List of works - Luis Galietta

3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators

scientific article published in August 2003

4-Chlorobenzo[F]isoquinoline (CBIQ), a novel activator of CFTR and DeltaF508 CFTR.

scientific article published in June 2005

A class of non-selective cation channels in human fibroblasts

scientific article published on 01 August 1989

A minimal isoform of the TMEM16A protein associated with chloride channel activity.

scientific article published on 30 May 2011

A novel missense mutation in ANO5/TMEM16E is causative for gnathodiaphyseal dyplasia in a large Italian pedigree.

scientific article published on 10 October 2012

A volume-sensitive chloride conductance revealed in cultured human keratinocytes by 36Cl- efflux and whole-cell patch clamp recording

scientific article published on 01 November 1992

Activation of Ca(2+)-dependent K+ and Cl- currents by UTP and ATP in CFPAC-1 cells

scientific article published on 01 April 1994

Alpha-aminoazaheterocyclic-methylglyoxal adducts do not inhibit cystic fibrosis transmembrane conductance regulator chloride channel activity.

scientific article published on 13 February 2008

Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker

scientific article published on January 2004

Altered expression of Ano1 variants in human diabetic gastroparesis

scientific article

Alternative splicing at a NAGNAG acceptor site as a novel phenotype modifier

scientific article

Alternative splicing of in-frame exon associated with premature termination codons: implications for readthrough therapies.

scientific article

Analysis of ion transport in the airway epithelium using RNA interference

scientific article published on June 2009

Anoctamin-1/TMEM16A is the major apical iodide channel of the thyrocyte

scientific article published on 08 October 2014

Antihypertensive 1,4-dihydropyridines as correctors of the cystic fibrosis transmembrane conductance regulator channel gating defect caused by cystic fibrosis mutations.

scientific article published on 8 September 2005

Association of TMEM16A chloride channel overexpression with airway goblet cell metaplasia.

scientific article

Asymmetric 4-aryl-1,4-dihydropyridines potentiate mutant cystic fibrosis transmembrane conductance regulator (CFTR).

scientific article published on 27 August 2012

Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain

scientific article published in September 2003

Binding site of activators of the cystic fibrosis transmembrane conductance regulator in the nucleotide binding domains.

scientific article published on February 2005

Biophysical Characteristics of Swelling-Activated Cl − Channels in Human Tracheal 9HTEo-Cells ⬇️

scientific article published on October 1, 1998

Block of CFTR-dependent chloride currents by inhibitors of multidrug resistance-associated proteins.

scientific article published on 3 February 2007

CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds

scientific article published on 21 March 2003

CFTR chloride channel drug discovery--inhibitors as antidiarrheals and activators for therapy of cystic fibrosis

scientific article published on January 2006

CFTR pharmacology.

scientific article

Ca2+-activated Cl- channels

scientific article published on October 2011

Cell-based imaging of sodium iodide symporter activity with the yellow fluorescent protein variant YFP-H148Q/I152L.

scientific article published on 20 September 2006

Characterization of the human gene coding for the swelling-dependent chloride channel ICln at position 11q13.5-14.1 (CLNS1A) and further characterization of the chromosome 6 (CLNS1B) localization.

scientific article

Chloride channels as drug targets

scientific article

Chromosomal localization of the genes (CLNS1A and CLNS1B) coding for the swelling-dependent chloride channel ICln

scientific article

Cl- currents activated by extracellular nucleotides in human bronchial cells

scientific article published on 01 April 1997

Contribution of CFTR to apical-basolateral fluid transport in cultured human alveolar epithelial type II cells

scientific article published on 2 September 2005

Correction of G551D-CFTR transport defect in epithelial monolayers by genistein but not by CPX or MPB-07.

scientific article

Correction: High-throughput screening for modulators of ACVR1 transcription: discovery of potential therapeutics for fibrodysplasia ossificans progressiva

scientific article

Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines.

scientific article published on 13 May 2011

DOG1 regulates growth and IGFBP5 in gastrointestinal stromal tumors.

