ORCID Profile
0000-0003-1702-8619
Current Organisation
University of California, San Diego
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Publisher: Springer Science and Business Media LLC
Date: 2011
DOI: 10.1038/NATURE09665
Publisher: Proceedings of the National Academy of Sciences
Date: 16-02-2018
Abstract: The orthosteric binding sites of the five muscarinic acetylcholine receptor (mAChR) subtypes are highly conserved, making the development of selective antagonists challenging. The allosteric sites of these receptors are more variable, allowing one to imagine allosteric modulators that confer subtype selectivity, which would reduce the major off-target effects of muscarinic antagonists. Accordingly, a large library docking c aign was prosecuted seeking unique positive allosteric modulators (PAMs) for antagonists, ultimately revealing a PAM that substantially potentiates antagonist binding leading to subtype selectivity at the M 2 mAChR. This study supports the feasibility of discovering PAMs that can convert an armamentarium of potent but nonselective G-protein–coupled receptor (GPCR) antagonist drugs into subtype-selective reagents.
Publisher: Springer Science and Business Media LLC
Date: 16-10-2018
Publisher: American Chemical Society (ACS)
Date: 13-11-2017
Publisher: Springer Science and Business Media LLC
Date: 30-11-2018
DOI: 10.1038/S41589-018-0182-5
Abstract: In the version of this paper originally published, the structure for epinephrine shown in Figure 1a was redrawn with an extra carbon. The structure has been replaced in the HTML and PDF versions of the article. The original and corrected versions of the structure are shown below.
Publisher: Oxford University Press (OUP)
Date: 30-04-2010
Publisher: American Society for Pharmacology & Experimental Therapeutics (ASPET)
Date: 05-11-2008
Publisher: American Chemical Society (ACS)
Date: 07-09-2018
Location: United States of America
No related grants have been discovered for Roger K. Sunahara.