Results 121 to 130 of about 139,314 (301)

Selective Modulation of OTUB1 Noncanonical Function via a bioPhosTAC Strategy

open access: yesAdvanced Science, EarlyView.
This work positions the versatile performance of the peptide‐based bioPhosTAC platform for dissecting phosphorylation‐dependent biology and expanding the scope of induced‐proximity technologies. We demonstrated that selective manipulation of a tyrosine phosphorylation site is sufficient to propagate coordinated cellular consequences.
Seung Un Seo   +7 more
wiley   +1 more source

Two allosteric modulators each binding to its own site.

open access: yes, 2019
Allosteric interaction between tracer X and allosteric modulators A and B at receptor R. Each allosteric modulator binds to its own site, with cooperative interaction between the two sites.
Esam E. El-Fakahany (339452)   +3 more
core   +1 more source

Entropy‐Driven Physical Amplification in Multivalent Biosensing

open access: yesAdvanced Science, EarlyView.
Detecting scarce molecules usually demands enzymatic amplification such as PCR. A statistical‐mechanical theory now reveals a purely physical alternative: distributing a fixed binding strength over more linker arms exponentially lowers the concentration at which multivalent sensors switch on.
Yuhan Peng, Xiuyang Xia, Ran Ni
wiley   +1 more source

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

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

Molecular Modeling Study of a Receptor–Orthosteric Ligand–Allosteric Modulator Signaling Complex

open access: yes
Allosteric modulators (AMs) are considered as a perpetual hotspot in research for their higher selectivity and various effects on orthosteric ligands (OL).
Yixuan Hao (13933634)   +8 more
core   +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

GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models

open access: yes, 2010
Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for treatment of seizures and epilepsy. Previous studies have shown that the endogenous peptide ligand galanin exerts powerful anticonvulsant ...
Roger Baldwin   +9 more
core   +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

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