Results 121 to 130 of about 1,156,973 (433)

Photochromic G-Protein Coupled Receptor Ligands [PDF]

, 2020
Diese Dissertation behandelt die Synthese, photophysikalische Charakterisierung und Anwendung von photochromen G-Protein gekoppelten Rezeptor-Liganden.
Lachmann, Daniel
core  

Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]

, 2017
The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M., Benovic, Jeffrey L., Betz, Robin M., Chung, Ka Young, Dror, Ron O., Du, Yang, Duc, Nguyen Minh, Kobilka, Brian K., Komolov, Konstantin E., Leib, Ryan D., Patra, Dhabaleswar, Rodrigues, João P.G.L.M., Skiniotis, Georgios   +12 more
core   +2 more sources

STAT3 expression is reduced in cardiac pericytes in HFpEF and its loss reduces cellular adhesion and induces pericyte senescence

FEBS Letters, EarlyView.
Heart failure with preserved ejection fraction (HFpEF) accounts for half of the heart failure cases. It is characterised by microvascular dysfunction, associated with reduced pericyte coverage and diminished STAT3 expression in pericytes. Loss of STAT3 impairs pericyte adhesion, promotes senescence, and activates a pro‐fibrotic gene program.
Leah Rebecca Vanicek, Ariane Fischer, Mariano Ruz Jurado, Anita Tamiato, Tara Procida‐Kowalski, Jochen Wilhelm, Dennis Hecker, Maximilian Merten, Felicitas Escher, Badder Kattih, Valentina Puntmann, David John, Marcel H. Schulz, Eike Nagel, Stefanie Dimmeler, Guillermo Luxán   +15 more
wiley   +1 more source

Functionally distinct and selectively phosphorylated GPCR subpopulations co-exist in a single cell. [PDF]

, 2018
G protein-coupled receptors (GPCRs) transduce pleiotropic intracellular signals in a broad range of physiological responses and disease states. Activated GPCRs can undergo agonist-induced phosphorylation by G protein receptor kinases (GRKs) and second ...
Chowdhury, Dhrubajyoti, Deng, Yawen, Hell, Johannes W, Navedo, Manuel F, Nieves-Cintron, Madeline, Qi, Jinyi, Shen, Ao, Shi, Qian, Xiang, Yang K   +8 more
core   +3 more sources

Cytoplasmic delivery of antibodies through grafting a functional single complementarity‐determining region loop

FEBS Letters, EarlyView.
We achieved cytoplasmic delivery of non‐cell‐penetrating IgGs by grafting a single functional complementarity‐determining region 1 (CDR1) from the light chain variable region (VL) of the cell‐internalizable 3D8 antibody. The engineered IgG acquired cell‐penetrating ability while maintaining antigen affinity, highlighting CDR1 grafting as a promising ...
Yerin Jeon, Juho Choi, Youngin Roh, Eunbin Lee, Luigie Villamante, Myung‐Hee Kwon   +5 more
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  

Ion channel function of polycystin‐2/polycystin‐1 heteromer revealed by structure‐guided mutagenesis

FEBS Letters, EarlyView.
Mutations in polycystin‐1 (PC1) or polycystin‐2 (PC2) cause autosomal‐dominant polycystic kidney disease (ADPKD). We generated a novel gain‐of‐function PC2/PC1 heteromeric ion channel by mutating pore‐blocking residues. Moreover, we demonstrated that PC2 will preferentially assemble with PC1 to form heteromeric complexes when PC1 is co‐expressed ...
Tobias Staudner, Juthamas Khamseekaew, M. Gregor Madej, Linda Geiges, Bardha Azemi, Christine Ziegler, Christoph Korbmacher, Alexandr V. Ilyaskin   +7 more
wiley   +1 more source

Kynurenic Acid as a Ligand for Orphan G Protein-coupled Receptor GPR35*

Journal of Biological Chemistry, 2006
Local catabolism of the essential amino acid tryptophan is considered an important mechanism in regulating immunological and neurological responses. The kynurenine pathway is the main route for the non-protein metabolism of tryptophan.
Jinghong Wang, Nicole Simonavicius, Xiaosu Wu, G. Swaminath, J. Reagan, H. Tian, L. Ling   +6 more
semanticscholar   +1 more source

Scalable Production of Highly-Sensitive Nanosensors Based on Graphene Functionalized with a Designed G Protein-Coupled Receptor [PDF]

, 2014
We have developed a novel, all-electronic biosensor for opioids that consists of an engineered mu opioid receptor protein, with high binding affinity for opioids, chemically bonded to a graphene field-effect transistor to read out ligand binding. A variant of the receptor protein that provided chemical recognition was computationally redesigned to ...
arxiv   +1 more source

Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]

, 2003
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio, Marinissen, Maria Julia, Offermanns, Stefan, Servitja, Joan-Marc, Simon, Melvin I.   +4 more
core   +1 more source