On March 31, 2010, Pillai, R.; Marinelli, E. R.; Fan, H.; Nanjappan, P.; Song, B.; von Wronski, M. A.; Cherkaoui, S.; Tardy, I.; Pochon, S.; Schneider, M.; Nunn, A. D.; Swenson, R. E. published an article.Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was A Phospholipid-PEG2000 Conjugate of a Vascular Endothelial Growth Factor Receptor 2 (VEGFR2)-Targeting Heterodimer Peptide for Contrast-Enhanced Ultrasound Imaging of Angiogenesis. And the article contained the following:
The transition of a targeted ultrasound contrast agent from animal imaging to testing in clin. studies requires considerable chem. development. The nature of the construct changes from an agent that is chem. attached to microbubbles to one where the targeting group is coupled to a phospholipid, for direct incorporation to the bubble surface. We provide an efficient method to attach a heterodimeric peptide to a pegylated phospholipid and show that the resulting construct retains nanomolar affinity for its target, vascular endothelial growth factor receptor 2 (VEGFR2), for both the human (kinase insert domain-containing receptor – KDR) and the mouse (fetal liver kinase 1 – Flk-1) receptors. The purified phospholipid-PEG-peptide isolated from TFA-based eluents is not stable with respect to hydrolysis of the fatty ester moieties. This leads to the time-dependent formation of the lysophospholipid and the phosphoglycerylamide derived from the degradation of the product. Purification of the product using neutral eluent systems provides a stable product. Methods to prepare the lysophospholipid (hydrolysis product) are also included. Biacore binding data demonstrated the retention of binding of the lipopeptide to the KDR receptor. The phospholipid-PEG2000-peptide is smoothly incorporated into gas-filled microbubbles and provides imaging of angiogenesis in a rat tumor model. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate
The Article related to preparation phospholipid polyethylene glycol conjugate contrast ultrasound imaging angiogenesis, Pharmaceuticals: Pharmaceutics and other aspects.Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate
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