Results 71 to 80 of about 64,182 (259)

Cardiac GPCRs: GPCR signaling in healthy and failing hearts

open access: yesBiochimica et Biophysica Acta (BBA) - Biomembranes, 2007
G protein-coupled receptors (GPCRs) are widely implicated in human heart disease, making them an important target for cardiac drug therapy. The most commonly studied and clinically targeted cardiac GPCRs include the adrenergic, angiotensin, endothelin, and adenosine receptors.
Salazar, Natasha C.   +2 more
openaire   +2 more sources

Illuminating the life of GPCRs [PDF]

open access: yesCell Communication and Signaling, 2009
The investigation of biological systems highly depends on the possibilities that allow scientists to visualize and quantify biomolecules and their related activities in real-time and non-invasively. G-protein coupled receptors represent a family of very dynamic and highly regulated transmembrane proteins that are involved in various important ...
Beck-Sickinger Annette G, Böhme Ilka
openaire   +3 more sources

Antigen‐Detected NMR for Minimal Epitope Engineering and Structure‐Guided Selection of a NaV1.7‐Selective Nanobody

open access: yesAdvanced Science, EarlyView.
A minimal extracellular epitope from voltage‐gated sodium channel NaV1.7 was engineered into an isotope‐labelled antigen for antigen‐detected nuclear magnetic resonance (NMR). Together with AlphaFold2 (AF2), this enabled structure‐guided selection of R4C8, a human NaV1.7‐selective nanobody that labels fixed NaV1.7‐expressing cells and produces staining
Junyu Liu   +27 more
wiley   +1 more source

Site‐Specific Protein Bioconjugation Through Cellular Incorporation of Noncanonical Amino Acids

open access: yesAngewandte Chemie, EarlyView.
Genetic code expansion (GCE) enables site‐specific installation of noncanonical amino acids containing bioorthogonal conjugation handles, allowing precise, homogeneous protein modification. This review examines the principles of orthogonal translation, surveys the chemistries available for chemoselective labeling, and highlights emerging multi‐site ...
Rahul Sarkar   +2 more
wiley   +2 more sources

Dampening of neurotransmitter action: molecular similarity within the melatonin structure

open access: yesEndocrine Regulations, 2018
Objectives. Melatonin initiates physiologic and therapeutic responses in various tissues through binding to poorly defined MT receptors regulated by G-proteins and purine nucleotides.
Williams Wynford R.
doaj   +1 more source

Spatial Transcriptomics Reveals a T Cell‐Mediated Microglial Activation Axis of Immune Checkpoint Inhibition‐Related Adverse Events in the Brain

open access: yesAdvanced Science, EarlyView.
Immune checkpoint inhibition (ICI) reshapes the hippocampal neuroimmune niche. Spatial transcriptomic profiling and human brain histological analyses identify neuroinflammation and altered neuronal and glial programs. Notably, T cell depletion prevents ICI‐driven microglial activation, establishing the T cell–microglia crosstalk axis as a driving ...
Devyani Swami   +7 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

open access: yesAngewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma   +5 more
wiley   +2 more sources

Astrocytes Coordinate Neurovascular Coupling During Prolonged Sensory Demand via AQP4/TRPA1/BEST1/D‐Serine Signaling

open access: yesAdvanced Science, EarlyView.
Neuronal activation leads to astrocytic transient volume changes, activating transient receptor potential ankyrin 1 (TRPA1) channels, leading to Ca2+ influx. Activation of TRPA1 causes the release of D‐serine through BEST1. Finally, the augmented extracellular levels of D‐serine boost neuronal activity by binding GluN1‐containing NMDARs, leading to CBV
Kayoung Han   +11 more
wiley   +1 more source

Cannabinoid CB1 Receptor in Nociceptors Mediates Postoperative Analgesia via ASIC3 Inhibition

open access: yesAdvanced Science, EarlyView.
CB1R and ASIC3 are co‐expressed in CGRP+ nociceptors of mouse DRG. Plantar incision triggers an upregulation of ASIC3 and activation of ASIC3+ neurons, driving mechanical allodynia. CB1R activation suppresses ASIC3 function and downstream ERK1/2 phosphorylation, thereby braking nociceptive signaling and accelerating pain resolution.
Kangtai Xu   +13 more
wiley   +1 more source

Molecular Basis of NPY Recognition and Ligand Selectivity at the Neuropeptide Y5 Receptor

open access: yesAngewandte Chemie, EarlyView.
Here, we present the first active structure of the neuropeptide Y5 receptor (NPY5R) in complex with its endogenous ligand NPY and the Gi1 protein. The cryo‐electron microscopy structure, validated by extensive mutagenesis studies, gives important insights into the molecular mechanisms underlying ligand binding and receptor activation.
Lisa Christin Peuker   +8 more
wiley   +2 more sources

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