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Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation.

Abstract：

:One hallmark of cancer cells is their adaptation to rely upon an altered metabolic scheme that includes changes in the glycolytic pathway, known as the Warburg effect, and elevated glutamine metabolism. Glutaminase, a mitochondrial enzyme, plays a key role in the metabolism of glutamine in cancer cells, and its inhibition could significantly impact malignant transformation. The small molecule 968, a dibenzophenanthridine, was recently shown to inhibit recombinantly expressed glutaminase C, to block the proliferation and anchorage-independent colony formation of human cancer cells in culture, and to inhibit tumor formation in mouse xenograft models. Here, we examine the structure-activity relationship that leads to 968-based inhibition of glutaminase and cancer cell proliferation, focusing upon a "hot-spot" ring previously identified as critical to 968 activity. We find that the hot-spot ring must be substituted with a large, nonplanar functionality (e.g., a t-butyl group) to bestow activity to the series, leading us to a model whereby the molecule binds glutaminase at a previously undescribed allosteric site. We conduct docking studies to locate potential 968-binding sites and proceed to test a specific set of docking solutions via site-directed mutagenesis. We verify the results from our initial assay of 968 and its analogues by cellular studies using MDA-MB-231 breast cancer cells.

journal_name

Mol Cancer Ther

journal_title

Molecular cancer therapeutics

authors

Katt WP,Ramachandran S,Erickson JW,Cerione RA

doi

10.1158/1535-7163.MCT-11-0942

subject

Has Abstract

pub_date

2012-06-01 00:00:00

pages

1269-78

issue

6

eissn

1535-7163

issn

1538-8514

pii

1535-7163.MCT-11-0942

journal_volume

11

pub_type

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