Results 231 to 240 of about 83,092 (356)

GPCRs in rat primary skeletal muscle cells

, 2012
Mansour Emil Goerge Haddad
openalex   +1 more source

Gβγ subunit activation of KV7 and BKCa channels underlies calcitonin gene‐related peptide vasorelaxation in myogenic rat coronary resistance arteries

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose CGRP is a potent, clinically relevant coronary vasodilator known to play a role in cardioprotection. Here, we investigated the precise intracellular signalling pathways leading to vasodilation in small coronary arteries.
Lucy A. Donovan, JinHeng Lin, Milind Khashu, Christopher J. Garland, Kim A. Dora   +4 more
wiley   +1 more source

SENSIT, a Modular Single-Chain Fluorescent Integrator Platform for GPCR Ligands. [PDF]

ACS Chem Biol
Putansu A, Solowiej I, Rivett-Trznadel H, Lakkanasirorat B, Moran L, Kroning KE, Liu J, Li X, Li P, Wang W.   +9 more
europepmc   +1 more source

Fluorescence‐ and bioluminescence‐based approaches to study GPCR ligand binding [PDF]

, 2015
Leigh A. Stoddart, Carl W. White, Kim Nguyen, Stephen J. Hill, Kevin D. G. Pfleger   +4 more
openalex   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Rab8 and TNPO1 function as the ciliary transport adapters for GPCRs. [PDF]

J Biol Chem
Mahajan D, Madugula V, Chia HM, Lu L.
europepmc   +1 more source

Multivalent antibody‐based conjugates as new tools for tailored modulation of G protein–coupled receptors

British Journal of Pharmacology, EarlyView.
The G protein–coupled receptor (GPCR) superfamily consists of the most common targets of approved drugs. Targeting GPCRs offers appealing avenues for therapeutic development. Antibodies and their fragments, such as single‐domain antibodies (VHHs or nanobodies), have emerged as useful alternatives to small molecule pharmacophores as building blocks in ...
Shivani Sachdev, Ross W. Cheloha
wiley   +1 more source

An Explorative Approach to Examining the Role of Ischemia and Inflammation on the Function of Autoantibodies Against G Protein-Coupled Receptors and Their Corresponding Agonists. [PDF]

Int J Mol Sci
Wallukat G, Lakatos P, Steinhorst K, Flecks M, Hohberger B.   +4 more
europepmc   +1 more source

Optimisation of a new class of inflammation-resolving GPCR agonists for the treatment of Heart Failure with preserved Ejection Fraction (HFpEF) 

Therapeutic Innovation Australia
openalex   +1 more source

Functional screen for subtype specificity of voltage sensor–targeted Kv7 potentiators

British Journal of Pharmacology, EarlyView.
Background and Purpose Voltage‐gated Kv7 (potassium channel subfamily Q [KCNQ]) potassium channels are powerful modulators of neuronal excitability. ICA‐069673 is a N‐aryl benzamide drug that targets the voltage‐sensing domain (VSD) of Kv7.2 with strong selectivity over Kv7.3 or Kv7.5, but the molecular basis of this selectivity remains poorly ...
Richard Kanyo, Thomas M. Hammond, Alice W. Wang, Caroline K. Wang, Varun Aggarwal, Shawn M. Lamothe, Harley T. Kurata   +6 more
wiley   +1 more source