Cargando…

Substrate-analogous inhibitors exert antimalarial action by targeting the Plasmodium lactate transporter PfFNT at nanomolar scale

Resistance against all available antimalarial drugs calls for novel compounds that hit unexploited targets in the parasite. Here, we show that the recently discovered Plasmodium falciparum lactate/proton symporter, PfFNT, is a valid druggable target, and describe a new class of fluoroalkyl vinylogou...

Descripción completa

Detalles Bibliográficos
Autores principales:	Golldack, André, Henke, Björn, Bergmann, Bärbel, Wiechert, Marie, Erler, Holger, Blancke Soares, Alexandra, Spielmann, Tobias, Beitz, Eric
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Public Library of Science 2017
Materias:	Research Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5298233/ https://www.ncbi.nlm.nih.gov/pubmed/28178358 http://dx.doi.org/10.1371/journal.ppat.1006172

Ejemplares similares

The Plasmodium Lactate/H(+) Transporter PfFNT Is Essential and Druggable In Vivo
por: Davies, Heledd, et al.
Publicado: (2023)

Cell-Free and Yeast-Based Production of the Malarial Lactate Transporter, PfFNT, Delivers Comparable Yield and Protein Quality
por: Hajek, Philipp, et al.
Publicado: (2019)

Structural characterization of the Plasmodium falciparum lactate transporter PfFNT alone and in complex with antimalarial compound MMV007839 reveals its inhibition mechanism
por: Peng, Xi, et al.
Publicado: (2021)

The Malaria Parasite's Lactate Transporter PfFNT Is the Target of Antiplasmodial Compounds Identified in Whole Cell Phenotypic Screens
por: Hapuarachchi, Sanduni V., et al.
Publicado: (2017)

Discovery and Development of Inhibitors of the Plasmodial FNT-Type Lactate Transporter as Novel Antimalarials
por: Nerlich, Cornelius, et al.
Publicado: (2021)

Pentafluoro‐3‐hydroxy‐pent‐2‐en‐1‐ones Potently Inhibit FNT‐Type Lactate Transporters from all Five Human‐Pathogenic Plasmodium Species
por: Walloch, Philipp, et al.
Publicado: (2021)

Pentamidine Is Not a Permeant but a Nanomolar Inhibitor of the Trypanosoma brucei Aquaglyceroporin-2
por: Song, Jie, et al.
Publicado: (2016)

Functional Characterization of the FNT Family Nitrite Transporter of Marine Picocyanobacteria
por: Maeda, Shin-ichi, et al.
Publicado: (2015)

Neurotoxicity of a Biopesticide Analog on Zebrafish Larvae at Nanomolar Concentrations
por: Nasri, Ahmed, et al.
Publicado: (2016)

Effects of protracted administration of FNT on immune function of surgical cancer patients
por: Bitzani, M, et al.
Publicado: (2003)

Stable Translocation Intermediates Jam Global Protein Export in Plasmodium falciparum Parasites and Link the PTEX Component EXP2 with Translocation Activity
por: Mesén-Ramírez, Paolo, et al.
Publicado: (2016)

Discovery of Small-Molecule Allosteric Inhibitors of PfATC as Antimalarials
por: Wang, Chao, et al.
Publicado: (2022)

Genetic validation of PfFKBP35 as an antimalarial drug target
por: Thommen, Basil T, et al.
Publicado: (2023)

Breast cancer stem cell selectivity of synthetic nanomolar-active salinomycin analogs
por: Huang, Xiaoli, et al.
Publicado: (2016)

Palmitic Acid Analogs Exhibit Nanomolar Binding Affinity for the HIV-1 CD4 Receptor and Nanomolar Inhibition of gp120-to-CD4 Fusion
por: Paskaleva, Elena E., et al.
Publicado: (2010)

Structural Optimization of BIPPO Analogs as Potent Antimalarials
por: Zheng, Yang, et al.
Publicado: (2023)

