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Optimization of Kinase Inhibitors for Activity on the Nuclear Receptor Nurr1

Undergraduate #3
Discipline: Biological Sciences
Subcategory: Biochemistry (not Cell and Molecular Biology and Genetics)
Session: 1

Michelle Asuquo - Shaw University
Co-Author(s): William Zeurcher (UNC Chapel Hill), Angela Allen (Shaw University), John Moore (North Carolina Central University)



NuNurr1 is a nuclear receptor that expressed predominantly in the central nervous system, which has been extensively validated as a target for Parkinson/s disease. A Nurr1 cellular reporter assay has been used to screen a set of approximately 370 kinase inhibitors from PKIS1 (published kinase inhibitor set provided by the SCG-UNC). Our research is a collaboration with the University of North Carolina Chapel Hill were we will focus on the chemical synthesis of various intermediate (prepared at UNC) with a variety of substituted anilines. After purification and characterization, the compound sill undergo biological evaluations as ligands for protein kinases. We will report the plans and initial data that will iterative the chemistry to optimize the cellular activities of the selected compounds.

Funder Acknowledgement(s): RIMI Grant (Shaw University)

Faculty Advisor: Dr. Angela Allen, aallen@shawu.edu

Role: The Part of the Research I did was synthesizing a varieties of substituted anilines.

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This material is based upon work supported by the National Science Foundation (NSF) under Grant No. DUE-1930047. Any opinions, findings, interpretations, conclusions or recommendations expressed in this material are those of its authors and do not represent the views of the AAAS Board of Directors, the Council of AAAS, AAAS’ membership or the National Science Foundation.

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