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Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays
المؤلفون المشاركون
Ye, Fei
Zhang, Weiyao
Lu, Wenchao
Xie, Yiqian
Jiang, Hao
Jin, Jia
Luo, Cheng
المصدر
العدد
المجلد 2016، العدد 2016 (31 ديسمبر/كانون الأول 2016)، ص ص. 1-8، 8ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2016-10-27
دولة النشر
مصر
عدد الصفحات
8
التخصصات الرئيسية
الملخص EN
Overexpression of coactivator associated arginine methyltransferase 1 (CARM1), a protein arginine N-methyltransferase (PRMT) family enzyme, is associated with various diseases including cancers.
Consequently, the development of small-molecule inhibitors targeting PRMTs has significant value for both research and therapeutic purposes.
In this study, together with structure-based virtual screening with biochemical assays, two compounds DC_C11 and DC_C66 were identified as novel inhibitors of CARM1.
Cellular studies revealed that the two inhibitors are cell membrane permeable and effectively blocked proliferation of cancer cells including HELA, K562, and MCF7.
We further predicted the binding mode of these inhibitors through molecular docking analysis, which indicated that the inhibitors competitively occupied the binding site of the substrate and destroyed the protein-protein interactions between CARM1 and its substrates.
Overall, this study has shed light on the development of small-molecule CARM1 inhibitors with novel scaffolds.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Ye, Fei& Zhang, Weiyao& Lu, Wenchao& Xie, Yiqian& Jiang, Hao& Jin, Jia…[et al.]. 2016. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International،Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Ye, Fei…[et al.]. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International No. 2016 (2016), pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Ye, Fei& Zhang, Weiyao& Lu, Wenchao& Xie, Yiqian& Jiang, Hao& Jin, Jia…[et al.]. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International. 2016. Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1098686
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
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تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر
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