Proton pump inhibitors drastically modify triosephosphate isomerase from Giardia lamblia at functional and structural levels, providing molecular leads in the design of new antigiardiasic drugs
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- 作者：Itzhel Garcí ; a-Torresa ; 1 ; itzheltorres@hotmail.com" class="auth_mail" title="E-mail the corresponding author ; Ignacio de la Mora-de la Moraa ; 1 ; ignaciodelamora@yahoo.com.mx" class="auth_mail" title="E-mail the corresponding author ; Jaime Marcial-Quinob ; jmarcialqu@conacyt.mx" class="auth_mail" title="E-mail the corresponding author ; Saú ; l Gó ; mez-Manzoa ; saulmanzo@ciencias.unam.mx" class="auth_mail" title="E-mail the corresponding author ; Amé ; rica Vanoye-Carloc ; america_vc@yahoo.com.mx" class="auth_mail" title="E-mail the corresponding author ; Gabriel Navarrete-Vá ; zquezd ; gabriel_navarrete@uaem.mx" class="auth_mail" title="E-mail the corresponding author ; Blanca Colí ; n-Lozanod ; clbi_ff@uaem.mx" class="auth_mail" title="E-mail the corresponding author ; Pedro Gutié ; rrez-Castrelló ; ne ; inpcochrane@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Edgar Sierra-Palaciosf ; edgar.sierra@uacm.edu.com" class="auth_mail" title="E-mail the corresponding author ; Gabriel Ló ; pez-Velá ; zqueza ; glv_1999@yahoo.com" class="auth_mail" title="E-mail the corresponding author ; Sergio Enrí ; quez-Floresa ; sergioenriquezflores@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Proton pump inhibitors ; Giardia lamblia ; Triosephosphate isomerase ; Structural perturbation ; Sulfenamide
- 刊名：Biochimica et Biophysica Acta (BBA) - General Subjects
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：1860
- 期：1
- 页码：97-107
- 全文大小：1115 K
文摘
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Proton pump inhibitors (PPIs) are extensively used in clinical practice because of their effectiveness and safety in humans.
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The glycolytic enzyme triosephosphate isomerase from Giardia lamblia (GlTIM) is a good target to generate antigiardiasic drugs.
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All the proton pump inhibitors efficiently inactivate and desestabilizate the GlTIM at functional and structural levels.
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Rabeprazole represents a promising lead in the search of new antigiardiasic drugs.
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The mechanisms of action of the PPIs on GlTIM can be helpful to understand their effectiveness and safety in human.