کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1214138 1494138 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Revealing multi-binding sites for taspine to VEGFR-2 by cell membrane chromatography zonal elution
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
Revealing multi-binding sites for taspine to VEGFR-2 by cell membrane chromatography zonal elution
چکیده انگلیسی

A new high-expression vascular endothelial growth factor receptor-2 (VEGFR-2) cell membrane chromatography (CMC) method was developed to investigate the affinity of ligands for VEGFR-2. An HEK293 VEGFR-2/CMC system was applied to specifically recognize ligands acting on VEGFR-2. Sorafenib was used as a mobile phase additive to evaluate the effect of the marker's concentration on the retention of sorafenib and taspine, respectively. The relationship among the retention, the types of binding sites and the affinity of taspine binding to VEGFR-2 has also been concerned. The retention behavior indicated that sorafenib had two major binding regions on VEGFR-2, and that taspine might act as a multi-target VEGFR-2 inhibitor with similar biological activity to sorafenib. The equilibrium dissociation constants (KD) obtained from the model are (5.25 ± 0.31) × 10−7 and (9.88 ± 0.54) × 10−5 mol L−1 for sorafenib at the high- and low-affinity sites, respectively, and the corresponding values for taspine are (3.88 ± 0.31) × 10−6 and (7.04 ± 0.49) × 10−5 mol L−1. The two types of binding sites contributed about a 1:2 ratio on the retention of taspine.


► The equilibrium dissociation constants of sorafenib and taspine binding to high- and low-affinity sites on VEGFR-2 were determined, respectively.
► Sorafenib had two major binding regions on VEGFR-2.
► Taspine might act as a multi-target VEGFR-2 inhibitor similar to sorafenib.
► Two types of binding sites contributed a 1:2 ratio on the retention of taspine.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Chromatography B - Volumes 887–888, 1 March 2012, Pages 67–72
نویسندگان
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