Cargando…

High-resolution structures of multiple 5-HT(3A)R-setron complexes reveal a novel mechanism of competitive inhibition

Serotonin receptors (5-HT(3A)R) play a crucial role in regulating gut movement, and are the principal target of setrons, a class of high-affinity competitive antagonists, used in the management of nausea and vomiting associated with radiation and chemotherapies. Structural insights into setron-bindi...

Descripción completa

Detalles Bibliográficos
Autores principales:	Basak, Sandip, Kumar, Arvind, Ramsey, Steven, Gibbs, Eric, Kapoor, Abhijeet, Filizola, Marta, Chakrapani, Sudha
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	eLife Sciences Publications, Ltd 2020
Materias:	Biochemistry and Chemical Biology
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7655109/ https://www.ncbi.nlm.nih.gov/pubmed/33063666 http://dx.doi.org/10.7554/eLife.57870

Ejemplares similares

Molecular mechanism of setron-mediated inhibition of full-length 5-HT(3A) receptor
por: Basak, Sandip, et al.
Publicado: (2019)

Competitive binding of MatP and topoisomerase IV to the MukB hinge domain
por: Fisher, Gemma LM, et al.
Publicado: (2021)

The gating cycle of a K(+) channel at atomic resolution
por: Cuello, Luis G, et al.
Publicado: (2017)

tRNA ligase structure reveals kinetic competition between non-conventional mRNA splicing and mRNA decay
por: Peschek, Jirka, et al.
Publicado: (2019)

The molecular appearance of native TRPM7 channel complexes identified by high-resolution proteomics
por: Kollewe, Astrid, et al.
Publicado: (2021)

A systematically-revised ribosome profiling method for bacteria reveals pauses at single-codon resolution
por: Mohammad, Fuad, et al.
Publicado: (2019)

Optical tools for visualizing and controlling human GLP-1 receptor activation with high spatiotemporal resolution
por: Duffet, Loïc, et al.
Publicado: (2023)

A mechanism for the extension and unfolding of parallel telomeric G-quadruplexes by human telomerase at single-molecule resolution
por: Paudel, Bishnu P, et al.
Publicado: (2020)

3.3-Å resolution cryo-EM structure of human ribonucleotide reductase with substrate and allosteric regulators bound
por: Brignole, Edward J, et al.
Publicado: (2018)

Biochemical basis for the regulation of biosynthesis of antiparasitics by bacterial hormones
por: Kapoor, Iti, et al.
Publicado: (2020)

CRISPR-Cas12a exploits R-loop asymmetry to form double-strand breaks
por: Cofsky, Joshua C, et al.
Publicado: (2020)

E. coli TraR allosterically regulates transcription initiation by altering RNA polymerase conformation
por: Chen, James, et al.
Publicado: (2019)

Interferon-β-induced miR-1 alleviates toxic protein accumulation by controlling autophagy
por: Nehammer, Camilla, et al.
Publicado: (2019)

Directed evolution of the rRNA methylating enzyme Cfr reveals molecular basis of antibiotic resistance
por: Tsai, Kaitlyn, et al.
Publicado: (2022)

The interplay of RNA:DNA hybrid structure and G-quadruplexes determines the outcome of R-loop-replisome collisions
por: Kumar, Charanya, et al.
Publicado: (2021)

Myosin with hypertrophic cardiac mutation R712L has a decreased working stroke which is rescued by omecamtiv mecarbil
por: Snoberger, Aaron, et al.
Publicado: (2021)

FER-mediated phosphorylation and PIK3R2 recruitment on IRS4 promotes AKT activation and tumorigenesis in ovarian cancer cells
por: Zhang, Yanchun, et al.
Publicado: (2022)

Redox-controlled reorganization and flavin strain within the ribonucleotide reductase R2b–NrdI complex monitored by serial femtosecond crystallography
por: John, Juliane, et al.
Publicado: (2022)

Schnyder corneal dystrophy-associated UBIAD1 inhibits ER-associated degradation of HMG CoA reductase in mice
por: Jo, Youngah, et al.
Publicado: (2019)

Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function
por: Gerndt, Susanne, et al.
Publicado: (2020)

New insights into the mechanism of dynein motor regulation by lissencephaly-1
por: Markus, Steven M, et al.
Publicado: (2020)

A tryparedoxin-coupled biosensor reveals a mitochondrial trypanothione metabolism in trypanosomes
por: Ebersoll, Samantha, et al.
Publicado: (2020)

Spreading of a mycobacterial cell-surface lipid into host epithelial membranes promotes infectivity
por: Cambier, CJ, et al.
Publicado: (2020)

Determinants of sugar-induced influx in the mammalian fructose transporter GLUT5
por: McComas, Sarah E, et al.
Publicado: (2023)

Single molecule poly(A) tail-seq shows LARP4 opposes deadenylation throughout mRNA lifespan with most impact on short tails
por: Mattijssen, Sandy, et al.
Publicado: (2020)

RNA-dependent RNA targeting by CRISPR-Cas9
por: Strutt, Steven C, et al.
Publicado: (2018)

Role of oxidation of excitation-contraction coupling machinery in age-dependent loss of muscle function in Caenorhabditis elegans
por: Dridi, Haikel, et al.
Publicado: (2022)

The shape of the bacterial ribosome exit tunnel affects cotranslational protein folding
por: Kudva, Renuka, et al.
Publicado: (2018)

Assessing target engagement using proteome-wide solvent shift assays
por: Van Vranken, Jonathan G, et al.
Publicado: (2021)

Identification of orphan ligand-receptor relationships using a cell-based CRISPRa enrichment screening platform
por: Siepe, Dirk H, et al.
Publicado: (2022)

Regulatory coiled-coil domains promote head-to-head assemblies of AAA+ chaperones essential for tunable activity control
por: Carroni, Marta, et al.
Publicado: (2017)

Correction: Proteomic mapping of cytosol-facing outer mitochondrial and ER membranes in living human cells by proximity biotinylation
por: Hung, Victoria, et al.
Publicado: (2019)

Proteomic mapping of cytosol-facing outer mitochondrial and ER membranes in living human cells by proximity biotinylation
por: Hung, Victoria, et al.
Publicado: (2017)

Hfq CLASH uncovers sRNA-target interaction networks linked to nutrient availability adaptation
por: Iosub, Ira Alexandra, et al.
Publicado: (2020)

Bacterial OTU deubiquitinases regulate substrate ubiquitination upon Legionella infection
por: Shin, Donghyuk, et al.
Publicado: (2020)

Cryo-EM reveals two distinct serotonin-bound conformations of full-length 5-HT(3A) receptor
por: Basak, Sandip, et al.
Publicado: (2018)

An engineered transcriptional reporter of protein localization identifies regulators of mitochondrial and ER membrane protein trafficking in high-throughput CRISPRi screens
por: Coukos, Robert, et al.
Publicado: (2021)

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei
por: Alghamdi, Ali H, et al.
Publicado: (2020)

Crystal structure and dynamics of a lipid-induced potential desensitized-state of a pentameric ligand-gated channel
por: Basak, Sandip, et al.
Publicado: (2017)

Protein quality control in the nucleolus safeguards recovery of epigenetic regulators after heat shock
por: Azkanaz, Maria, et al.
Publicado: (2019)

Cannot write session to /tmp/vufind_sessions/sess_rnrr2mldb1d23hma6puhtjqei5