.
Administration of a positive
allosteric modulator of the type 1 metabotropic glutamate receptors mGluR1 during the first postnatal week restored DA neuron excitatory synapse transmission and partially rescued the social preference defects, while optogenetic DA neuron stimulation was sufficient to enhance social preference.
Not exact matches
His work helped discover a class
of molecules called core protein
allosteric modulators, or CpAMs, that disrupt capsid protein assembly.
Identification
of an antithrombotic
allosteric modulator that acts through helix 8
of PAR1.
Title: Selective Remediation
of Reversal Learning Deficits in the Neurodevelopmental MAM Model
of Schizophrenia by a Novel mGlu5 Positive
Allosteric Modulator Author: F. Gastambide et al..
Muscarinic receptor M4 positive
allosteric modulators attenuate central effects
of cocaine...
The PI
of the proposal has also experience in cheminformatics method development for chemical biology and therapeutic development (Mueller, R., et al.; «Discovery
of 2 -(2 - Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine as Negative
Allosteric Modulators (NAMs)
of Metabotropic Glutamate Receptor 5 (mGlu5): From an Artificial Neural Network Virtual Screen to an In Vivo Tool Compound»; ChemMedChem; 2012; 7; 406).
One particular focus in our work is structure, dynamics, and interactions
of G - Protein Coupled Receptors (Wu, H.; et al. «Structure
of a class C GPCR metabotropic glutamate receptor 1 bound to an
allosteric modulator»; Science; 2014; 58 or Alexander, N.; et al. «Energetic analysis
of the rhodopsin - G - protein complex links the alpha5 helix to GDP release»; Nat Struct Mol Biol; 2014; 56).
• Alfred J, Uberti M, Dovlatyan M, Li Z, Smith D, Weiss J, Jubian V, Grenon M, Li G, Doller D and Brodbeck R: The Synthesis and invitro pharmacology
of the selective mGLUR5 negative
allosteric modulator (NAM).