Rodriguez-menchaca and chloroquine


McPate a 1 Yi hong Zhang a Henggui Zhang b Jules C. Here, we employed patch-clamp methods, mutagenesis analysis, and molecular modeling to characterize the molecular pharmacology of Kir4.1 inhibition by CQ Tricyclic antidepressants such as for example nortriptyline stop Kir4.1 stations with IC50 beliefs within the 20 to 100 ?M range (Furutani et al. Eur J Pharmacol. Administration of chloroquine alone, an IK1 channel antagonist, had no effect on all the parameters measured, but significantly blocked the beneficial effects rodriguez-menchaca and chloroquine of ZAC on cardiac repair. 1364-8, 2008 U. Rupp Chloroquine inhibits tumor-related Kv10.1 channel and decreases migration of MDA-MB-231 breast cancer cells in vitro. Motivated by reports that chloroquine inhibition of cardiac IKATP is anti-fibrillatory in rabbit ventricle, we investigated the mechanism of chloroquine inihibition of cardiac KATP channels …. In conclusion, opening of the IK1 channel with ZAC inhibits maladaptive tissue repair and improves cardiac function, potentially rodriguez-menchaca and chloroquine mediated by the inhibition of. , 2009 ) The molecular basis of chloroquine block of the inward rectifier Kir2. Rodriguez-Menchaca - Google Scholar Citations scholar.google.com/citations?user=nE-YHpIAAAAJ&hl=en The molecular basis of chloroquine block of the inward rectifier Kir2. Director of R&D, IonChannels Millipore Corporation Cambridge, UK. Site-directed mutagenesis revealed the location of the chloroquine-binding site. The truth about this effective and safe medication is far more sinister It is inhibited by chloroethylclonidine and pentamidine which bind in the channel (Rodríguez-Menchaca et al. Mutagenesis and molecular modeling showed that chloroquine did not penetrate deeply into the channel and was stabilized within the binding pocket by negatively charged and aromatic amino acids Although chloroquine remains an important therapeutic agent for treatment of malaria in many parts of the world, its safety margin is very narrow. S Images of Rodriguez Menchaca And chloroquine bing.com/images See all See more images of Rodriguez Menchaca And chloroquine Molecular mechanisms of chloroquine inhibition of https://www.ncbi.nlm.nih.gov/pubmed/22851715 Molecular mechanisms of chloroquine inhibition of heterologously expressed Kir6.2/SUR2A channels. Rodríguez-Menchaca et rodriguez-menchaca and chloroquine al. 35 x 35 Rodríguez-Menchaca, A.A., Navarro-Polanco, R.A., Ferrer-Villada, T. Rodríguez-Menchaca, Angélica López-Izquierdo, Tania Ferrer, Harley T Chloroquine inhibits tumor-related Kv10.1 channel and https://www.ncbi.nlm.nih.gov/pubmed/31082369 Jul 15, 2019 · Electronic address: aldo.rodriguez@uaslp.mx. Nichols, and Jose´A.Sa´nchez-Chapula 803. Research in my laboratory focuses on the following topics: 1. One of the options under investigation is the old antimalarial drug, chloroquine, and its analog, hydroxychloroquine. Slough, Thanh Tran, Nhi Tran, Michelle Aldo A. et al. Rodríguez-Menchaca AA, Cui M, Sánchez-Chapula JA, Ferrer T. Renewed interest in chloroquine has emerged after recent reports of its effectiveness in reducing viral loads of HIV-1 (1, 2) We hypothesize that the antimalarial quinoline chloroquine exerts potent antiarrhythmic effects by interacting with the cytoplasmic domains of Kir2.1 (I K1), Kir3.1 (I KACh), or Kir6.2 (I KATP) and reducing inward rectifier potassium currents. 2009), or by cations such as barium and cesium (Hibino et al. For this, we developed a 2D model of atrial tissue under pAF conditions rodriguez-menchaca and chloroquine Available online at www.sciencedirect.com ScienceDirect Cardiac and renal inward rectifier potassium channel pharmacology: emerging tools for integrative physiology and therapeutics Daniel R Swale1, Sujay V Kharade1 and Jerod rodriguez-menchaca and chloroquine S Denton1,2,3,4 Inward rectifier potassium (Kir) channels play fundamental roles in cardiac and renal function and may represent unexploited …. Eur J Pharmacol. We observed voltage-dependent pentamidine block, that is the outward component of I K1 was more strongly affected than the inward component, and altered kinetics with respect to maximum current rise time …. 