Ontology highlight
ABSTRACT:
SUBMITTER: Cavalier MC
PROVIDER: S-EPMC4732916 | biostudies-literature | 2016 Jan
REPOSITORIES: biostudies-literature
Cavalier Michael C MC Ansari Mohd Imran MI Pierce Adam D AD Wilder Paul T PT McKnight Laura E LE Raman E Prabhu EP Neau David B DB Bezawada Padmavani P Alasady Milad J MJ Charpentier Thomas H TH Varney Kristen M KM Toth Eric A EA MacKerell Alexander D AD Coop Andrew A Weber David J DJ
Journal of medicinal chemistry 20160113 2
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) studies were therefore completed here with 23 pentamidine analogues, and X-ray structures of (Ca)S100B·inhibitor complexes revealed that the C-terminus of S100B adopts two different conformations, with loc ...[more]