Results 121 to 130 of about 5,959,864 (346)

Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators

Frontiers in Pharmacology
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten, Katrijn Boon, Max Van Hoof, Wim Dehaen, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Steven De Jonghe, Tom Van Loy   +8 more
doaj   +1 more source

A new target for G protein signaling

eLife, 2017
G protein-coupled receptor stimulation inhibits TRPM3 channel activity through direct binding of the Gβγ subunit to the channel.
László Csanády
doaj   +1 more source

Joint Public Review: Dynamic allosteric networks drive adenosine A1 receptor activation and G-protein coupling

, 2023

openalex   +1 more source

No evidence for oncogenic mutations in guanine nucleotide-binding proteins of human adrenocortical neoplasms [PDF]

, 1933
G-Proteins are membrane-bound heterotrimeric polypeptides that couple receptor signals to second messenger systems such as cAMP. Recently, point mutations at 2 codons of the highly preserved alpha-chain of Gs, the adenyl cyclase-stimulating G-protein ...
Chrousos, G. P., Karl, M., Reincke, Martin, Travis, W.   +3 more
core  

Structural instability impairs function of the UDP‐xylose synthase 1 Ile181Asn variant associated with short‐stature genetic syndrome in humans

FEBS Letters, EarlyView.
The Ile181Asn variant of human UDP‐xylose synthase (hUXS1), associated with a short‐stature genetic syndrome, has previously been reported as inactive. Our findings demonstrate that Ile181Asn‐hUXS1 retains catalytic activity similar to the wild‐type but exhibits reduced stability, a looser oligomeric state, and an increased tendency to precipitate ...
Tuo Li, Pedro A. Sánchez‐Murcia, Bernd Nidetzky   +2 more
wiley   +1 more source

Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor

Nature Communications, 2018
G protein-coupled receptors (GPCRs) activate and dissociate the G protein heterotrimer into Gα-GTP and Gβγ dimer, which facilitate distinct signalling events.
Sahil Gulati, Hui Jin, Ikuo Masuho, Tivadar Orban, Yuan Cai, Els Pardon, Kirill A. Martemyanov, Philip D. Kiser, Phoebe L. Stewart, Christopher P. Ford, Jan Steyaert, Krzysztof Palczewski   +11 more
doaj   +1 more source

Additional file 2 of O-GlcNAcylation protein disruption by Thiamet G promotes changes on the GBM U87-MG cells secretome molecular signature

, 2021
Maria Cecília Oliveira-Nunes, Glaucia Julião, Aline Menezes, Fernanda Mariath, John A. Hanover, Joseph Albert Medeiros Evaristo, Fábio César Sousa Nogueira, Wagner B. Dias, Denise de Abreu Pereira, K. Carneiro   +9 more
openalex   +1 more source

PICALM::MLLT10 translocated leukemia

FEBS Letters, EarlyView.
This comprehensive review of PICALM::MLLT10 translocated acute leukemia provides an in‐depth review of the structure and function of CALM, AF10, and the fusion oncoprotein (1). The multifaceted molecular mechanisms of oncogenesis, including nucleocytoplasmic shuttling (2), epigenetic modifications (3), and disruption of endocytosis (4), are then ...
John M. Cullen, Antonia C. Nakatsugawa, Natalie Barton, Henry Haines, Gary S. Stein, Janet L. Stein, Daniel S. Wechsler, Jessica L. Heath   +7 more
wiley   +1 more source

Structural mechanism underlying G protein family-specific regulation of G protein-gated inwardly rectifying potassium channel

Nature Communications, 2019
Opening of G protein-gated inwardly rectifying potassium channels (GIRK) is coupled to the activation of a GPCR. Here the authors use NMR and cell-based BRET assays to gain insights into the mechanisms underlying family-specific activation and find that ...
Hanaho Kano, Yuki Toyama, Shunsuke Imai, Yuta Iwahashi, Yoko Mase, Mariko Yokogawa, Masanori Osawa, Ichio Shimada   +7 more
doaj   +1 more source

Polarity conserved positions in transmembrane domains of G‐protein coupled receptors and bacteriorhodopsin [PDF]

, 1994
Daqun Zhang, Harel Weinstein
openalex   +1 more source