A superior drug carrier--aponeocarzinostatin in partially unfolded state fully protects the labile antitumor enediyne.

ABSTRACT:

Background

Neocarzinostatin is a potent antitumor drug consisting of an enediyne chromophore and a protein carrier.

Methods

We characterized an intermediate in the equilibrium unfolding pathway of aponeocarzinostatin, using a variety of biophysical techniques including 1-anilino-8-napthalene sulfonate binding studies, size-exclusion fast protein liquid chromatography, intrinsic tryptophan fluorescence, circular dichroism, and 1H-15N heteronuclear single quantum coherence spectroscopy.

Results

The partially unfolded protein is in molten globule-like state, in which approximately 60% and approximately 20% tertiary and secondary structure is disrupted respectively. Despite lacking a fully coordinated tertiary structure for assembling a functional binding cleft, the prote

SUBMITTER: Shanmuganathan A 

PROVIDER: S-EPMC2694159 | biostudies-literature | 2009 May

REPOSITORIES: biostudies-literature