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Structure-based design of potent aromatase inhibitors by high-throughput docking.

Abstract：

:Cytochrome P450 aromatase catalyzes the conversion of androgen substrates into estrogens. Aromatase inhibitors (AIs) have been used as first-line drugs in the treatment of estrogen-dependent breast cancer in postmenopausal women. However, the search for new, more potent, and selective AIs still remains necessary to avoid the risk of possible resistances and reduce toxicity and side effects of current available drugs. The publication of a high resolution X-ray structure of human aromatase has opened the way to structure-based virtual screening to identify new small-molecule inhibitors with structural motifs different from all known AIs. In this context, a high-throughput docking protocol was set up and led to the identification of nanomolar AIs with new core structures.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Caporuscio F,Rastelli G,Imbriano C,Del Rio A

doi

10.1021/jm2000689

subject

Has Abstract

pub_date

2011-06-23 00:00:00

pages

4006-17

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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