| Literature DB >> 26461041 |
Rajeshwar Narlawar, Eryn L Werry, Alana M Scarf, Raphy Hanani, Sook Wern Chua1, Victoria A King, Melissa L Barron, Ralph N Martins2, Lars M Ittner1, Louis M Rendina, Michael Kassiou.
Abstract
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.Entities:
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Year: 2015 PMID： 26461041 DOI： 10.1021/acs.jmedchem.5b01288
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446