Results 111 to 120 of about 3,750,504 (279)

Anti-stress neuropharmacological mechanisms and targets for addiction treatment: A translational framework

open access: yesNeurobiology of Stress, 2018
Stress-related substance use is a major challenge for treating substance use disorders. This selective review focuses on emerging pharmacotherapies with potential for reducing stress-potentiated seeking and consumption of nicotine, alcohol, marijuana ...
Mark K. Greenwald
doaj   +1 more source

The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned fear

open access: yes, 2014
The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned ...
CE Handford (15829580)   +3 more
core  

Switching Spike Plasticity Shapes ACE2 Engagement Across SARS‐CoV‐2 Variants

open access: yesAdvanced Science, EarlyView.
Conformational plasticity governs SARS‐CoV‐2 spike function and ACE2 recognition. Using high‐speed AFM and single‐molecule force spectroscopy, we analyzed the ancestral spike and nine variants, revealing progressive rigidification from Delta, variable plasticity in Omicron sublineages, and JN.1 compaction.
Sarah Stainer   +17 more
wiley   +1 more source

The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors SB269652 May Lead to a New Generation of Antipsychotic Drugs [PDF]

open access: yes, 2017
D2 and D3 dopamine receptors belong to the largest family of cell surface proteins in eukaryotes, the G protein-coupled receptors (GPCRs). Considering their crucial physiological functions and their relatively accessible cellular locations, GPCRs ...
Irene Fasciani   +9 more
core   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

open access: yesAdvanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu   +8 more
wiley   +1 more source

Targeting β2‐Adrenergic Receptor Stability With Lycorine Reveals a Host‐Directed Pathway for Antiviral Defense Against Poxviruses

open access: yesAdvanced Science, EarlyView.
Chronic stress drives autophagy‐mediated β2‐AR degradation, impairing antiviral immunity and promoting poxvirus lethality. Lycorine directly stabilizes β2‐AR to restore host defense, suppress excessive inflammation and improve survival. ABSTRACT Psychological stress is a pervasive yet poorly understood modulator of infectious disease outcomes. Here, we
Xin Zhang   +12 more
wiley   +1 more source

Small-angle neutron scattering studies on the AMPA receptor GluA2 in the resting, AMPA-bound and GYKI-53655-bound states

open access: yesIUCrJ, 2018
The AMPA receptor GluA2 belongs to the family of ionotropic glutamate receptors, which are responsible for most of the fast excitatory neuronal signalling in the central nervous system. These receptors are important for memory and learning, but have also
Andreas Haahr Larsen   +7 more
doaj   +1 more source

A Synthetic Platform for Antibody Junctional Diversification Beyond Natural Constraints

open access: yesAdvanced Science, EarlyView.
ARESEC is a synthetic platform that reconstructs functional V(D)J recombination in HEK293T cells. By introducing RSS elements and co‐expressing RAG1/2 and TdT across all three antibody CDRs, it enables programmable junctional diversification and direct generation of high‐affinity variants targeting PD‐1/PD‐L1, overcoming the evolutionary constraints of
Wang Liu   +3 more
wiley   +1 more source

Targeting the PHB2–ACSL3 Lipid‐Remodeling Axis Overcomes Cisplatin Resistance by Restoring Ferroptosis in Gastric Cancer

open access: yesAdvanced Science, EarlyView.
ABSTRACT Platinum‐based chemotherapy resistance remains a major obstacle in gastric cancer (GC) treatment. Through integrated transcriptomic profiling of cisplatin‐resistant xenografts and pharmacogenomic interrogation of the NCI‐60 dataset, we identified Prohibitin‐2 (PHB2) as a previously unrecognized determinant of chemoresistance.
Liang Xu   +10 more
wiley   +1 more source

Novel binding mode for negative allosteric NMDA receptor modulators

open access: yesJournal of General Physiology
NMDA-type ionotropic glutamate receptors mediate excitatory neurotransmission and synaptic plasticity, but aberrant signaling by these receptors is also implicated in brain disorders. Here, we present the binding site and the mechanism of action for UCM-101, a novel negative NMDA receptor modulator that produces full inhibition of NMDA receptor ...
James S. Lotti   +13 more
openaire   +2 more sources

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