Small Molecule Inhibitors of Ca(2+)-S100B Reveal Two Protein Conformations

The drug pentamidine inhibits calcium-dependent complex formation with p53 ((Ca)S100B•p53) in malignant melanoma (MM), and restores p53 tumor suppressor activity in vivo. However, off-target effects associated with this drug were problematic in MM patients. Structure-activity relationship (SAR) stud...

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Pubblicato in:J Med Chem
Autori principali: Cavalier, Michael C., Ansari, Mohd. Imran, Pierce, Adam D., Wilder, Paul T., McKnight, Laura E., Raman, E. Prabhu, Neau, David B., Bezawada, Padmavani, Alasady, Milad J., Charpentier, Thomas H., Varney, Kristen M., Toth, Eric A., MacKerell, Alexander D., Coop, Andrew, Weber, David J.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4732916/
https://ncbi.nlm.nih.gov/pubmed/26727270
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b01369
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