{"id":3856,"date":"2008-02-01T17:05:00","date_gmt":"2008-02-01T22:05:00","guid":{"rendered":"https:\/\/www.med.unc.edu\/biochem\/discovery-of-overdrive-protein-could-broaden-drug-design-options\/"},"modified":"2018-08-01T10:16:22","modified_gmt":"2018-08-01T14:16:22","slug":"discovery-of-overdrive-protein-could-broaden-drug-design-options","status":"publish","type":"post","link":"https:\/\/www.med.unc.edu\/biochem\/news\/discovery-of-overdrive-protein-could-broaden-drug-design-options\/","title":{"rendered":"Discovery of “Overdrive” Protein Could Broaden Drug Design Options"},"content":{"rendered":"
\n

New research from scientists at the University of North Carolina at Chapel Hill, by graduate student Michael Lee, Pharmacology, and Dr. Henrik Dohlman, Professor & Vice Chair of Biochemistry & Biophysics, shows for the first time that an important family of proteins known to function at the cell surface also functions at a site within the cell.<\/p>\n

The findings have potential implications for drug development as they involve G protein-coupled receptors (GPCRs). These molecules are the target of forty to fifty percent of modern medicinal drugs, such as antihistamines and drugs for high blood pressure.<\/p>\n

The study identified the first protein to activate the G-protein signaling pathway from within a cell. In humans, reactions to everything from taste and smell to stimulants like adrenaline or caffeine requires G-protein signaling.<\/p>\n

More than half of all drugs, from asthma and heart medicine to antidepressants, target G-protein receptors. Discovering a protein that activates G-proteins from inside a cell could open up an entirely new pathway for drug development, said Henrik Dohlman, Ph.D., senior study author and a professor of biochemistry and biophysics in UNC\u2019s School of Medicine.<\/p>\n

\u201cNo drug is 100 percent effective, 100 percent free of side effects and 100 percent safe. The more options we have biochemically, the more selective we can be in designing new drugs. If we can find another way of modulating G-proteins, we could expand the drug targets that are available to pharmacology,\u201d Dohlman said.<\/p>\n

The study appeared online Feb.7, 2008, in the journal Current Biology and will be published in the Feb. 14, 2008, print edition. Funding was provided by the National Institutes of Health and a UNC Cell and Molecular Biology Program predoctoral fellowship.<\/p>\n

Despite 20 years of study, G-protein signaling continues to produce surprises. The advent of the human genome project revealed that some three percent of our DNA is dedicated to these messenger molecules. However, the genomic data also drew biologists away from the research technique the UNC team used to discover the new protein, Dohlman said. \u201cPeople stopped looking for things that could activate G-proteins using functional criteria,\u201d he said. Instead, they searched for new receptors and activators based on common genetic patterns.<\/p>\n

Mike Lee, a graduate student in the UNC School of Medicine\u2019s department of pharmacology, identified the new protein, called Arr4, in yeast cells. Lee employed a mutant form of G-protein to search for any messengers inside the yeast cell with an affinity for G-proteins.<\/p>\n

\u201cWe went looking for things that could activate G-proteins but don\u2019t resemble known receptors,\u201d Lee said.<\/p>\n

He identified seven proteins that weren\u2019t receptors, but did bind to G-proteins, and did further tests on one of the seven proteins, Arr4, to determine its function.<\/p>\n

In yeast, Arr4 is involved in cell fusion, a process in which two yeasts fuse together to form one cell, combining their genetic data. A G-protein coupled receptor (GPCR) controls cell fusion, while Arr4 appears to play a supporting role.<\/p>\n

Lee said he thinks that Arr4 may allow the cell to go through several additional rounds of signal activation without needing to go back to the receptor.<\/p>\n

\u201cOur current thinking is it\u2019s not so much that this is the ignition for signaling, it\u2019s more like an overdrive. Once the pathway is activated by the hormone outside, Arr4 sustains the activity inside,\u201d Lee said. \u201cWhat we don\u2019t know is if Arr4 is itself stimulated by some signal, and of course we\u2019re very interested in finding out if that\u2019s the case.\u201d<\/p>\n

Note:<\/span> Dohlman can be reached at (919) 843-6894 or hdohlman@med.unc.edu<\/a>
School of Medicine contact:<\/span> Les Lang, (919) 843-9687 or llang@med.unc.edu<\/a>
News Services contact:<\/span> Patric Lane , (919) 962-8596 or patric_lane@unc.edu<\/a><\/p>\n<\/div>\n","protected":false},"excerpt":{"rendered":"

<\/p>\n

New research from scientists at the University of North Carolina at Chapel Hill, by graduate student Michael Lee, Pharmacology, and Dr. Henrik Dohlman, Professor & Vice Chair of Biochemistry & Biophysics, shows for the first time that an important family of proteins known to function at the cell surface also functions at a site within the cell.<\/p>\n","protected":false},"author":12066,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"layout":"","cellInformation":"","apiCallInformation":"","footnotes":"","_links_to":"","_links_to_target":""},"categories":[2],"tags":[11,4],"class_list":["post-3856","post","type-post","status-publish","format-standard","hentry","category-news","tag-news_2008","tag-recent-news","odd"],"acf":[],"yoast_head":"\nDiscovery of "Overdrive" Protein Could Broaden Drug Design Options | Biochemistry and Biophysics<\/title>\n<meta name=\"robots\" content=\"index, follow, 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