| Chapter title |
Protein–Protein Interaction Inhibitors of BRCA1 Discovered Using Small Molecule Microarrays
|
|---|---|
| Chapter number | 10 |
| Book title |
Small Molecule Microarrays
|
| Published in |
Methods in molecular biology, November 2016
|
| DOI | 10.1007/978-1-4939-6584-7_10 |
| Pubmed ID | |
| Book ISBNs |
978-1-4939-6582-3, 978-1-4939-6584-7
|
| Authors |
Zhenkun Na, Sijun Pan, Mahesh Uttamchandani, Shao Q. Yao |
| Editors |
Mahesh Uttamchandani, Shao Q. Yao |
| Abstract |
Microarray screening technology has transformed the life sciences arena over the last decade. The platform is widely used in the area of mapping interaction networks, to molecular fingerprinting and small molecular inhibitor discovery. The technique has significantly impacted both basic and applied research. The microarray platform can likewise enable high-throughput screening and discovery of protein-protein interaction (PPI) inhibitors. Herein we demonstrate the application of microarray-guided PPI inhibitor discovery, using human BRCA1 as an example. Mutations in BRCA1 have been implicated in ~50 % of hereditary breast cancers. By targeting the (BRCT)2 domain, we showed compound 15a and its prodrug 15b inhibited BRCA1 activities in tumor cells. Unlike previously reported peptide-based PPI inhibitors of BRCA1, the compounds identified could be directly administered to tumor cells, thus making them useful in targeting BRCA1/PARP-related pathways involved in DNA damage and repair response, for cancer therapy. |
X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 11 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 3 | 27% |
| Student > Bachelor | 2 | 18% |
| Researcher | 2 | 18% |
| Student > Doctoral Student | 1 | 9% |
| Unknown | 3 | 27% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 3 | 27% |
| Medicine and Dentistry | 2 | 18% |
| Chemistry | 2 | 18% |
| Biochemistry, Genetics and Molecular Biology | 1 | 9% |
| Unknown | 3 | 27% |