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Cover Picture: Design, Synthesis and Bioevaluation of an EphA2 Receptor‐Based Targeted Delivery System (ChemMedChem 7/2014)
Author(s) -
Barile Elisa,
Wang Si,
Das Swadesh K.,
Noberini Roberta,
Dahl Russell,
Stebbins John L.,
Pasquale Elena B.,
Fisher Paul B.,
Pellecchia Maurizio
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490024
Subject(s) - conjugate , eph receptor a2 , endocytosis , internalization , chemistry , drug delivery , targeted drug delivery , receptor , receptor mediated endocytosis , drug , cancer research , biophysics , pharmacology , biochemistry , biology , receptor tyrosine kinase , mathematical analysis , mathematics , organic chemistry
The front cover picture shows that targeted delivery of Taxol (surface and stick representation) can be accomplished by conjugating the drug with a specific agent (green rod shape) targeting the membrane‐anchored EphA2 receptor (orange). Binding of the drug conjugate causes receptor phosphorylation (indicated by a P) and internalization via endocytosis. The EphA2‐bound drug conjugate is therefore actively internalized in the lysosomes where it gets cleaved delivering free Taxol. The EphA2 receptor is overexpressed in cancer cells and during angiogenesis. Therefore, drug conjugates targeting this receptor can selectively deliver chemotherapeutic agents to tumors and their vasculature. For more details, see the Full Paper by Maurizio Pellecchia et al. on p. 1403 ff.