Characterization of PfTrxR inhibitors using antimalarial assays and in silico techniques
por: Munigunti, Ranjith, et al.
Publicado: (2013)

Orthosteric–allosteric dual inhibitors of PfHT1 as selective antimalarial agents
por: Huang, Jian, et al.
Publicado: (2021)

Modified DNA Aptamers for C-Reactive Protein and Lactate Dehydrogenase-5 with Sub-Nanomolar Affinities
por: Minagawa, Hirotaka, et al.
Publicado: (2020)

The C-terminal Six Amino Acids of the FNT Channel FocA Are Required for Formate Translocation But Not Homopentamer Integrity
por: Hunger, Doreen, et al.
Publicado: (2017)

Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4
por: Ashton, Trent D., et al.
Publicado: (2023)

Identification and Functional Validation of the Novel Antimalarial Resistance Locus PF10_0355 in Plasmodium falciparum
por: Van Tyne, Daria, et al.
Publicado: (2011)

Combined Transcriptome and Proteome Profiling for Role of pfEMP1 in Antimalarial Mechanism of Action of Dihydroartemisinin
por: Chen, Lina, et al.
Publicado: (2021)

Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
por: Aguiar, Anna C.C., et al.
Publicado: (2018)

Synthesis and antiplasmodial assessment of nitazoxanide and analogs as new antimalarial candidates
por: Irabuena, Camila, et al.
Publicado: (2022)

5-Phenoxy Primaquine Analogs and the Tetraoxane Hybrid as Antimalarial Agents
por: Jansongsaeng, Somruedee, et al.
Publicado: (2021)

Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials
por: Mahindra, Amit, et al.
Publicado: (2020)

Emerging Southeast Asian PfCRT mutations confer Plasmodium falciparum resistance to the first-line antimalarial piperaquine
por: Ross, Leila S., et al.
Publicado: (2018)

Plasmodium falciparum Thioredoxin Reductase (PfTrxR) and Its Role as a Target for New Antimalarial Discovery
por: McCarty, Sara E., et al.
Publicado: (2015)

Fluorescence Cross-Correlation Spectroscopy Yields True Affinity and Binding Kinetics of Plasmodium Lactate Transport Inhibitors
por: Jakobowska, Iga, et al.
Publicado: (2021)

The glycyl-radical enzyme 2-ketobutyrate formate-lyase, TdcE, interacts specifically with the formate-translocating FNT-channel protein FocA
por: Falke, Dörte, et al.
Publicado: (2016)

Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds
por: Pingaew, Ratchanok, et al.
Publicado: (2010)

Nanomolar Inhibitors of Trypanosoma brucei RNA Triphosphatase
por: Smith, Paul, et al.
Publicado: (2016)

Anticancer metallohelices: nanomolar potency and high selectivity
por: Kaner, Rebecca A., et al.
Publicado: (2016)

Na(+) Regulation in the Malaria Parasite Plasmodiumfalciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials
por: Spillman, Natalie J., et al.
Publicado: (2013)

Targeting Channels and Transporters in Protozoan Parasite Infections
por: Meier, Anna, et al.
Publicado: (2018)

Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL(3)B
por: Reynolds, Jennifer M, et al.
Publicado: (2007)

The malaria parasite cation ATPase PfATP4 and its role in the mechanism of action of a new arsenal of antimalarial drugs
por: Spillman, Natalie Jane, et al.
Publicado: (2015)

Mutations in the P-Type Cation-Transporter ATPase 4, PfATP4, Mediate Resistance to Both Aminopyrazole and Spiroindolone Antimalarials
por: Flannery, Erika L., et al.
Publicado: (2014)

Mechanism of artemisinin resistance for malaria PfATP6 L263 mutations and discovering potential antimalarials: An integrated computational approach
por: N., Nagasundaram, et al.
Publicado: (2016)

Cannot write session to /tmp/vufind_sessions/sess_3gdbdif4o17ee3duna374kb17s