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ID: ALA3632527

Journal: J Med Chem

Title: First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).

Authors: Narlawar R, Werry EL, Scarf AM, Hanani R, Chua SW, King VA, Barron ML, Martins RN, Ittner LM, Rendina LM, Kassiou M.

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.

CiteXplore: 26461041

DOI: 10.1021/acs.jmedchem.5b01288