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  • Title: A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
    Author: Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM.
    Journal: Bioorg Med Chem Lett; 2012 Apr 15; 22(8):2811-7. PubMed ID: 22444683.
    Abstract:
    A new structural class of potent prolylcarboxypeptidase (PrCP) inhibitors was discovered by high-throughput screening. The series possesses a tractable SAR profile with sub-nanomolar in vitro IC(50) values. Compared to prior inhibitors, the new series demonstrated minimal activity shifts in pure plasma and complete ex vivo plasma target engagement in mouse plasma at the 20 h post-dose time point (po). In addition, the in vivo level of CNS and non-CNS drug exposure was measured.
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