Allosteric modulators are substances that can control how proteins work. They can attach to a protein in a place that is different than where other substances usually attach, and change the protein's shape or activity. This can either increase or decrease the protein's function, making
allosteric modulators useful for regulating key processes in the body.
Full definition
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.
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 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).
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..
• 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).
The research, which appears in the journal Biological Psychiatry, finds that the use of compounds called
positive allosteric modulators, or PAMs, enhances the effect of pain - relief chemicals naturally produced by the body in response to stress or injury.
The findings indicate that compounds known as positive
allosteric modulators, or PAMS, can increase the natural pain - relief chemicals produced by the body in response to injury.
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).
Phrases with «allosteric modulators»