F
Francis S. Willard
Researcher at Eli Lilly and Company
Publications - 97
Citations - 5904
Francis S. Willard is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: Heterotrimeric G protein & G protein-coupled receptor. The author has an hindex of 39, co-authored 93 publications receiving 5249 citations. Previous affiliations of Francis S. Willard include University of North Carolina at Chapel Hill & Australian National University.
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Journal ArticleDOI
D2 dopamine receptor activation of potassium channels is selectively decoupled by Gαi-specific GoLoco motif peptides
Christina K. Webb,Christina K. Webb,Christopher R. McCudden,Francis S. Willard,Randall J. Kimple,David P. Siderovski,Gerry Stephen Oxford +6 more
TL;DR: GoLoco motif‐based peptides will be useful tools in examining the specificity of G‐protein‐coupled receptor–effector coupling, and have no effect on either basal channel activity or the initial responses to agonists, suggesting that the Go loco motif cannot disrupt pre‐formed G‐ protein heterotrimers.
Journal ArticleDOI
The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Gα-interaction face
Adam J. Kimple,Francis S. Willard,Patrick M. Giguère,Christopher A. Johnston,Viorel Mocanu,David P. Siderovski +5 more
TL;DR: The mechanism of action of the RGS protein inhibitor CCG-4986 is via covalent modification of Cys-132 of RGS4, likely causing steric hindrance with the all-helical domain of the Galpha substrate.
Journal ArticleDOI
Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Takahiro Kawai,Bingfa Sun,Hitoshi Yoshino,Dan Feng,Yoshiyuki Suzuki,Masanori Fukazawa,Shunsuke Nagao,David B. Wainscott,Aaron D. Showalter,Brian A. Droz,Tong Sun Kobilka,Matthew P. Coghlan,Francis S. Willard,Yoshiki Kawabe,Brian K. Kobilka,Kyle W. Sloop +15 more
TL;DR: Together, this work determined the molecular basis for the activity of an oral agent being developed for the treatment of type 2 diabetes mellitus, offering insights into the activation of class B GPCRs by nonpeptide ligands.
Book ChapterDOI
High-affinity immobilization of proteins using biotin- and GST-based coupling strategies.
Stephanie Q. Hutsell,Randall J. Kimple,David P. Siderovski,Francis S. Willard,Adam J. Kimple +4 more
TL;DR: This chapter focuses on high-affinity immobilization of protein substrates for affinity and kinetic analyses using biotin/streptavidin interaction and GST/anti-GST-antibody interaction.
Journal ArticleDOI
Open Innovation for Phenotypic Drug Discovery The PD2 Assay Panel
Jonathan A. Lee,Shaoyou Chu,Francis S. Willard,Karen Leigh Cox,Rachelle J. Sells Galvin,Robert B. Peery,Sarah E. Oliver,Jennifer Oler,Tamika D. Meredith,Steven A. Heidler,Wendy H. Gough,Saba Husain,Alan David Palkowitz,Christopher M. Moxham +13 more
TL;DR: Screening results for the first 4691 compounds submitted to PD2 have confirmed hit rates from 1.6% to 10%, with the majority of active compounds exhibiting acceptable potency and selectivity, indicating that chemical diversity from open source collaborations complements internal sources.