First demonstration of positive allosteric-like modulation at the human wild type translocator protein (TSPO)

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*

*Corresponding author for this work

Research output: Contribution to journalArticle

8 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)8743-8749
Number of pages7
JournalJournal of Medicinal Chemistry
Volume58
Issue number21
DOIs
Publication statusPublished - 12 Nov 2015
Externally publishedYes

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