The scientists: This project concerns “Antitubercular BirA inhibitors” and is being conducted by Curtis Engelhart, a scientist at the Center for Drug Design at the University of Minnesota. The research conducted by Curtis is focused on tuberculosis and seeks to exploit a recently-validated target for the discovery of a new antitubercular agent. Curtis holds a Bachelor of Science Degree in Chemistry from North Dakota State University and graduated in December 2012 with a Master’s of Science Degree in Medicinal Chemistry from the University of Minnesota.
The sponsor: This collaboration with the University of Minnesota is led by Principal Investigator Professor Courtney Aldrich. Founded in 1851, the University of Minnesota is ranked among the top public research universities in the United States. As a land-grant institution, the University of Minnesota is committed to engaging Minnesota, national and global communities to advance interdisciplinary knowledge; enhance students’ academic, civic, career, social and personal development; and apply intellectual and human capital to serve the public good.
Foundation funding: The Foundation is providing £109,801 in support.
GlaxoSmithKline’s contribution: GSK is providing in-kind contributions (including facilities and expertise from supporting scientists for HTS and access to the compounds library).
Project Description: BirA is an enzyme that links the bio-molecule biotin to Mycobacterium cellular proteins and controls Mycobacterium tuberculosis lipid metabolism. Before coming to the Open Lab to advance his research in the anti-TB compound library, Curtis optimised a cellular high throughput assay at the University of Minnesota.
The project’s overarching objective is to identify lead compounds which are active on this target (BirA). To help confirm activity on this target, scientists at the University of Minnesota have developed Mycobacterium tuberculosis mutants endowed with different expression levels of the BirA gene: deletion, under-expression and over-expression. During his time at the Open Lab, in addition to biochemical assays based on isolated BirA enzyme, Curtis is using these mutants to run cellular assays that will allow him to remove false positives.
“The open Lab offers us the technical expertise and equipment necessary to perform the research for this project. We would not be able to carry out this research project in our own academic research lab. The Open Lab provides the necessary equipment, resources, and expertise for the work – but it also provides an invaluable atmosphere of support, a center that works to find new treatments to combat diseases of the developing world.” (Curtis Engelhart, Open Lab scientist)