A Photochromic Agonist of AMPA Receptors

Stawski, Philipp; Sumser, Martin; Trauner, Dirk

doi:10.1002/anie.201109265

Cited by 80 publications

(81 citation statements)

References 16 publications

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“…Initial PCLs were agonists of GluA2, with the best compound being ATA[7]. The active trans -isomer of ATA allows photo-control of action potential firing in layer 2/3 neurons from mouse cortical slices.…”

Section: Glutamate Receptors (Glurs)mentioning

confidence: 99%

Precise modulation of neuronal activity with synthetic photoswitchable ligands

Kienzler

Isacoff

2017

Current Opinion in Neurobiology

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Section: Glutamate Receptors (Glurs)mentioning

confidence: 99%

Precise modulation of neuronal activity with synthetic photoswitchable ligands

Kienzler

Isacoff

2017

Current Opinion in Neurobiology

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“…A recently obtained structure of trans GluAzo bound to GluK2 might serve as a guide for improving its efficacy as a trans -agonist [22]. The soluble photoswitch approach has also been applied to a series of AMPA receptor specific agonists, called ATAs , based on a benzyltetrazolyl-substituted AMPA derivative [23]. Most recently, Pittolo et al described Alloswitch-1 , a compound based on the mGluR4 positive allosteric modulator (PAM) VUO415374, which functions as a photoswitchable mGluR5-specific negative allosteric modulator (NAM) [24].…”

Section: Soluble Photoswitches (Reversibly ‘Caged’ Ligands)mentioning

confidence: 99%

Controlling ionotropic and metabotropic glutamate receptors with light: principles and potential

Reiner

Levitz

Isacoff

2015

Current Opinion in Pharmacology

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Light offers unique advantages for studying and manipulating biomolecules and the cellular processes that they control. Optical control of ionotropic and metabotropic glutamate receptors has garnered significant interest, since these receptors are central to signaling at neuronal synapses and only optical approaches provide the spatial and temporal resolution required to directly probe receptor function in cells and tissue. Following the classical method of glutamate photo-uncaging, recently developed methods have added other forms of remote control, including those with high molecular specificity and genetic targeting. These tools open the door to the direct optical control of synaptic transmission and plasticity, as well as the probing of native receptor function in intact neural circuits.

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“…However, sufficient structural differences exist between the subfamilies and these differences prevented the direct application or even modification of 4-GluAzo as a PCL of AMPARs and NMDARs. To functionally discriminate between AMPAR and other iGluRs, BnTetAMPA, a highly specific AMPAR agonist with a lipophilic tail was derivatized into AB-tetrazolyl-AMPA-3 (ATA-3) (Stawski et al 2012). Like 4-GluAzo, ATA-3 is functionally active in its dark-adapted trans-isomer.…”

Section: Pcls Of Ligand-gated Ion Channelsmentioning

confidence: 99%

Flipping the Photoswitch: Ion Channels Under Light Control

McKenzie

Sánchez-Romero

Janovjak

2015

Advances in Experimental Medicine and Biology

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Nature has incorporated small photochromic molecules, colloquially termed 'photoswitches', in photoreceptor proteins to sense optical cues in phototaxis and vision. While Nature's ability to employ light-responsive functionalities has long been recognized, it was not until recently that scientists designed, synthesized and applied synthetic photochromes to manipulate biological processes with the temporal and spatial resolution of light. Ion channels in particular have come to the forefront of proteins that can be put under the designer control of synthetic photochromes.Photochromic ion channel controllers are comprised of three classes, photochromic soluble ligands (PCLs), photochromic tethered ligands (PTLs) and photochromic crosslinkers (PXs), and in each class ion channel functionality is controlled through reversible changes in photochrome structure. By acting as light-dependent ion channel agonists, antagonist or modulators, photochromic controllers effectively converted a wide range of ion channels, including voltage-gated ion channels, 'leak channels', tri-, tetra-and pentameric ligand-gated ion channels, and temperaturesensitive ion channels, into man-made photoreceptors. Control by photochromes is reversible, unlike in the case of 'caged' compounds, and non-invasive with high spatial precision, unlike pharmacology and electrical manipulation. Here, we introduce design principles of emerging photochromic molecules that act on ion channels and discuss the impact that these molecules are beginning to have on ion channel biophysics and neuronal physiology.

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A Photochromic Agonist of AMPA Receptors

Cited by 80 publications

References 16 publications

Precise modulation of neuronal activity with synthetic photoswitchable ligands

Precise modulation of neuronal activity with synthetic photoswitchable ligands

Controlling ionotropic and metabotropic glutamate receptors with light: principles and potential

Flipping the Photoswitch: Ion Channels Under Light Control

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