Characterization of the Raf Kinase Inhibitory Protein (RKIP) Binding Pocket: NMR-Based Screening Identifies Small-Molecule Ligands
Anne N. Shemon, Gary L. Heil, Alexey E. Granovsky et al. · 2010
Read Characterization of the Raf Kinase Inhibitory Protein (RKIP) Binding Pocket: NMR-Based Screening Identifies Small-Molecule Ligands by Anne N. Shemon, Gary L. Heil, Alexey E. Granovsky et al. (2010) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/plos-pone-0010479.txt.
Description
Anne Shemon and colleagues mapped the pocket where a cancer-related protein grips small molecules in PLOS ONE in 2010. The protein, RKIP, brakes a major growth signaling route in cells. It also helps suppress the spread of tumors. Finding small molecules that fit RKIP could restore its braking power. The team used NMR screening, a magnetic method, to fish for such molecules and locate the binding pocket.
Knowing the pocket's shape is the first step in drug design. Even weak initial binders can be improved once the site is known. RKIP loss is seen in several aggressive cancers. A drug that boosts its action would be a new kind of therapy. This study provides the structural foothold for that search.
Catalog record
| CREATOR | Anne N. Shemon, Gary L. Heil, Alexey E. Granovsky et al. |
|---|---|
| YEAR | 2010 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 48 KB |
| LICENSE | Creative Commons Attribution License |
| RIGHTS | CC BY |
| SOURCE | PLOS ONE |
Source: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0010479