The path to the G protein‐coupled receptor structural landscape: Major milestones and future directions

MM Kogut‐Günthel, Z Zara, A Nicoli… - British Journal of …, 2024 - Wiley Online Library
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing
signals from the extracellular environment to the inside of the cell. They mediate the effects …

Chemokines in the tumor microenvironment: implications for lung cancer and immunotherapy

H Jung, S Paust - Frontiers in Immunology, 2024 - frontiersin.org
The tumor microenvironment (TME) is a complex interconnected network of immune cells,
fibroblasts, blood vessels, and extracellular matrix surrounding the tumor. Because of its …

Interaction and dynamics of chemokine receptor CXCR4 binding with CXCL12 and hBD-3

J Penfield, L Zhang - Communications Chemistry, 2024 - nature.com
Chemokine receptor CXCR4 is involved in diverse diseases. A comparative study was
conducted on CXCR4 embedded in a POPC lipid bilayer binding with CXCL12 in full and …

Allosteric modulation of the CXCR4: CXCL12 axis by targeting receptor nanoclustering via the TMV-TMVI domain

EM García-Cuesta, P Martínez, K Selvaraju, G Ulltjärn… - Elife, 2024 - elifesciences.org
CXCR4 is a ubiquitously expressed chemokine receptor that regulates leukocyte trafficking
and arrest in both homeostatic and pathological states. It also participates in organogenesis …

Free-energy landscapes of transmembrane homodimers by bias-exchange adaptively biased molecular dynamics

S Ito, Y Sugita - Biophysical Chemistry, 2024 - Elsevier
Membrane proteins play essential roles in various biological functions within the cell. One of
the most common functional regulations involves the dimerization of two single-pass …

Minute-timescale free-energy calculations reveal a pseudo-active state in the adenosine A2A receptor activation mechanism

VM D'Amore, P Conflitti, L Marinelli, V Limongelli - Chem, 2024 - cell.com
G protein-coupled receptors (GPCRs) are membrane proteins targeted by over one-third of
marketed drugs. Understanding their activation mechanism is essential for precise …

A homotrimeric GPCR architecture of the human cytomegalovirus revealed by cryo-EM

Y Chen, Y Li, Q Zhou, Z Cong, S Lin, J Yan, X Chen… - Cell Discovery, 2024 - nature.com
Dear Editor, Herpesviruses encode G protein-coupled receptors (GPCRs) in their viral
genomes and express these receptors in infected host cells to reprogram cell signaling …

Computational Characterization of Membrane Proteins as Anticancer Targets: Current Challenges and Opportunities

M Gorostiola González, PRJ Rakers, W Jespers… - International Journal of …, 2024 - mdpi.com
Cancer remains a leading cause of mortality worldwide and calls for novel therapeutic
targets. Membrane proteins are key players in various cancer types but present unique …

Early Events in β2AR Dimer Dynamics Mediated by Activation-Related Microswitches

A Kotipalli, S Koulgi, V Jani, U Sonavane… - The Journal of Membrane …, 2024 - Springer
Abstract G-Protein-Coupled Receptors (GPCRs) make up around 3–4% of the human
genome and are the targets of one-third of FDA-approved drugs. GPCRs typically exist as …

Disruption of basal CXCR4 oligomers impairs oncogenic properties in lymphoid neoplasms

S Mobach, ND Bergkamp, Z Ma, MV Haselager… - bioRxiv, 2024 - biorxiv.org
The chemokine receptor CXCR4 is overexpressed in many cancers and contributes to
pathogenesis, disease progression, and resistance to therapies. CXCR4 is known to form …