105(4) , pp. 105(4) , pp. Cited by: 1 Publish Year: 2019 Author: Belkis Valdés-Abadía, Rita Morán-Zendejas, José M. There is a nearly 92 percent chance that the much-hyped anti-malaria drugs chloroquine (CQ) and hydroxychloroquine (HCQ) can help patients afflicted by the novel coronavirus, doctors told the governor of Arizona in a letter this week.. Palacio, Bojjibabu Chidipi, Diana P. The molecular basis of chloroquine block of the inward rectifier KIR2.1 channel Article (PDF Available) in Proceedings of the National Academy of Sciences 105(4):1364-8 · …. Chloroquine blocks the Kir4.1 channels by an open-pore blocking mechanism. NEWARK – Addressing concerns of potential drug shortages caused by the inappropriate prescribing and hoarding of drugs touted by some as possible treatments for COVID-19, Attorney General Gurbir S. This broad range of …. 2016; Aréchiga-Figueroa et al. 8 have shown that amino acids E224, D259, E299, F254, and D255 of the Kir2.1 intracellular domain are critical for chloroquine blockade Chloroquine and related compounds can inhibit inwardly-rectifying potassium channels by multiple potential mechanisms, including pore block and allosteric effects on channel gating. Several amino acid residues within the central pore of Kir2.1 channels have been identified as critical binding sites for these compounds (Rodriguez-Menchaca et al., 2008) Chloroquine (CQ) is an amino quinolone derivative known to inhibit Kir2.1 and Kir6.2 channels with different action mechanism and binding site. Chloroquine inhibits tumor-related Kv10.1 channel and decreases migration of MDA-MB-231 breast cancer cells in vitro. Rodriguez-Menchaca et al. A Rodriguez-Menchaca, T Ferrer-Villada, J Lara, D Fernandez,. Chloroquine was found to inhibit the K IR 2.1 based I K1 channel in a voltage dependent mode by plugging the cytoplasmic pore region (Rodríguez-Menchaca et al., 2008). Molecular Mechanisms of Chloroquine Inhibition of Heterologously Expressed Kir6.2/SUR2A Channels Daniela Ponce-Balbuena, Aldo A. The unique short QT syndrome type-3 phenotype is associated with an extremely abbreviated QT interval (200 ms) on ECG and paroxysmal atrial fibrillation. A fast-onset effect is observed at depolarized membrane voltages and enhanced by the N160D mutation in the central cavity, probably reflecting direct channel block resulting from the drug entering the. The I K1 pore blockers chloroquine (Rodríguez‐Menchaca et al., 2008) and pentamidine may, in principle, serve as an alternative for Ba 2+ in experimental use. 1364-8, 2008 U. 1 channel AA Rodríguez-Menchaca, RA Navarro-Polanco, T Ferrer-Villada, J Rupp, Proceedings of the National Academy of Sciences 105 (4), 1364-1368 , 2008. As chloroquine has been shown to inhibits several potassium channels, we decided to study its effect on the tumor-related Kv10.1 channel by using patch-clamp electrophysiology and cell migration assays Chloroquine and related compounds can inhibit inwardly-rectifying potassium channels by multiple potential mechanisms, including pore block and allosteric effects on channel gating. Developed as synthetic succedanea of cinchona alkaloids, these chiral antimalarials are currently in use as the racemate Although chloroquine remains an important therapeutic agent for treatment of malaria in many parts of the world, its safety margin is very narrow. Vossius , and R. Here, we employed patch-clamp methods, mutagenesis analysis, and molecular modeling to characterize the molecular pharmacology of Kir4.1 inhibition by CQ. Cited by: 1 Publish Year: 2019 Author: Catalina Tobón, Laura C. Blocking mechanisms of several cationic amphiphilic drugs such as chloroquine have been deciphered by means of molecular modeling and Ala-scanning mutagenesis. The cytoplasmic pore of Kir2.1 reportedly binds the antimalarial agent chloroquine, leading to current inhibition (Rodríguez-Menchaca et al., 2008). Rangel-Flores, Aldo A. Rodríguez-Menchaca, Ricardo A. 1 channel AA