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Progress towards a clinically-successful ATR inhibitor for cancer therapy
Abstract The DNA damage response (DDR) is now known to play an important role in both cancer development and its treatment. Targeting proteins such as ATR (Ataxia telangiectasia mutated and… Expand
Abstract 241: An efficient cell-based assay for quantification of cellular polysialic acid in neuroblastoma
Introduction Polysialic acid (polySia) decorates the surface of NCAM (neuronal cell adhesion molecule) on neuroendocrine tumors, notably neuroblastoma and small cell lung cancer, and is strongly… Expand
Probing cytochrome P450 (CYP) bioactivation with chloromethylindoline bioprecursors derived from the duocarmycin family of compounds.
- Natalia Ortúzar, K. Karu, +8 authors M. Searcey
- Bioorganic & medicinal chemistry
- 21 April 2021
The duocarmycins belong to a class of agent which has great potential for use in cancer therapy. Their exquisite potency means they are too toxic for systemic use, and targeted approaches are… Expand
Abstract 350: Investigating the mechanisms of cellular uptake and metabolism of ICT2588, an MT-MMP-activated prodrug
ICT2588 is a non-toxic MT1-MMP-activated peptide prodrug of the potent vascular disrupting agent (VDA) azademethylcolchicine . ICT2588 produces significant tumor-selective delivery (≥10-fold) of… Expand