How neuromembrane lipids modulate membrane proteins: insights from G-protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs)
Lipids play a diverse and critical role in cellular processes in all tissues. The unique lipid
composition of nerve membranes is particularly interesting because it contains, among other …
composition of nerve membranes is particularly interesting because it contains, among other …
Perspectives on Ligand/Protein Binding Kinetics Simulations: Force Fields, Machine Learning, Sampling, and User-Friendliness
Computational techniques applied to drug discovery have gained considerable popularity
for their ability to filter potentially active drugs from inactive ones, reducing the time scale …
for their ability to filter potentially active drugs from inactive ones, reducing the time scale …
Stabilization of interdomain closure by a G protein inhibitor
TD Todd, N Vithani, S Singh, GR Bowman… - Proceedings of the …, 2024 - pnas.org
Inhibitors of heterotrimeric G proteins are being developed as therapeutic agents.
Epitomizing this approach are YM-254890 (YM) and FR900359 (FR), which are efficacious …
Epitomizing this approach are YM-254890 (YM) and FR900359 (FR), which are efficacious …
Multiple recent HCAR2 structures demonstrate a highly dynamic ligand binding and G protein activation mode
A Shenol, R Tenente, M Lückmann, TM Frimurer… - Nature …, 2024 - nature.com
A surprisingly clear picture of the allosteric mechanism connecting G protein-coupled
receptor agonists with G protein binding—and back–is revealed by a puzzle of thirty novel …
receptor agonists with G protein binding—and back–is revealed by a puzzle of thirty novel …
Connexin Gap Junction Channels and Hemichannels: Insights from High-Resolution Structures
M Jagielnicki, I Kucharska, BC Bennett, AL Harris… - Biology, 2024 - mdpi.com
Simple Summary Gap junction channels are composed of an assembly of connexin proteins
and allow direct communication between cells. They are highly conserved across …
and allow direct communication between cells. They are highly conserved across …
Differential G protein activation by the long and short isoforms of the dopamine D2 receptor
Background and Purpose The dopamine D2 receptor is expressed as a short (D2S) and a
long (D2L) isoform with 29 additional amino acids in the third intracellular loop. The D2S …
long (D2L) isoform with 29 additional amino acids in the third intracellular loop. The D2S …
Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors, with
many GPCRs having crucial roles in endocrinology and metabolism. Cryogenic electron …
many GPCRs having crucial roles in endocrinology and metabolism. Cryogenic electron …
Relevance of G protein‐coupled receptor (GPCR) dynamics for receptor activation, signalling bias and allosteric modulation
M Lopez‐Balastegui, TM Stepniewski… - British Journal of …, 2024 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are one of the major drug targets. In recent years,
computational drug design for GPCRs has mainly focused on static structures obtained …
computational drug design for GPCRs has mainly focused on static structures obtained …
G protein-mediated signal transduction: a molecular choreography of G protein activation after GTP binding
E Kostenis, L Jürgenliemke, J Alenfelder - Signal Transduction and …, 2024 - nature.com
A recent report from the Skiniotis group, 1 published in Nature, provides fascinating insight
into the molecular choreography underlying a quintessential cellular signaling mechanism …
into the molecular choreography underlying a quintessential cellular signaling mechanism …
Structural and Computational Insights into Dynamics and Intermediate States of Orexin 2 Receptor Signaling
Orexin 2 receptor (OX2R) is a G protein-coupled receptor (GPCR) whose activation is crucial
to regulation of the sleep-wake cycle. Recently, inactive and active state structures were …
to regulation of the sleep-wake cycle. Recently, inactive and active state structures were …