Literature DB >> 26459896

The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity.

Venée N Tubman1, Pedro Mejia2, Boris E Shmukler3, Amy K Bei4, Seth L Alper5, James R Mitchell2, Carlo Brugnara6, Manoj T Duraisingh7.   

Abstract

Senicapoc, a Gardos channel inhibitor, prevented erythrocyte dehydration in clinical trials of patients with sickle cell disease. We tested the hypothesis that senicapoc-induced blockade of the Gardos channel inhibits Plasmodium growth. Senicapoc inhibited in vitro growth of human and primate plasmodia during the clinical blood stage. Senicapoc treatment suppressed P. yoelii parasitemia in vivo in C57BL/6 mice. The reassuring safety and biochemical profile of senicapoc encourage its use in antimalarial development.
Copyright © 2015, American Society for Microbiology. All Rights Reserved.

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Year:  2015        PMID： 26459896      PMCID： PMC4704178          DOI： 10.1128/AAC.01668-15

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  13 in total

1.  Cell volume control in the Plasmodium-infected erythrocyte.

Authors:  Richard J W Allen; Kiaran Kirk
Journal:  Trends Parasitol       Date:  2004-01

2.  Efficacy and safety of the Gardos channel blocker, senicapoc (ICA-17043), in patients with sickle cell anemia.

Authors:  Kenneth I Ataga; Wally R Smith; Laura M De Castro; Paul Swerdlow; Yogen Saunthararajah; Oswaldo Castro; Elliot Vichinsky; Abdullah Kutlar; Eugene P Orringer; Greg C Rigdon; Jonathan W Stocker
Journal:  Blood       Date:  2008-01-11       Impact factor: 22.113

3.  Potent antimalarial activity of clotrimazole in in vitro cultures of Plasmodium falciparum.

Authors:  T Tiffert; H Ginsburg; M Krugliak; B C Elford; V L Lew
Journal:  Proc Natl Acad Sci U S A       Date:  2000-01-04       Impact factor: 11.205

4.  Dose-escalation study of ICA-17043 in patients with sickle cell disease.

Authors:  Kenneth I Ataga; Eugene P Orringer; Lori Styles; Elliott P Vichinsky; Paul Swerdlow; George A Davis; Philip A Desimone; Jonathan W Stocker
Journal:  Pharmacotherapy       Date:  2006-11       Impact factor: 4.705

5.  ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice.

Authors:  Jonathan W Stocker; Lucia De Franceschi; Grant A McNaughton-Smith; Roberto Corrocher; Yves Beuzard; Carlo Brugnara
Journal:  Blood       Date:  2002-11-14       Impact factor: 22.113

Review 6.  Sickle cell disease: from membrane pathophysiology to novel therapies for prevention of erythrocyte dehydration.

Authors:  Carlo Brugnara
Journal:  J Pediatr Hematol Oncol       Date:  2003-12       Impact factor: 1.289

7.  Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies.

Authors:  Sandra Gemma; Giuseppe Campiani; Stefania Butini; Gagan Kukreja; Salvatore Sanna Coccone; Bhupendra P Joshi; Marco Persico; Vito Nacci; Isabella Fiorini; Ettore Novellino; Ernesto Fattorusso; Orazio Taglialatela-Scafati; Luisa Savini; Donatella Taramelli; Nicoletta Basilico; Silvia Parapini; Giulia Morace; Vanessa Yardley; Simon Croft; Massimiliano Coletta; Stefano Marini; Caterina Fattorusso
Journal:  J Med Chem       Date:  2008-02-16       Impact factor: 7.446

8.  Plasmodium falciparum: growth response to potassium channel blocking compounds.

Authors:  Karena L Waller; Kami Kim; Thomas V McDonald
Journal:  Exp Parasitol       Date:  2008-07-30       Impact factor: 2.011

9.  Novel inhibitors of the Gardos channel for the treatment of sickle cell disease.

Authors:  Grant A McNaughton-Smith; J Ford Burns; Jonathan W Stocker; Gregory C Rigdon; Christopher Creech; Susan Arrington; Tara Shelton; Lucia de Franceschi
Journal:  J Med Chem       Date:  2008-01-31       Impact factor: 7.446

Review 10.  The functional network of ion channels in T lymphocytes.

Authors:  Michael D Cahalan; K George Chandy
Journal:  Immunol Rev       Date:  2009-09       Impact factor: 12.988
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  2 in total

1.  Identification of Clotrimazole Derivatives as Specific Inhibitors of Arenavirus Fusion.

Authors:  Sylvia Rothenberger; Christian Widmann; Stefan Kunz; Giulia Torriani; Evgeniya Trofimenko; Jennifer Mayor; Chiara Fedeli; Hector Moreno; Sébastien Michel; Mathieu Heulot; Nadja Chevalier; Gert Zimmer; Neeta Shrestha; Philippe Plattet; Olivier Engler
Journal:  J Virol       Date:  2019-03-05       Impact factor: 5.103

Review 2.  Turf wars: exploring splenomegaly in sickle cell disease in malaria-endemic regions.

Authors:  Venée N Tubman; Julie Makani
Journal:  Br J Haematol       Date:  2017-05-11       Impact factor: 6.998
  2 in total

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