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  • Identification and characterization of novel inhibitors of Mammalian aspartyl aminopeptidase.

Identification and characterization of novel inhibitors of Mammalian aspartyl aminopeptidase.

Molecular pharmacology (2014-06-11)
Yuanyuan Chen, Hong Tang, William Seibel, Ruben Papoian, Ki Oh, Xiaoyu Li, Jianye Zhang, Marcin Golczak, Krzysztof Palczewski, Philip D Kiser
ABSTRACT

Aspartyl aminopeptidase (DNPEP) has been implicated in the control of angiotensin signaling and endosome trafficking, but its precise biologic roles remain incompletely defined. We performed a high-throughput screen of ∼25,000 small molecules to identify inhibitors of DNPEP for use as tools to study its biologic functions. Twenty-three confirmed hits inhibited DNPEP-catalyzed hydrolysis of angiotensin II with micromolar potency. A counter screen against glutamyl aminopeptidase (ENPEP), an enzyme with substrate specificity similar to that of DNPEP, identified eight DNPEP-selective inhibitors. Structure-activity relationships and modeling studies revealed structural features common to the identified inhibitors, including a metal-chelating group and a charged or polar moiety that could interact with portions of the enzyme active site. The compounds identified in this study should be valuable tools for elucidating DNPEP physiology.

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