@article{9f3697245a5c48e1a5c50d3d47d349d7,
title = "Unraveling structural mechanisms of allosteric drug action",
abstract = "Orthosteric drugs block the active site to obstruct function; allosteric drugs modify the population of the active state, to modulate function. Available data lead us to propose that allosteric drugs can constitute anchors and drivers. The anchor docks into an allosteric pocket. The conformation with which it interacts is unchanged during the transition between the inactive and active states. The anchor provides the foundation that allows the driver to exert a 'pull' and/or 'push' action that shifts the receptor population from the inactive to the active state. The presence or absence of driver atom in an allosteric drug can exert opposite agonism. We map a strategy for driver identification and expect the allosteric trigger concept to transform agonist/antagonist drug discovery.",
keywords = "agonist, allosteric drug discovery, allostery, anchor atom, antagonist, driver atom, protocol",
author = "Ruth Nussinov and Tsai, {Chung Jung}",
note = "Funding Information: This project has been funded in whole or in part with federal funds from the National Cancer Institute, National Institutes of Health (NIH) under contract number HHSN261200800001E. The content of this publication does not necessarily reflect the views or policies of the Department of Health and Human Services nor does mention of trade names, commercial products, or organizations imply endorsement by the US Government. This research was supported in part by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research.",
year = "2014",
month = may,
doi = "10.1016/j.tips.2014.03.006",
language = "אנגלית",
volume = "35",
pages = "256--264",
journal = "Trends in Pharmacological Sciences",
issn = "0165-6147",
publisher = "Elsevier Ltd.",
number = "5",
}