Jill Ferguson
Scripps Research Institute
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Publication
Featured researches published by Jill Ferguson.
Journal of the American Chemical Society | 2012
Alexander Adibekian; Brent R. Martin; Jae Won Chang; Ku-Lung Hsu; Katsunori Tsuboi; Daniel A. Bachovchin; Anna E Speers; Steven J. Brown; Timothy P. Spicer; Virneliz Fernandez-Vega; Jill Ferguson; Peter Hodder; Hugh Rosen; Benjamin F. Cravatt
The development of small-molecule inhibitors for perturbing enzyme function requires assays to confirm that the inhibitors interact with their enzymatic targets in vivo. Determining target engagement in vivo can be particularly challenging for poorly characterized enzymes that lack known biomarkers (e.g., endogenous substrates and products) to report on their inhibition. Here, we describe a competitive activity-based protein profiling (ABPP) method for measuring the binding of reversible inhibitors to enzymes in animal models. Key to the success of this approach is the use of activity-based probes that show tempered rates of reactivity with enzymes, such that competition for target engagement with reversible inhibitors can be measured in vivo. We apply the competitive ABPP strategy to evaluate a newly described class of piperazine amide reversible inhibitors for the serine hydrolases LYPLA1 and LYPLA2, two enzymes for which selective, in vivo active inhibitors are lacking. Competitive ABPP identified individual piperazine amides that selectively inhibit LYPLA1 or LYPLA2 in mice. In summary, competitive ABPP adapted to operate with moderately reactive probes can assess the target engagement of reversible inhibitors in animal models to facilitate the discovery of small-molecule probes for characterizing enzyme function in vivo.
Archive | 2011
D Gianni; N Nicolas; H Zhang; C Der Mardirossian; J Kister; L Martinez; Jill Ferguson; William R. Roush; Steven J. Brown; Gm Bokoch; Peter Hodder; Hugh Rosen
Archive | 2014
Alexander Adibekian; Brent R. Martin; Jae Won Chang; Ku-Lung Hsu; Katsunori Tsuboi; Daniel A. Bachovchin; Anna E Speers; Steven J. Brown; Timothy P. Spicer; Virneliz Fernandez-Vega; Jill Ferguson; Benjamin F. Cravatt; Peter Hodder; Hugh Rosen
Archive | 2013
Alexander Adibekian; Brent R. Martin; Anna E Speers; Steven J. Brown; Timothy P. Spicer; Virneliz Fernandez-Vega; Jill Ferguson; Benjamin F. Cravatt; Peter Hodder; Hugh Rosen
Archive | 2010
Michael B. A. Oldstone; Peter Hodder; Melissa Crisp; Edward Roberts; Miguel Guerrero; Mariangela Urbano; Subash Velaparthi; Jian Zhao; Hugh Rosen; Marie-Therese Schaeffer; Steven J. Brown; Jill Ferguson
Archive | 2014
Thomas D. Bannister; Hui Wang; So Abdul-Hay; A Masson; Franck Madoux; Jill Ferguson; Becky A. Mercer; Stephan C. Schürer; Andrea M. Zuhl; Benjamin F. Cravatt; Ma Leissring; Peter Hodder
Archive | 2013
Christina J. Dreyton; Justin E. Jones; Bryan Knuckley; Venkatamaran Subramanian; Erin D. Anderson; Steven J. Brown; Virneliz Fernandez-Vega; Christina Eberhart; Timothy P. Spicer; Andrea M. Zuhl; Jill Ferguson; Anna E Speers; Chu Wang; Dale L. Boger; Paul R. Thompson; Benjamin F. Cravatt; Peter Hodder; Hugh Rosen
Archive | 2013
Kelin Li; Kevin J. Frankowski; Alicia M. Hanson; Jean Ndjomou; Matthew A. Shanahan; Sourav Mukherjee; Rajesh Kolli; William R. Shadrick; Noreena L. Sweeney; Craig A. Belon; Ben Neuenswander; Jill Ferguson; Jeffrey Aubé; Frank J. Schoenen; Brian S. J. Blagg; David N. Frick
Archive | 2014
Frank J. Schoenen; Warren S. Weiner; Pierre Baillargeon; Christopher L. Brown; Peter Chase; Jill Ferguson; Virneliz Fernandez-Vega; Partha Ghosh; Peter Hodder; Jeffrey P. Krise; Daljit S. Matharu; Benjamin Neuenswander; Patrick Porubsky; Steven A. Rogers; Tina S. Skinner-Adams; Melinda Sosa; Timothy P. Spicer; Joyce To; Nichole A. Tower; Katharine R. Trenholme; Jenna Wang; David A Whipple; Jeffrey Aubé; Hugh Rosen; E. Lucile White; John P. Dalton; Donald L. Gardiner
Archive | 2013
Ku-Lung Hsu; Katsunori Tsuboi; Anna E Speers; Steven J. Brown; Timothy P. Spicer; Virneliz Fernandez-Vega; Jill Ferguson; Benjamin F. Cravatt; Peter Hodder; Hugh Rosen