Receptor Activation

Activated and endocytosed Endothelin A receptors un U2OS cells carrying a fluorescent protein tag
Activated and endocytosed Endothelin A receptors un U2OS cells carrying a fluorescent protein tag

There are many image based approaches for studying receptor activation. Binding of fluorescently labeled ligands to the receptors on the plasma membrane, eventually followed by internalization of the ligand-receptor complex is one of them.

A more relevant method of studying receptor activation is to monitor the processes which follow activation of a receptor, such as internalization and endocytosis of activated receptors carrying a fluorescent tag.  This produces a more accurate readout with less false positives.

Another approach is based on signal molecule recruitment to activated receptor complexes. G protein coupled receptor (GPCR) activation, for example, can be studied by the binding of arrestin carrying a fluorescent protein tag followed by the formation of fluorescent clathrin-coated pits at the cell surface or fluorescent clathrin-coated vesicles in the cytoplasm.

One of the earliest structural changes observed in cells in response to many extracellular factors is membrane ruffling: the formation of motile cell surface protrusions containing a meshwork of newly polymerized actin filaments.

It is becoming clear that actin reorganization is an integral part of early signal transduction pathways, and that many signaling molecules interact with the actin cytoskeleton.

Our Receptor Activation solutions

Drawing on many years of experience and in-depth knowledge, PerkinElmer offers solutions for every throughput, a starting point for typical receptor activation assays and unlimited possibilities for customization:

Opera High Content Screening System
  • High sample throughput with multi-color parallel image acquisition and over 100,000 data points per day
Operetta Compact High Content Screening System
  • High speed with large field of view and large cell number captured with every image
  • Ready-made image analysis sequences for receptor internalization, building blocks for signal molecule recruitment and documentation on how to customize
  • Unlimited possibilities for adding parameters and modifying readout
Acapella Image Analysis Software
  • Unlimited possibilities for adding parameters and modifying readout
  • Image analysis sequences for receptor internalization and translocation assays
Columbus High Volume Data Management and Analysis System
  • Enterprise level data management from assay development to high throughput screening seamlessly linking high content data, research data, in vivo imaging data, result management, screening statistics, biological and chemical data
cell::explorer Automated High Content Screening System
  • Full environmental control and workstation with hand-over of plates from imager to incubator for short-term and long-term live cell assays

You may also be interested in: Live Cell Imaging.