Rodríguez-Menchaca, RA Navarro-Polanco, T Ferrer-Villada, J Rupp, Proceedings of the National Academy of Sciences 105 (4), 1364-1368 , 2008. Navarro-Polanco , Tania Ferrer-Villada , Jason Rupp , Frank B. Sachse, Martin Tristani-Firouzi and José A. 1 channel. Localization and function of transient …. Action potential clamp and chloroquine sensitivity of mutant Kir2.1 channels responsible for variant 3 short QT syndrome Author links open overlay panel Aziza El Harchi a Mark J. Rodríguez-Menchaca AA et al. Chloroquine inhibits the cardiac inward rectifier K + current I K1 and can induce lethal ventricular arrhythmias Chloroquine can be used to treat porphyria cutanea tarda, but in a very low dose (125 mg twice weekly) as a dosage of 250 mg/day can trigger a porphyria crisis, which can be fatal. Chloroquine rodriguez-menchaca and chloroquine overdose remains the most severe and frequent cause of antimalarial drug poisonings. 2153-Pos, 2008. We found rodriguez-menchaca and chloroquine that chloroquine inhibits the Kir6.2/SUR2A channel by interacting with at least two different sites and by two mechanisms of action. 105(4) , pp. Chloroquine availability. 2017, 800, 40-47 The desperate need to find drugs for COVID-19 has indicated repurposing strategies as our quickest way to obtain efficacious medicines. Chloroquine (CQ) is an amino quinolone derivative known to inhibit Kir2.1 and Kir6.2 channels with different action mechanism and binding site Chloroquine phosphate, an old drug for treatment of malaria, is shown to have apparent efficacy and acceptable safety against COVID-19 associated pneumonia in multicenter clinical trials …. 2019 May 10;855:262-266.. Proc Natl Acad Sci USA 105:1364–1368 PubMed CrossRef Google Scholar. Its prognosis and high mortality should be improved by adequate supportive treatment and by the. Cdc Chloroquine Prophylaxis Transmission of malaria to humans occurs through the bite of infected female Anopheles mosquitoes From CDC website: Hydroxychloroquine and chloroquine are oral prescription drugs that have rodriguez-menchaca and chloroquine been used for treatment of malaria and certain inflammatory conditions Recently, the widely used antimalarial drug chloroquine and the oestrogen receptor antagonist tamoxifen were demon-strated to inhibit K IR2.1-based I K1 by blocking the ion channel pore from the cytoplasmic side or by interfering in the K IR2.1– PIP 2 interaction, respectively (Rodríguez-Menchaca et al., 2008; Ponce-Balbuena et al., 2009) Mar 12, 2013 · We describe a mutation (E299V) in KCNJ2 , the gene that encodes the strong inward rectifier K+ channel protein (Kir2.1), in an 11-y-old boy. 2008), tamoxifen (Ponce-Balbuena et rodriguez-menchaca and chloroquine al. Here, we employed patch-clamp methods, mutagenesis analysis, and molecular modeling to characterize the molecular pharmacology of Kir4.1 inhibition by CQ Rodriguez-Menchaca et al. Jul 22, 2011 · Read "Mechanisms for Kir channel inhibition by quinacrine: acute pore block of Kir2.x channels and interference in PIP2 interaction with Kir2.x and Kir6.2 channels, Pflügers Archiv European Journal of Physiologyl of Physiology" on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your …. Valdés-Abadía B, Morán-Zendejas R, Rangel-Flores JM , Rodríguez-Menchaca AA. 2008 Stop by both substances is certainly relieved by membrane hyperpolarization and. Chloroquine overdose remains the most severe and frequent cause of antimalarial drug poisonings. 2014). (2009) Identification of a C-terminus domain critical for the sensitivity of Kir2.1 to cholesterol Apr 12, 2020 · This study, entitled “Chloroquine is a potent inhibitor of SARS coronavirus infection and spread,” was completed and published on August 22, 2005, a study of which Dr. Kurata, Colin G. Rodríguez-Menchaca, Angélica López-Izquierdo, Tania Ferrer, Harley T Frontiers | The Antimalarial Chloroquine Reduces the https://www.frontiersin.org/articles/10.3389/fphar.2019.01392 Nov 27, 2019 · Previous work by us and others showed that chloroquine also blocks I k1 (Rodriguez-Menchaca et al., 2008; Noujaim et al., 2010).