کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2151474 | 1089996 | 2013 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Targeting Cathepsin E in Pancreatic Cancer by a Small Molecule Allows In Vivo Detection
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
تحقیقات سرطان
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Targeting Cathepsin E in Pancreatic Cancer by a Small Molecule Allows In Vivo Detection Targeting Cathepsin E in Pancreatic Cancer by a Small Molecule Allows In Vivo Detection](/preview/png/2151474.png)
چکیده انگلیسی
When resectable, invasive pancreatic ductal adenocarcinoma (PDAC) is most commonly treated with surgery and radiochemotherapy. Given the intricate local anatomy and locoregional mode of dissemination, achieving clean surgical margins can be a significant challenge. On the basis of observations that cathepsin E (CTSE) is overexpressed in PDAC and that an United States Food and Drug Administration (FDA)-approved protease inhibitor has high affinity for CTSE, we have developed a CTSE optical imaging agent [ritonavir tetramethyl-BODIPY (RIT-TMB)] for potential intraoperative use.We show nanomolar affinity [half maximal inhibitory concentration (IC50) of 39.9 ± 1.2 nM] against CTSE of the RIT-TMB in biochemical assays and intracellular accumulation and target-to-background ratios that allow specific delineation of individual cancer cells. This approach should be useful for more refined surgical staging, planning, and resection with curative intent.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neoplasia - Volume 15, Issue 7, July 2013, Pages 684-693, IN1-IN3
Journal: Neoplasia - Volume 15, Issue 7, July 2013, Pages 684-693, IN1-IN3
نویسندگان
Edmund J. Keliher, Thomas Reiner, Sarah Earley, Jenna Klubnick, Carlos Tassa, Andrew J. Lee, Sridhar Ramaswamy, Nabeel Bardeesy, Douglas Hanahan, Ronald A. DePinho, Cesar M. Castro, Ralph Weissleder,