First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO)
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- 作者：Rajeshwar Narlawar ; Eryn L. Werry ; Alana M. Scarf ; Raphy Hanani ; Sook Wern Chua ; Victoria A. King ; Melissa L. Barron ; Ralph N. Martins ; Lars M. Ittner ; Louis M. Rendina ; Michael Kassiou
- 刊名：Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：November 12, 2015
- 年：2015
- 卷：58
- 期：21
- 页码：8743-8749
- 全文大小：407K
- ISSN：1520-4804
文摘
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.