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

Abstract：

: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 location of Phe87 and Phe88 being the distinguishing feature and termed the "FF-gate". For symmetric pentamidine analogues ((Ca)S100B·5a, (Ca)S100B·6b) a channel between sites 1 and 2 on S100B was occluded by residue Phe88, but for an asymmetric pentamidine analogue ((Ca)S100B·17), this same channel was open. The (Ca)S100B·17 structure illustrates, for the first time, a pentamidine analog capable of binding the "open" form of the "FF-gate" and provides a means to block all three "hot spots" on (Ca)S100B, which will impact next generation (Ca)S100B·p53 inhibitor design.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Cavalier MC,Ansari MI,Pierce AD,Wilder PT,McKnight LE,Raman EP,Neau DB,Bezawada P,Alasady MJ,Charpentier TH,Varney KM,Toth EA,MacKerell AD Jr,Coop A,Weber DJ

doi

10.1021/acs.jmedchem.5b01369

subject

Has Abstract

pub_date

2016-01-28 00:00:00

pages

592-608

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

59

pub_type

杂志文章

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