New possible target for treating major common diseases

There is a large, untapped potential for developing drugs against cancer, fibrosis and cardiovascular diseases by targeting a family of receptors known as Frizzleds, researchers at Karolinska Institutet in Sweden believe. ...

Cryo-EM reveals structure and mechanism of the 5-HT3 receptor

In November 2017, a Titan Krios cryo-electron microscope (cryo-EM) was inaugurated at the ESRF, the European Synchrotron, France. Data collected on this cryo-EM features in a Nature publication describing the activation cycle ...

A step ahead in pharmaceutical research

Hormones and other neurotransmitters, but also drugs, act upon receptors. "Their active substances bind to the receptors and modify the three-dimensional receptor arrangement regulating the downstream signal pathways," says ...

Scientists alter membrane proteins to make them easier to study

About 30 percent of the proteins encoded by the human genome are membrane proteins—proteins that span the cell membrane so they can facilitate communication between cells and their environment. These molecules are critical ...

Computer simulation of receptors reveals a new ligand-binding site

Using a computer simulation of an important receptor, EPFL scientists have discovered a novel binding site for natural ligands and drugs. The new site might be present on other receptors and can be exploited in novel treatments ...

Cryo-EM reveals interaction between major drug targets

For the first time, scientists have visualized the interaction between two critical components of the body's vast cellular communication network, a discovery that could lead to more effective medications with fewer side effects ...

Understanding a cell's 'doorbell'

A multi-institutional project to understand one of the major targets of human drug design has produced new insights into how structural communication works in a cell component called a G protein-coupled receptor (GPCRs), ...

Scientists solve structure of complement C5a receptor

Scientists at Heptares Therapeutics have published the first high-resolution X-ray crystal structure of the complement C5a receptor (a G protein-coupled receptor, GPCR) binding a small molecule allosteric antagonist.

Researchers map trends in drug development

From a drug perspective, G protein-coupled receptors are the most utilised cell receptors in the body. They are uniquely accessible at the cell surface, and a third of all drugs sold in the US target them.

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