scientific article published on 10 April 2013

Development of substituted Benzo[c]quinolizinium compounds as novel activators of the cystic fibrosis chloride channel.

scientific article published on September 1999

Development of the Olfactory Epithelium and Nasal Glands in TMEM16A-/- and TMEM16A+/+ Mice

scientific article published on 11 June 2015

Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel

scientific article published on 21 February 2020

Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy

scientific article

Double mechanism for apical tryptophan depletion in polarized human bronchial epithelium

scientific article

Dual activity of aminoarylthiazoles on the trafficking and gating defects of the cystic fibrosis transmembrane conductance regulator chloride channel caused by cystic fibrosis mutations.

scientific article

Effect of inflammatory stimuli on airway ion transport.

scientific article

Epithelial sodium channel inhibition in primary human bronchial epithelia by transfected siRNA.

scientific article published on 21 August 2008

Epithelial sodium channel silencing as a strategy to correct the airway surface fluid deficit in cystic fibrosis

scientific article published in September 2013

Esculentin-1a-Derived Peptides Promote Clearance of Pseudomonas aeruginosa Internalized in Bronchial Cells of Cystic Fibrosis Patients and Lung Cell Migration: Biochemical Properties and a Plausible Mode of Action

scientific article published on 26 September 2016

Evaluation of a systems biology approach to identify pharmacological correctors of the mutant CFTR chloride channel

scientific article published on 10 March 2016

Evidence against the rescue of defective DeltaF508-CFTR cellular processing by curcumin in cell culture and mouse models.

scientific article published on 26 July 2004

Evidence for direct CFTR inhibition by CFTR(inh)-172 based on Arg347 mutagenesis.

scientific article

Finding new drugs to enhance anion secretion in cystic fibrosis: Toward suitable systems for better drug screening. Report on the pre-conference meeting to the 12th ECFS Basic Science Conference, Albufeira, 25-28 March 2015.

scientific article

Functional analysis of acid-activated Cl⁻ channels: properties and mechanisms of regulation.

scientific article published on January 2015

Functional analysis of mutations in the putative binding site for cystic fibrosis transmembrane conductance regulator potentiators. Interaction between activation and inhibition

scientific article published on 23 January 2007

Gelsolin Secretion in Interleukin-4–treated Bronchial Epithelia and in Asthmatic Airways

scientific article published on 11 August 2005

Genetic Inhibition Of The Ubiquitin Ligase Rnf5 Attenuates Phenotypes Associated To F508del Cystic Fibrosis Mutation.

scientific article published on 17 July 2015

Goblet Cell Hyperplasia Requires High Bicarbonate Transport To Support Mucin Release

scientific article published on 27 October 2016

High-affinity activators of cystic fibrosis transmembrane conductance regulator (CFTR) chloride conductance identified by high-throughput screening

scientific article published on 2 August 2002

High-throughput screening for modulators of ACVR1 transcription: discovery of potential therapeutics for fibrodysplasia ossificans progressiva

scientific article published on 28 April 2016

High-throughput screening identifies FAU protein as a regulator of mutant cystic fibrosis transmembrane conductance regulator channel.

scientific article published on 20 November 2017

High-throughput screening of libraries of compounds to identify CFTR modulators.

scientific article

IL-4 is a potent modulator of ion transport in the human bronchial epithelium in vitro

scientific article published on 01 January 2002

Identification and characterization of a novel promoter for the human ANO1 gene regulated by the transcription factor signal transducer and activator of transcription 6 (STAT6)

scientific article

Identification of CFTR activators and inhibitors: chance or design?

scientific article published in October 2004

Increased expression of ATP12A proton pump in cystic fibrosis airways

scientific article published on 18 October 2018

Influence of cell background on pharmacological rescue of mutant CFTR.

scientific article

Intermolecular Interactions in the TMEM16A Dimer Controlling Channel Activity

scientific article published on 8 December 2016

Ion channel and lipid scramblase activity associated with expression of TMEM16F/ANO6 isoforms.

