Researchers detail major molecular target for drugs

By Lynne Friedmann

Three international teams of scientists, led by researchers at UCSD, University of Michigan and Stanford University, have published a trio of papers describing the structure and workings of G protein-coupled receptors (GPCRs), a large family of human proteins that are the target of one-third to one-half of modern drugs.

GPCRs are involved in almost every human physiological function. Located within the membranes of cells, these receptors detect arriving hormones, chemical neurotransmitters, odors and other signaling molecules, then activate internal proteins, which, behaving like molecular switches, initiate other events that affect everything from the senses and behavior to fundamental functions like heart rate and blood pressure. Malfunctions in these signaling pathways have been linked to dozens of diseases, including diabetes, blindness, asthma, depression and some forms of cancer.

But historically GPCRs have been very difficult to work with and many drugs based on targeting GPCRs have been hit or miss because little has been known about how GPCRs work at the sub-molecular level. These three complementary papers go a long way toward addressing that shortfall.

Two of the papers are cover-story articles in the journal Nature. The third paper appears in the Proceedings of the National Academy of Sciences (PNAS). News release at bit.ly/saAtL3.

Scripps Research gets top ranking
The Scripps Research Institute (TSRI) tops a recent decade-long international ranking of institutions for “impact” (citations per scientific paper) in the field of chemistry. The ranking, published in Thomson Reuter’s ScienceWatch newsletter, tracks trends and performance in basic research during the period 2001 to 2011. The report, “Chemistry, at the Highest Level,” scored TSRI as first on the list of high impact institutions with nearly 42 citations per paper. This was followed in the ranking by Harvard University, Rice University, and Caltech. More information at bit.ly/p04F5S.

Genetics and alcoholism
A study by UCSD School of Medicine researchers suggests that differences in brain activation in individuals with a low level of response to alcohol may contribute to their inability to recognize modest levels of alcohol intoxication. A low level of response to alcohol is a genetically influenced characteristic that carries significant risk for the later development of alcoholism.

In the study researchers used functional magnetic resonance imaging (fMRI) to examine brain activation in young men and women, ages 18 to 25, with both low and high level of response to alcohol and found significant differences in brain activation between individuals while performing a cognitive task.

The findings could provide a marker to identify individuals at risk for developing an alcohol-use disorder before it develops. The findings appear online in the journal Alcoholism: Clinical & Experimental Research. News release bit.ly/nR69QN.

Lynne Friedmann is a science writer based in Solana Beach.

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