| Structural highlights
4mzk is a 2 chain structure with sequence from Plaf7. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| NonStd Res: | , |
Related: | 4aom, 4mzj, 4mzl |
Gene: | MTIP, PFL2225w (PLAF7) |
Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
By using a phage display derived peptide as an initial template, compounds have been developed that are highly specific against Mdm2/Mdm4. These compounds exhibit greater potency in p53 activation and protein-protein interaction assays than a compound derived from the p53 wild-type sequence. Unlike Nutlin, a small molecule inhibitor of Mdm2/Mdm4, the phage derived compounds can arrest cells resistant to p53 induced apoptosis over a wide concentration range without cellular toxicity, suggesting they are highly suitable for cyclotherapy.
Stapled peptides with improved potency and specificity that activate p53.,Brown CJ, Quah ST, Jong J, Goh AM, Chiam PC, Khoo KH, Choong ML, Lee MA, Yurlova L, Zolghadr K, Joseph TL, Verma CS, Lane DP ACS Chem Biol. 2013 Mar 15;8(3):506-12. doi: 10.1021/cb3005148. Epub 2012 Dec 18. PMID:23214419[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Brown CJ, Quah ST, Jong J, Goh AM, Chiam PC, Khoo KH, Choong ML, Lee MA, Yurlova L, Zolghadr K, Joseph TL, Verma CS, Lane DP. Stapled peptides with improved potency and specificity that activate p53. ACS Chem Biol. 2013 Mar 15;8(3):506-12. doi: 10.1021/cb3005148. Epub 2012 Dec 18. PMID:23214419 doi:http://dx.doi.org/10.1021/cb3005148
|