scientific article published on 24 June 2015

KCNE1-like gene is deleted in AMME contiguous gene syndrome: identification and characterization of the human and mouse homologs.

scientific article

Lectin conjugates as potent, nonabsorbable CFTR inhibitors for reducing intestinal fluid secretion in cholera.

scientific article published on 7 February 2007

Ligand-based design, in silico ADME-Tox filtering, synthesis and biological evaluation to discover new soluble 1,4-DHP-based CFTR activators ⬇️

scientific article published on July 23, 2012

Low Ca2+-sensitive maxi-K+ channels in human cultured fibroblasts

scientific article published on 01 November 1988

Managing the Underlying Cause of Cystic Fibrosis: A Future Role for Potentiators and Correctors ⬇️

scientific article published on October 1, 2013

Modulation of cystic fibrosis transmembrane conductance regulator (CFTR) activity and genistein binding by cytosolic pH.

scientific article published on 25 October 2010

Molecular cloning and functional characterization of a GABA/betaine transporter from human kidney

scientific journal article

Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators.

scientific article published on 02 June 2009

Nanomolar CFTR inhibition by pore-occluding divalent polyethylene glycol-malonic acid hydrazides

scientific article published in July 2008

Nanomolar affinity small molecule correctors of defective Delta F508-CFTR chloride channel gating.

scientific article published on 27 June 2003

New pulmonary therapies directed at targets other than CFTR.

scientific article published on June 2013

Non-canonical translation start sites in the TMEM16A chloride channel

scientific article published on 28 August 2013

Novel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.

scientific article published on 11 November 2015

Peripheral localization of the epithelial sodium channel in the apical membrane of bronchial epithelial cells

scientific article published on 08 April 2019

Pharmacological Correctors of Mutant CFTR Mistrafficking

scientific article

Pharmacological analysis of epithelial chloride secretion mechanisms in adult murine airways

scientific article published on 7 April 2016

Pharmacological rescue of mutant CFTR protein improves the viscoelastic properties of CF mucus.

scientific article published on 8 December 2015

Pharmacoproteomics pinpoints HSP70 interaction for correction of the most frequent Wilson disease-causing mutant of ATP7B

scientific article published on 07 December 2020

Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating

scientific article

Phenylhydrazones as Correctors of a Mutant Cystic Fibrosis Transmembrane Conductance Regulator.

scientific article published on 23 December 2015

Phenylquinoxalinone CFTR activator as potential prosecretory therapy for constipation

scientific article

Proinflammatory cytokine secretion is suppressed by TMEM16A or CFTR channel activity in human cystic fibrosis bronchial epithelia

scientific article

Proteomic analysis of the airway surface liquid: modulation by proinflammatory cytokines

article

Regulation of TMEM16A chloride channel properties by alternative splicing

scientific article

Regulation of taurine transport in murine macrophages ⬇️

scientific article published on January 1, 2001

Regulation of transepithelial ion transport by two different purinoceptors in the apical membrane of canine kidney (MDCK) cells.

scientific article published on March 1995

Rescue of the mutant CFTR chloride channel by pharmacological correctors and low temperature analyzed by gene expression profiling.

scientific article

Rheological Properties of Cystic Fibrosis Bronchial Secretion and in Vitro Drug Permeation Study: The Effect of Sodium Bicarbonate

scientific article

Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening.

scientific article

Speeding Up the Identification of Cystic Fibrosis Transmembrane Conductance Regulator-Targeted Drugs: An Approach Based on Bioinformatics Strategies and Surface Plasmon Resonance.

scientific article published on 8 January 2018

Structure and function of TMEM16 proteins (anoctamins)

scientific article

Structure-activity relationship of 1,4-dihydropyridines as potentiators of the cystic fibrosis transmembrane conductance regulator chloride channel

scientific article published on 23 April 2007

Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).

scientific article published on 11 May 2017

Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis.

