Cell-based biosensors and their application in biomedicine

Q Liu, C Wu, H Cai, N Hu, J Zhou, P Wang - Chemical reviews, 2014 - ACS Publications
A biosensor is an analytical device that can be used for detecting analytes and combines a
biological component with a physicochemical detecting transducer. In recent years …

Tools for GPCR drug discovery

R Zhang, X Xie - Acta Pharmacologica Sinica, 2012 - nature.com
G-protein-coupled receptors (GPCRs) mediate many important physiological functions and
are considered as one of the most successful therapeutic targets for a broad spectrum of …

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

T Kenakin, LJ Miller - Pharmacological reviews, 2010 - ASPET
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …

The significance of G protein-coupled receptor crystallography for drug discovery

JA Salon, DT Lodowski, K Palczewski - Pharmacological reviews, 2011 - ASPET
Crucial as molecular sensors for many vital physiological processes, seven-transmembrane
domain G protein-coupled receptors (GPCRs) comprise the largest family of proteins …

Cell-based assays: fuelling drug discovery

E Michelini, L Cevenini, L Mezzanotte, A Coppa… - Analytical and …, 2010 - Springer
It has been estimated that over a billion dollars in resources can be consumed to obtain
clinical approval, and only a few new chemical entities are approved by the US Food and …

Label-free whole-cell assays: expanding the scope of GPCR screening

CW Scott, MF Peters - Drug discovery today, 2010 - Elsevier
A new class of instruments offers an unprecedented combination of label-free detection with
exquisite sensitivity to live-cell responses. These instruments can quantify G-protein-coupled …

The application of cell‐based label‐free technology in drug discovery

B Xi, N Yu, X Wang, X Xu… - Biotechnology Journal …, 2008 - Wiley Online Library
Cell‐based assays are an important part of the drug discovery process allowing for
interrogation of targets and pathways in a more physiological setting compared to …

Decoding signaling and function of the orphan G protein–coupled receptor GPR17 with a small-molecule agonist

S Hennen, H Wang, L Peters, N Merten, K Simon… - Science …, 2013 - science.org
Replacement of the lost myelin sheath is a therapeutic goal for treating demyelinating
diseases of the central nervous system (CNS), such as multiple sclerosis (MS). The G …

Cellular assays as portals to seven-transmembrane receptor-based drug discovery

TP Kenakin - Nature reviews Drug discovery, 2009 - nature.com
As technology advances to the point at which various behaviours of seven-transmembrane
(7TM) receptors (also known as G protein-coupled receptors (GPCRs)) can be observed …

Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins

EM Rosethorne, SJ Charlton - Molecular pharmacology, 2011 - ASPET
The Gi/o-coupled histamine H4 receptor is highly expressed in hemopoietic cells and is a
promising new target for the treatment of chronic inflammatory diseases. 1-[(5-Chloro-1 H …