English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Zendy Plus

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Zendy Tools

Zendy Open

Herein we report the first example of an  iso DGR–drug conjugate ( 2 ), designed to release paclitaxel selectively within cancer cells expressing integrin α V β 3 . Conjugate  2  was synthesized by connecting the  iso DGR peptidomimetic  5  with paclitaxel via the lysosomally cleavable Val–Ala dipeptide linker. Conjugate  2  displayed a low nanomolar affinity for the purified integrin α V β 3  receptor (IC 50 =11.0 n m ). The tumor targeting ability of conjugate  2  was assessed in vitro in anti‐proliferative assays on two isogenic cancer cell lines characterized by different integrin α V β 3  expression: human glioblastoma U87 (α V β 3 +) and U87 β 3 ‐KO (α V β 3 −). The  iso DGR‐PTX conjugate  2  displayed a remarkable targeting index (TI=9.9), especially when compared to the strictly related RGD‐PTX conjugate  4  (TI=2.4).

Tumor Targeting with an iso DGR–Drug Conjugate