| Chapter title |
Discovery and Evaluation of PRL Trimer Disruptors for Novel Anticancer Agents
|
|---|---|
| Chapter number | 8 |
| Book title |
Protein Tyrosine Phosphatases
|
| Published in |
Methods in molecular biology, January 2016
|
| DOI | 10.1007/978-1-4939-3746-2_8 |
| Pubmed ID | |
| Book ISBNs |
978-1-4939-3744-8, 978-1-4939-3746-2
|
| Authors |
Yunpeng Bai, Zhi-Hong Yu, Zhong-Yin Zhang, Bai, Yunpeng, Yu, Zhi-Hong, Zhang, Zhong-Yin |
| Abstract |
Overexpression of PRL phosphatases (PRL1, PRL2, and PRL3) has been found in a variety of late-stage tumors and their distant metastatic sites. Therefore, the oncogenic PRL phosphatases represent intriguing targets for cancer therapy. There is considerable interest in identifying small molecule inhibitors targeting PRLs as novel anticancer agents. However, it has been difficult to acquire phosphatase activity-based PRL inhibitors due to the unusual wide and shallow catalytic pockets of PRLs revealed by crystal structure studies. Here, we present a novel method to identify PRL1 inhibitors by targeting the PRL1 trimer interface and the procedure to characterize their biochemical and cellular activity. |
X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 5 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 2 | 40% |
| Unspecified | 1 | 20% |
| Student > Bachelor | 1 | 20% |
| Student > Doctoral Student | 1 | 20% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 2 | 40% |
| Unspecified | 1 | 20% |
| Medicine and Dentistry | 1 | 20% |
| Engineering | 1 | 20% |