Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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In Vitro Screening of Some Heterocyclic Compounds Against Human ABHD6 and ABHD12 Hydrolases

Author(s): Monika Pitucha, Antti Poso, Agnieszka A. Kaczor.

Graphical Abstract:


Abstract:

The ABHD6 and ABHD12 are newly discovered post-genomic proteins which act as 2-arachidonoylglycerol hydrolases. Their physiological importance is largely unknown, however high expression of ABHD6 is attributed to some forms of cancer. Only a few inhibitors are known for ABHD6 and ABHD12 enzymes. In search for novel inhibitors of ABHD6 and ABHD12 hydrolases we tested a set of heterocyclic compounds which are lipophilic as required by the protein binding pockets and possess suitable properties for being tested in the designed assay. The rationale of the study may be summarized as follows: (1) almost all the compounds are relatively lipophilic; (2) some of the selected compounds exhibited anticancer activity; (3) some of the selected compounds shared the same structural features with known ABHD6 inhibitors and (4) physicochemical properties of the compounds make it possible to test them in the in vitro assay against ABHD6 and ABHD12 hydrolases. Although the studies did not make it possible to identify novel very potentABHD6 and ABHD12 inhibitors, we have identified 6 weak inhibitors of ABHD6 and ABHD12 (non-selective) and inhibiting both enzymes. The results obtained may be helpful for the design of novel active compounds.

Keywords: ABHD6 inhibitors, ABHD12 inhibitors, In vitro screening.

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Article Details

VOLUME: 11
ISSUE: 7
Year: 2014
Page: [944 - 952]
Pages: 9
DOI: 10.2174/1570180811666140313233940
Price: $58