Ticlopidine in Its Prodrug Form Is a Selective Inhibitor of Human NTPDase1
المؤلفون المشاركون
Sévigny, Jean
Lecka, Joanna
Fausther, Michel
Künzli, Beat
المصدر
العدد
المجلد 2014، العدد 2014 (31 ديسمبر/كانون الأول 2014)، ص ص. 1-8، 8ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2014-08-11
دولة النشر
مصر
عدد الصفحات
8
التخصصات الرئيسية
الملخص EN
Nucleoside triphosphate diphosphohydrolase-1 (NTPDase1), like other ectonucleotidases, controls extracellular nucleotide levels and consequently their (patho)physiological responses such as in thrombosis, inflammation, and cancer.
Selective NTPDase1 inhibitors would therefore be very useful.
We previously observed that ticlopidine in its prodrug form, which does not affect P2 receptor activity, inhibited the recombinant form of human NTPDase1 ( K i = 14 μM).
Here we tested whether ticlopidine can be used as a selective inhibitor of NTPDase1.
We confirmed that ticlopidine inhibits NTPDase1 in different forms and in different assays.
The ADPase activity of intact HUVEC as well as of COS-7 cells transfected with human NTPDase1 was strongly inhibited by 100 µM ticlopidine, 99 and 86%, respectively.
Ticlopidine (100 µM) completely inhibited the ATPase activity of NTPDase1 in situ as shown by enzyme histochemistry with human liver and pancreas sections.
Ticlopidine also inhibited the activity of rat and mouse NTPDase1 and of potato apyrase.
At 100 µM ticlopidine did not affect the activity of human NTPDase2, NTPDase3, and NTPDase8, nor of NPP1 and NPP3.
Weak inhibition (10–20%) of NTPDase3 and -8 was observed at 1 mM ticlopidine.
These results show that ticlopidine is a specific inhibitor of NTPDase1 that can be used in enzymatic and histochemistry assays.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Lecka, Joanna& Fausther, Michel& Künzli, Beat& Sévigny, Jean. 2014. Ticlopidine in Its Prodrug Form Is a Selective Inhibitor of Human NTPDase1. Mediators of Inflammation،Vol. 2014, no. 2014, pp.1-8.
https://search.emarefa.net/detail/BIM-1043637
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Lecka, Joanna…[et al.]. Ticlopidine in Its Prodrug Form Is a Selective Inhibitor of Human NTPDase1. Mediators of Inflammation No. 2014 (2014), pp.1-8.
https://search.emarefa.net/detail/BIM-1043637
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Lecka, Joanna& Fausther, Michel& Künzli, Beat& Sévigny, Jean. Ticlopidine in Its Prodrug Form Is a Selective Inhibitor of Human NTPDase1. Mediators of Inflammation. 2014. Vol. 2014, no. 2014, pp.1-8.
https://search.emarefa.net/detail/BIM-1043637
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1043637
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
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