New Approaches to Difficult Drug Targets: The Phosphatase Story
| Autor: | Kelley E. McQueeney, Elizabeth R. Sharlow, John S. Lazo |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug Drug discovery media_common.quotation_subject Phosphatase Druggability Protein tyrosine phosphatase Computational biology Biology Biochemistry Analytical Chemistry 03 medical and health sciences 030104 developmental biology 0302 clinical medicine 030220 oncology & carcinogenesis Molecular targets Molecular Medicine Biotechnology media_common |
| Zdroj: | SLAS discovery : advancing life sciences RD. 22(9) |
| ISSN: | 2472-5560 |
| Popis: | The drug discovery landscape is littered with promising therapeutic targets that have been abandoned because of insufficient validation, historical screening failures, and inferior chemotypes. Molecular targets once labeled as "undruggable" or "intractable" are now being more carefully interrogated, and while they remain challenging, many target classes are appearing more approachable. Protein tyrosine phosphatases represent an excellent example of a category of molecular targets that have emerged as druggable, with several small molecules and antibodies recently becoming available for further development. In this review, we examine some of the diseases that are associated with protein tyrosine phosphatase dysfunction and use some prototype contemporary strategies to illustrate approaches that are being used to identify small molecules targeting this enzyme class. |
| Databáze: | OpenAIRE |
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