Published October 23, 2015
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First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO)
Creators
- 1. School of Chemistry, Bosch Institute, The University of Sydney, Sydney, NSW 2006, Australia
- 2. Faculty of Health Sciences, Bosch Institute, The University of Sydney, Sydney, NSW 2006, Australia
- 3. School of Medical Sciences (Pharmacology), Bosch Institute, The University of Sydney, Sydney, NSW 2006, Australia
- 4. Dementia Research Unit, School of Medical Sciences, University of New South Wales, Sydney, NSW 2052, Australia
- 5. School of Medical Sciences, Edith Cowan University, Joondalup, WA 6027, Australia
- 6. School of Chemistry and Faculty of Health Sciences, Bosch Institute, The University of Sydney, Sydney, NSW 2006, Australia
Description
We show that changing the number and position of nitrogen atoms in the heteroatomic core of a pyrazolopyrimidine acetamide is sufficient to induce complex binding to wild type human TSPO. Only compounds with this complex binding profile lacked intrinsic effect on glioblastoma proliferation but positively modulated the antiproliferative effects of a synthetic TSPO ligand. To the best of our knowledge this is the first demonstration of allosteric-like interaction at the wild type human TSPO.
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