Results 71 to 80 of about 61,745 (283)

Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]

, 2010
To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
core   +2 more sources

G protein-coupled receptor kinases in normal and failing myocardium.

Frontiers in Bioscience, 2011
Heart failure (HF) is the end stage of many underlying cardiovascular diseases and is among the leading causes of morbidity and mortality in industrialized countries.
Z. Huang, Jessica I. Gold, W. Koch
semanticscholar   +1 more source

Endothelium‐Independent Relaxation of Alkaloid Boldine in Isolated Aortas From Normotensive and Hypertensive Rats: Participation of Ca2+ Channels

Chemistry &Biodiversity, EarlyView.
Involvement of Ca2+ channels in boldine‐induced vascular relaxation. ABSTRACT The regulation of vascular tone plays a fundamental role in blood pressure homeostasis and still represents a significant challenge in clinical practice. Boldine, a naturally occurring alkaloid from Peumus boldus, has emerged as a compound of interest due to its therapeutic ...
Martina Odebrecht Cavichiolo, Rita de Cássia Vilhena da Silva, Valdir Cechinel Filho, Priscila de Souza   +3 more
wiley   +1 more source

Tailoring therapy for heart failure: the pharmacogenomics of adrenergic receptor signaling. [PDF]

, 2014
Heart failure is one of the leading causes of mortality in Western countries, and β-blockers are a cornerstone of its treatment. However, the response to these drugs is variable among individuals, which might be explained, at least in part, by genetic ...
Barrese, V, Femminella, GD, Ferrara, N, Rengo, G   +3 more
core   +2 more sources

Essential role of β-adrenergic receptor kinase 1 in cardiac development and function [PDF]

Proceedings of the National Academy of Sciences, 1996
The β-adrenergic receptor kinase 1 (βARK1) is a member of the G protein-coupled receptor kinase (GRK) family that mediates the agonist-dependent phosphorylation and desensitization of G protein-coupled receptors. We have cloned and disrupted the βARK1 gene in mice by homologous recombination. No homozygote βARK1 −/−
Howard A. Rockman, Robert J. Lefkowitz, Mohamed Jaber, John Ross, Walter J. Koch, Bradley R. Smith, Marc G. Caron, Bruno Giros, Bruno Giros, Richard A. Bond, Kathleen K. Sulik   +10 more
openaire   +3 more sources

Repurposing Acebutolol for Osteoporosis Treatment: Insights From Multi‐Omics and Multi‐Modal Data Analysis

Clinical Pharmacology &Therapeutics, EarlyView.
Overview of a multi‐omics based drug repurposing strategy. The systematic drug repurposing strategy included the following steps: (1) osteoporosis driver signaling networks were identified from multi‐omics data; (2) drug functional modules were obtained using a network fusion approach to integrate drug similarity information; (3) all drugs were ranked ...
Dan‐Yang Liu, Hui Shen, Jonathan Greenbaum, Qiao‐Rong Yi, Shuang Liang, Yue Zhang, Jia‐Chen Liu, Chuan Qiu, Lan‐Juan Zhao, Qing Tian, Kuan‐Jui Su, Zhe Luo, Li Wu, Xiang‐He Meng, Hong‐Mei Xiao, Yun Deng, Yang Li, Dragana Lovre, Vivian Fonseca, Fernando L. Sanchez, Li‐Jun Tan, Hong‐Wen Deng   +21 more
wiley   +1 more source

Alterations in vasodilator-stimulated phosphoprotein (VASP) phosphorylation: associations with asthmatic phenotype, airway inflammation and β\u3csub\u3e2\u3c/sub\u3e-agonist use [PDF]

, 2006
Background Vasodilator-stimulated phosphoprotein (VASP) mediates focal adhesion, actin filament binding and polymerization in a variety of cells, thereby inhibiting cell movement.
Batra, Vikas, Cirelli, Rosemary, Foster, Gayle C., Hastie, Annette T., Hawkins, Gregory A., Peters, Stephen P., Rybinski, Katherine A., Wu, Min, Zangrilli, James G.   +8 more
core   +1 more source

GRK et arrestines : la piste thérapeutique ? [PDF]

, 2006
La phosphorylation d’un récepteur couplé aux protéines G (RCPG) par une kinase spécifique, nommée GRK (G protein-coupled receptor kinase), est une première étape qui participe, avec l’action des arrestines, à l’arrêt de la transmission du signal, au ...
Kraimps, Jean-Louis, Métayé, Thierry, Perdrisot, Rémy   +2 more
core   +1 more source

Redefining the Skin Barrier: A Microbiome‐Integrated Multilayered Defense Model

Barrier Immunity, EarlyView.
ABSTRACT The skin constitutes a dynamic interface orchestrating a sophisticated multilayered defense system comprising physical, chemical, immune, and microbial barriers. This review synthesizes current understanding of the structural and functional integration of these barriers, emphasizing their synergistic interactions in maintaining cutaneous ...
Jingjing Xia, Mathias Hochgerner, Qingzhen Wei, Xian'ge Zhong, Jiucun Wang   +4 more
wiley   +1 more source

Inflammation produces catecholamine resistance in obesity via activation of PDE3B by the protein kinases IKKε and TBK1. [PDF]

, 2013
Obesity produces a chronic inflammatory state involving the NFκB pathway, resulting in persistent elevation of the noncanonical IκB kinases IKKε and TBK1.
Chang, Louise, Chiang, Shian-Huey, Leto, Dara, Mowers, Jonathan, Reilly, Shannon M, Saltiel, Alan R, Simon, Joshua, Uhm, Maeran   +7 more
core   +3 more sources