Gregory Zilberg
YOU?
Author Swipe
View article: Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor
Structural and dynamic studies uncover a distinct allosteric modulatory site at the μ-opioid receptor Open
Positive allosteric modulators (PAMs) of the μ opioid receptor (MOR) offer a promising path toward safer opioid therapeutics, yet their mechanisms of action remain poorly understood. Here, we uncover the structural and mechanistic basis of…
View article: Structural determinants of G protein subtype selectivity at the serotonin receptor 5-HT1A
Structural determinants of G protein subtype selectivity at the serotonin receptor 5-HT1A Open
Activation of the serotonin receptor 5-HT1A has been shown to regulate mood and cognition, making 5-HT1A an important target in the treatment of anxiety, depression, and psychosis. Although the receptor signals through inhibitory G protein…
View article: Structural insights into the unexpected agonism of tetracyclic antidepressants at serotonin receptors 5-HT <sub>1e</sub> R and 5-HT <sub>1F</sub> R
Structural insights into the unexpected agonism of tetracyclic antidepressants at serotonin receptors 5-HT <sub>1e</sub> R and 5-HT <sub>1F</sub> R Open
Serotonin [5-hydroxytryptamine (5-HT)] acts via 13 different receptors in humans. Of these receptor subtypes, all but 5-HT 1e R have confirmed roles in native tissue and are validated drug targets. Despite 5-HT 1e R’s therapeutic potential…
View article: Molecular basis of human trace amine-associated receptor 1 activation
Molecular basis of human trace amine-associated receptor 1 activation Open
The human trace amine-associated receptor 1 (hTAAR1, hTA1) is a key regulator of monoaminergic neurotransmission and the actions of psychostimulants. Despite preclinical research demonstrating its tractability as a drug target, its molecul…
View article: Structural Insights into the Unexpected Agonism of Tetracyclic Antidepressants at Serotonin Receptors 5-HT<sub>1e</sub>R and 5-HT<sub>1F</sub>R
Structural Insights into the Unexpected Agonism of Tetracyclic Antidepressants at Serotonin Receptors 5-HT<sub>1e</sub>R and 5-HT<sub>1F</sub>R Open
Serotonin (5-hydroxytryptamine, 5-HT) acts via 13 different receptors in humans. Of these receptor subtypes, all but 5-HT 1e R have confirmed roles in native tissue and are validated drug targets. Despite 5-HT 1e R’s therapeutic potential …
View article: Molecular Basis of Human Trace Amine-Associated Receptor 1 Activation
Molecular Basis of Human Trace Amine-Associated Receptor 1 Activation Open
The human trace amine-associated receptor 1 (hTAAR1, hTA1) is a key regulator of monoaminergic neurotransmission and the actions of psychostimulants. Despite preclinical research demonstrating its tractability as a drug target, its molecul…
View article: Substrate Binding and Inhibition of the Anion Exchanger 1 Transporter
Substrate Binding and Inhibition of the Anion Exchanger 1 Transporter Open
Anion Exchanger 1 (AE1, SLC4A1) is the primary bicarbonate (HCO 3 - ) transporter expressed in erythrocyte membranes where it mediates transport of CO 2 between lungs and other tissues via import/export of bicarbonate. It is also a key reg…
View article: A Novel Cryo-EM Structure Enables Development of Selective Cannabinoid Receptor Drugs
A Novel Cryo-EM Structure Enables Development of Selective Cannabinoid Receptor Drugs Open
ADVERTISEMENT RETURN TO ISSUEPREVViewpointNEXTA Novel Cryo-EM Structure Enables Development of Selective Cannabinoid Receptor DrugsGregory ZilbergGregory ZilbergDepartment of Neuroscience, Icahn School of Medicine at Mount Sinai, New York,…
View article: Fife organizes synaptic vesicles and calcium channels for high-probability neurotransmitter release
Fife organizes synaptic vesicles and calcium channels for high-probability neurotransmitter release Open
The strength of synaptic connections varies significantly and is a key determinant of communication within neural circuits. Mechanistic insight into presynaptic factors that establish and modulate neurotransmitter release properties is cru…