Cargando…

Discovery of Glycine Hydrazide Pore-occluding CFTR Inhibitors: Mechanism, Structure–Activity Analysis, and In Vivo Efficacy

The cystic fibrosis transmembrane conductance regulator (CFTR) protein is a cAMP-regulated epithelial Cl(−) channel that, when defective, causes cystic fibrosis. Screening of a collection of 100,000 diverse small molecules revealed four novel chemical classes of CFTR inhibitors with K(i) < 10 μM,...

Descripción completa

Detalles Bibliográficos
Autores principales:	Muanprasat, Chatchai, Sonawane, N.D., Salinas, Danieli, Taddei, Alessandro, Galietta, Luis J.V., Verkman, A.S.
Formato:	Texto
Lenguaje:	English
Publicado:	The Rockefeller University Press 2004
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2229623/ https://www.ncbi.nlm.nih.gov/pubmed/15277574 http://dx.doi.org/10.1085/jgp.200409059

Ejemplares similares

Steviol Reduces MDCK Cyst Formation and Growth by Inhibiting CFTR Channel Activity and Promoting Proteasome-Mediated CFTR Degradation
por: Yuajit, Chaowalit, et al.
Publicado: (2013)

Antidiarrheal efficacy of a quinazolin CFTR inhibitor on human intestinal epithelial cell and in mouse model of cholera
por: Patanayindee, Jenvit, et al.
Publicado: (2012)

Determinants of [Cl(−)] in recycling and late endosomes and Golgi complex measured using fluorescent ligands
por: Sonawane, N.D., et al.
Publicado: (2003)

Proinflammatory cytokine secretion is suppressed by TMEM16A or CFTR channel activity in human cystic fibrosis bronchial epithelia
por: Veit, Guido, et al.
Publicado: (2012)

Pharmacological Correctors of Mutant CFTR Mistrafficking
por: Pedemonte, Nicoletta, et al.
Publicado: (2012)

Transmembrane helical interactions in the CFTR channel pore
por: Das, Jhuma, et al.
Publicado: (2017)

CFTR-Adenylyl Cyclase I Association Responsible for UTP Activation of CFTR in Well-Differentiated Primary Human Bronchial Cell Cultures
por: Namkung, Wan, et al.
Publicado: (2010)

Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel
por: Pedemonte, Nicoletta, et al.
Publicado: (2020)

Probing an Open CFTR Pore with Organic Anion Blockers
por: Zhou, Zhen, et al.
Publicado: (2002)

Chitin and Chitosan Derivatives as Biomaterial Resources for Biological and Biomedical Applications
por: Satitsri, Saravut, et al.
Publicado: (2020)

Deoxyelephantopin and Its Isomer Isodeoxyelephantopin: Anti-Cancer Natural Products with Multiple Modes of Action
por: Mehmood, Tahir, et al.
Publicado: (2022)

Potential Applications of Chitosan-Based Nanomaterials to Surpass the Gastrointestinal Physiological Obstacles and Enhance the Intestinal Drug Absorption
por: Pathomthongtaweechai, Nutthapoom, et al.
Publicado: (2021)

A European regulatory perspective on cystic fibrosis: current treatments, trends in drug development and translational challenges for CFTR modulators
por: Ponzano, Stefano, et al.
Publicado: (2018)

Bioactive Thymosin Alpha-1 Does Not Influence F508del-CFTR Maturation and Activity
por: Armirotti, Andrea, et al.
Publicado: (2019)

Ex vivo model predicted in vivo efficacy of CFTR modulator therapy in a child with rare genotype
por: Terlizzi, Vito, et al.
Publicado: (2021)

Chitosan Oligosaccharide Prevents Afatinib-Induced Barrier Disruption and Chloride Secretion through Modulation of AMPK, PI3K/AKT, and ERK Signaling in T84 Cells
por: Mehmood, Tahir, et al.
Publicado: (2022)

Chitosan Oligosaccharide Promotes Junction Barrier through Modulation of PI3K/AKT and ERK Signaling Intricate Interplay in T84 Cells
por: Mehmood, Tahir, et al.
Publicado: (2023)

