Results 81 to 90 of about 851,179 (309)

Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor [PDF]

, 2012
G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce signals. Although GPCRs represent the largest class of therapeutic targets, only a small percentage of their ligand-binding sites are ...
Abrol, Ravinder, Goddard, William A., III, Grunbeck, Amy, Huber, Thomas, Sakmar, Thomas P., Trzaskowski, Bartosz   +5 more
core   +1 more source

Tau acetylation at K331 has limited impact on tau pathology in vivo

FEBS Letters, EarlyView.
We mapped tau post‐translational modifications in humanized MAPT knock‐in mice and in amyloid‐bearing double knock‐in mice. Acetylation within the repeat domain, particularly around K331, showed modest increases under amyloid pathology. To test functional relevance, we generated MAPTK331Q knock‐in mice.
Shoko Hashimoto, Yukio Matsuba, Mika Takahashi, Takaomi C. Saido   +3 more
wiley   +1 more source

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

Current and future G protein-coupled receptor signaling targets for heart failure therapy

Drug Design, Development and Therapy, 2013
Ashley Siryk-Bathgate, Samalia Dabul, Anastasios Lymperopoulos Laboratory for the Study of Neurohormonal Control of the Circulation, Department of Pharmaceutical Sciences, Nova Southeastern University College of Pharmacy, Fort Lauderdale, FL, USA ...
Siryk-Bathgate A, Dabul S, Lymperopoulos A   +2 more
doaj  

Expression and Role of Gonadotropin-Releasing Hormone 2 and Its Receptor in Mammals

Frontiers in Endocrinology, 2017
Gonadotropin-releasing hormone 1 (GnRH1) and its receptor (GnRHR1) drive mammalian reproduction via regulation of the gonadotropins. Yet, a second form of GnRH (GnRH2) and its receptor (GnRHR2) also exist in mammals.
Amy T. Desaulniers, Rebecca A. Cederberg, Clay A. Lents, Brett R. White   +3 more
doaj   +1 more source

The G protein-coupled receptor heterodimer network (GPCR-HetNet) and its hub components [PDF]

, 2014
G protein-coupled receptors (GPCRs) oligomerization has emerged as a vital characteristic of receptor structure. Substantial experimental evidence supports the existence of GPCR-GPCR interactions in a coordinated and cooperative manner.
Agnati, Luigi F, Borroto-Escuela, Dasiel O, Brito, Ismel, Di Palma, Michael, Duchou, Jolien, Fuxe, Kjell, Guidolin, Diego, Oflijan, Julia, Rivera, Alicia, Romero-Fernandez, Wilber, Skieterska, Kamila, Suárez-Boomgaard, Diana, Van Craenenbroeck, Kathleen   +12 more
core   +4 more sources

G PROTEIN–COUPLED RECEPTOR KINASES [PDF]

Annual Review of Biochemistry, 1998
G protein–coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein–coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
J A, Pitcher, N J, Freedman, R J, Lefkowitz   +2 more
openaire   +2 more sources

Valosin‐containing protein counteracts ATP‐driven dissolution of FUS condensates through its ATPase activity in vitro

FEBS Letters, EarlyView.
Biomolecular condensates formed by fused in sarcoma (FUS) are dissolved by high ATP concentrations yet persist in cells. Using a reconstituted system, we demonstrate that valosin‐containing protein (VCP), an AAA+ ATPase, counteracts ATP‐driven dissolution of FUS condensates through its D2 ATPase activity.
Hitomi Kimura, Shin‐ichi Tate, Kyota Yasuda   +2 more
wiley   +1 more source

The role of orphan G protein-coupled receptors in pain

Heliyon
G protein-coupled receptors (GPCRs), which form the largest family of membrane protein receptors in humans, are highly complex signaling systems with intricate structures and dynamic conformations and locations.
Chengfei Xu, Yahui Wang, Huadong Ni, Ming Yao, Liang Cheng, Xuewu Lin   +5 more
doaj   +1 more source

Estrogen, angiogenesis, immunity and cell metabolism: Solving the puzzle [PDF]

, 2018
Estrogen plays an important role in the regulation of cardiovascular physiology and the immune system by inducing direct effects on multiple cell types including immune and vascular cells. Sex steroid hormones are implicated in cardiovascular protection,
Bolego, Chiara, BOSCARO, CARLOTTA, Cignarella, Andrea, Tedesco, Serena, Trenti, Annalisa, Trevisi, Lucia   +5 more
core   +2 more sources