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  • Title: Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs).
    Author: Pomplun S, Wang Y, Kirschner A, Kozany C, Bracher A, Hausch F.
    Journal: Angew Chem Int Ed Engl; 2015 Jan 02; 54(1):345-8. PubMed ID: 25412894.
    Abstract:
    To create highly efficient inhibitors for FK506-binding proteins, a new asymmetric synthesis for pro-(S)-C(5) -branched [4.3.1] aza-amide bicycles was developed. The key step of the synthesis is an HF-driven N-acyliminium cyclization. Functionalization of the C(5)  moiety resulted in novel protein contacts with the psychiatric risk factor FKBP51, which led to a more than 280-fold enhancement in affinity. The most potent ligands facilitated the differentiation of N2a neuroblastoma cells with low nanomolar potency.
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