Recent Strategic Advances in CFTR Drug Discovery: An Overview
por: Rusnati, Marco, et al.
Publicado: (2020)

Nonintegral stoichiometry in CFTR gating revealed by a pore-lining mutation
por: Jih, Kang-Yang, et al.
Publicado: (2012)

Discovery of Fungus-Derived Nornidulin as a Novel TMEM16A Inhibitor: A Potential Therapy to Inhibit Mucus Secretion in Asthma
por: Pongkorpsakol, Pawin, et al.
Publicado: (2023)

Novel Role for CFTR in Fluid Absorption from the Distal Airspaces of the Lung
por: Fang, X., et al.
Publicado: (2002)

cAMP Stimulates SLC26A3 Activity in Human Colon by a CFTR-Dependent Mechanism That Does Not Require CFTR Activity
por: Tse, Chung-Ming, et al.
Publicado: (2019)

Isonicotinic Acid Hydrazide
Publicado: (1952)

An Update on CFTR Drug Discovery: Opportunities and Challenges
por: D’Ursi, Pasqualina, et al.
Publicado: (2022)

Structure-based discovery of CFTR potentiators and inhibitors
por: Liu, Fangyu, et al.
Publicado: (2023)

Unblocking Ion‐occluded Pore Channels in Poly(triazine imide) Framework for Proton Conduction
por: Chi, Heng‐Yu, et al.
Publicado: (2022)

Functionalization of Magnetic Chitosan Particles for the Sorption of U(VI), Cu(II) and Zn(II)—Hydrazide Derivative of Glycine-Grafted Chitosan
por: Hamza, Mohammed F., et al.
Publicado: (2017)

Patent arterial duct occlusion with two Amplatzer Duct Occluder devices
por: Grech, V, et al.
Publicado: (2011)

CFTR Channel Pharmacology: Novel Pore Blockers Identified by High-throughput Screening
por: Sheppard, David N.
Publicado: (2004)

Mutation-induced Blocker Permeability and Multiion Block of the CFTR Chloride Channel Pore
por: Gong, Xiandi, et al.
Publicado: (2003)

Obligate coupling of CFTR pore opening to tight nucleotide-binding domain dimerization
por: Mihályi, Csaba, et al.
Publicado: (2016)

Production and purification of mannan oligosaccharide with epithelial tight junction enhancing activity
por: Nopvichai, Chatchai, et al.
Publicado: (2019)

Evaluation of Fused Pyrrolothiazole Systems as Correctors of Mutant CFTR Protein
por: Spanò, Virginia, et al.
Publicado: (2021)

An Adult Mouse Model of Vibrio cholerae-induced Diarrhea for Studying Pathogenesis and Potential Therapy of Cholera
por: Sawasvirojwong, Sutthipong, et al.
Publicado: (2013)

Novel Potential Application of Chitosan Oligosaccharide for Attenuation of Renal Cyst Growth in the Treatment of Polycystic Kidney Disease
por: Pathomthongtaweechai, Nutthapoom, et al.
Publicado: (2020)

High-Throughput Screening for Modulators of CFTR Activity Based on Genetically Engineered Cystic Fibrosis Disease-Specific iPSCs
por: Merkert, Sylvia, et al.
Publicado: (2019)

Repurposing calcium-sensing receptor agonist cinacalcet for treatment of CFTR-mediated secretory diarrheas
por: Oak, Apurva A., et al.
Publicado: (2021)

A pore-occluding phenylalanine gate prevents ion slippage through plant ammonium transporters
por: Ganz, Pascal, et al.
Publicado: (2019)

IMAGE-BASED β-ADRENERGIC SWEAT RATE ASSAY CAPTURES MINIMAL CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) FUNCTION
por: Salinas, Danieli Barino, et al.
Publicado: (2019)

Positive Charges at the Intracellular Mouth of the Pore Regulate Anion Conduction in the CFTR Chloride Channel
por: Aubin, Chantal N. St., et al.
Publicado: (2006)

Cannot write session to /tmp/vufind_sessions/sess_vavkeq9hpmlihno9rcdj1l3ilt