Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines.

ABSTRACT:

Aims

Modulation of DNA base excision repair (BER) has the potential to enhance response to chemotherapy and improve outcomes in tumours such as melanoma and glioma. APE1, a critical protein in BER that processes potentially cytotoxic abasic sites (AP sites), is a promising new target in cancer. In the current study, we aimed to develop small molecule inhibitors of APE1 for cancer therapy.

Methods

An industry-standard high throughput virtual screening strategy was adopted. The Sybyl8.0 (Tripos, St Louis, MO, USA) molecular modelling software suite was used to build inhibitor templates. Similarity searching strategies were then applied using ROCS 2.3 (Open Eye Scientific, Santa Fe, NM, USA) to extract pharmacophorically related subsets of compounds from a chemically diverse da

SUBMITTER: Mohammed MZ 

PROVIDER: S-EPMC3049581 | biostudies-literature | 2011 Feb

REPOSITORIES: biostudies-literature