S
Shaun R. Stauffer
Researcher at Vanderbilt University
Publications - 132
Citations - 5313
Shaun R. Stauffer is an academic researcher from Vanderbilt University. The author has contributed to research in topics: Metabotropic glutamate receptor 5 & Allosteric regulation. The author has an hindex of 38, co-authored 125 publications receiving 4843 citations. Previous affiliations of Shaun R. Stauffer include University of Illinois at Chicago & Janssen Pharmaceutica.
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Journal ArticleDOI
Pyrazole Ligands: Structure−Affinity/Activity Relationships and Estrogen Receptor-α-Selective Agonists
Shaun R. Stauffer,Christopher J Coletta,Rosanna Tedesco,Gisele Nishiguchi,Kathryn E. Carlson,Jun Sun,Benita S. Katzenellenbogen,John A. Katzenellenbogen +7 more
TL;DR: Investigations suggest that the pyrazole triols prefer to bind to ERalpha with their C(3)-phenol in the estradiol A-ring binding pocket and that binding selectivity results from differences in the interaction of thePyrazole core and C(4)-propyl group with portions of the receptor where ERalpha has a smaller residue than ERbeta.
Journal ArticleDOI
High turnover number and rapid, room-temperature amination of chloroarenes using saturated carbene ligands.
TL;DR: A catalytic system for the mild amination of aryl chlorides is described, which consists of a Pd(0) precursor and a dihydroimidazoline carbene ligand generated in situ from its protonated tetrafluoroborate salt.
Journal ArticleDOI
Novel structural templates for estrogen-receptor ligands and prospects for combinatorial synthesis of estrogens
Brian E. Fink,Deborah S. Mortensen,Shaun R. Stauffer,Zachary D Aron,John A. Katzenellenbogen +4 more
TL;DR: An estrogen pharmacophore is developed that consists of a simple heterocyclic core scaffold, amenable to construction by combinatorial methods, onto which are appended 3-4 peripheral substituents that embody substructural motifs commonly found in nonsteroidal estrogens.
Journal ArticleDOI
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Alice L. Rodriguez,Mark D. Grier,Carrie K. Jones,Elizabeth J. Herman,Alexander S. Kane,Randy L. Smith,Richard Williams,Ya Zhou,Joy E. Marlo,Emily Days,Tasha N. Blatt,Satyawan Jadhav,Usha N. Menon,Paige N. Vinson,Jerri M. Rook,Shaun R. Stauffer,Colleen M. Niswender,Craig W. Lindsley,C. David Weaver,P. Jeffrey Conn +19 more
TL;DR: Discovery of structurally and functionally diverse allosteric modulators of mGluR5 that demonstrate in vivo efficacy in rodent models of anxiety and antipsychotic activity provide further support for the tremendous diversity of chemical scaffolds and modes of efficacy of mR5 ligands.
Journal ArticleDOI
Discovery, synthesis, and structure-based optimization of a series of N -(tert -Butyl)-2-(N -arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease
Jon Jacobs,Valerie Grum-Tokars,Ya Zhou,Mark Turlington,S. Adrian Saldanha,Peter Chase,Aimee Eggler,Eric S. Dawson,Yahira M. Báez-Santos,Sakshi Tomar,Anna M. Mielech,Susan C. Baker,Craig W. Lindsley,Peter Hodder,Andrew D. Mesecar,Shaun R. Stauffer +15 more
TL;DR: 16-(R) is a noncovalent SARS-CoV 3CL Pro inhibitor with moderate MW and good enzyme and antiviral inhibitory activity and provides an excellent starting point for the further design and refinement of 3CLpro inhibitors that act by a non covalent mechanism of action.