Biased receptor signaling in drug discovery

T Kenakin, EL Barker - Pharmacological reviews, 2019 - Elsevier
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Remote control of neuronal signaling

SC Rogan, BL Roth, AL Morrow - Pharmacological reviews, 2011 - Elsevier
A significant challenge for neuroscientists is to determine how both electrical and chemical
signals affect the activity of cells and circuits and how the nervous system subsequently …

Remote control of neuronal activity in transgenic mice expressing evolved G protein-coupled receptors

GM Alexander, SC Rogan, AI Abbas, BN Armbruster… - Neuron, 2009 - cell.com
Examining the behavioral consequences of selective CNS neuronal activation is a powerful
tool for elucidating mammalian brain function in health and disease. Newly developed …

[HTML][HTML] Engineering GPCR signaling pathways with RASSLs

BR Conklin, EC Hsiao, S Claeysen, A Dumuis… - Nature …, 2008 - nature.com
We are creating families of designer G protein–coupled receptors (GPCRs) to allow for
precise spatiotemporal control of GPCR signaling in vivo. These engineered GPCRs, called …

PPARγ2 nuclear receptor controls multiple regulatory pathways of osteoblast differentiation from marrow mesenchymal stem cells

KR Shockley, OP Lazarenko, PJ Czernik… - Journal of cellular …, 2009 - Wiley Online Library
Rosiglitazone (Rosi), a member of the thiazolidinedione class of drugs used to treat type 2
diabetes, activates the adipocyte‐specific transcription factor peroxisome proliferator …

[图书][B] A pharmacology primer: techniques for more effective and strategic drug discovery

TP Kenakin - 2018 - books.google.com
A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Fifth
Edition features the latest ideas and research regarding the application of pharmacology to …

DREADDs: novel tools for drug discovery and development

HM Lee, PM Giguere, BL Roth - Drug discovery today, 2014 - Elsevier
Highlights•DREADD is the acronym for Designer Receptors Exclusively Activated by
Designer Drugs.•Available DREADDs are activated by the inert ligand clozapine-N …

Wnt-signaling in skeletal development

S Teufel, C Hartmann - Current topics in developmental biology, 2019 - Elsevier
As the vertebrate skeleton develops it progresses from a solely cartilaginous scaffold to a
mineralized bony skeleton. The cells that build up the skeleton, the chondrocytes and …

Osteoblast expression of an engineered Gs-coupled receptor dramatically increases bone mass

EC Hsiao, BM Boudignon, WC Chang… - Proceedings of the …, 2008 - National Acad Sciences
Osteoblasts are essential for maintaining bone mass, avoiding osteoporosis, and repairing
injured bone. Activation of osteoblast G protein-coupled receptors (GPCRs), such as the …

CXCL12/CXCR4 signaling in the osteoblast regulates the mesenchymal stem cell and osteoclast lineage populations

M Shahnazari, V Chu, TJ Wronski… - The FASEB …, 2013 - Wiley Online Library
The chemokine CXCL12 and its receptor CXCR4 play a key role in regulation of
hematopoietic stem cells and cell migratory function during morphogenesis. Osteoblasts …