scientific article published on 28 May 2015

Synthesis of 4-thiophen-2'-yl-1,4-dihydropyridines as potentiators of the CFTR chloride channel

scientific article published on 20 October 2009

TMEM16 Proteins: Membrane Channels with Unusual Pores

scientific article published on November 2016

TMEM16A alternative splicing coordination in breast cancer.

scientific article published on 16 July 2013

TMEM16A protein: a new identity for Ca(2+)-dependent Cl⁻ channels

scientific article published on December 2010

TMEM16A, a membrane protein associated with calcium-dependent chloride channel activity

scientific article

TMEM16A-TMEM16B chimaeras to investigate the structure-function relationship of calcium-activated chloride channels.

scientific article published in June 2013

TRPV4 and purinergic receptor signalling pathways are separately linked in airway epithelia to CFTR and TMEM16A chloride channels

scientific article published on 12 November 2019

Targeting ion channels in cystic fibrosis

scientific article published on 23 June 2015

The Autophagy Inhibitor Spautin-1 Antagonizes Rescue of Mutant CFTR Through an Autophagy-Independent and USP13-Mediated Mechanism

The TMEM16 protein family: a new class of chloride channels?

scientific article

The TMEM16A chloride channel as an alternative therapeutic target in cystic fibrosis.

scientific article published on April 2014

The anoctamin family: TMEM16A and TMEM16B as calcium-activated chloride channels

scientific article

The combined therapeutic effects of bortezomib and fenretinide on neuroblastoma cells involve endoplasmic reticulum stress response

scientific article

The extracellular calcium-sensing receptor regulates human fetal lung development via CFTR.

scientific article

The search for a common structural moiety among selected pharmacological correctors of the mutant CFTR chloride channel.

scientific article published on January 2014

Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.

scientific article

Thiocyanate transport in resting and IL-4-stimulated human bronchial epithelial cells: role of pendrin and anion channels

scientific article

Thymosin α-1 does not correct F508del-CFTR in cystic fibrosis airway epithelia

scientific article published on 04 April 2019

Thymosin α-1 does not correct F508del-CFTR in cystic fibrosis airway epithelia.

scientific article published on 8 February 2018

Two CFTR mutations within codon 970 differently impact on the chloride channel functionality

scientific article published on 28 March 2019

Unravelling druggable signalling networks that control F508del-CFTR proteostasis

scientific article published on 23 December 2015

Upregulation of TMEM16A Protein in Bronchial Epithelial Cells by Bacterial Pyocyanin

scientific article published on 29 June 2015

Why is the cystic fibrosis gene so frequent?

scientific article published on December 1989

List of works by Luis Galietta

3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators

4-Chlorobenzo[F]isoquinoline (CBIQ), a novel activator of CFTR and DeltaF508 CFTR.

A class of non-selective cation channels in human fibroblasts

A minimal isoform of the TMEM16A protein associated with chloride channel activity.

A novel missense mutation in ANO5/TMEM16E is causative for gnathodiaphyseal dyplasia in a large Italian pedigree.

A volume-sensitive chloride conductance revealed in cultured human keratinocytes by 36Cl- efflux and whole-cell patch clamp recording

Activation of Ca(2+)-dependent K+ and Cl- currents by UTP and ATP in CFPAC-1 cells

Alpha-aminoazaheterocyclic-methylglyoxal adducts do not inhibit cystic fibrosis transmembrane conductance regulator chloride channel activity.

Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker

Altered expression of Ano1 variants in human diabetic gastroparesis

Alternative splicing at a NAGNAG acceptor site as a novel phenotype modifier

Alternative splicing of in-frame exon associated with premature termination codons: implications for readthrough therapies.

Analysis of ion transport in the airway epithelium using RNA interference

Anoctamin-1/TMEM16A is the major apical iodide channel of the thyrocyte

Antihypertensive 1,4-dihydropyridines as correctors of the cystic fibrosis transmembrane conductance regulator channel gating defect caused by cystic fibrosis mutations.

Association of TMEM16A chloride channel overexpression with airway goblet cell metaplasia.

Asymmetric 4-aryl-1,4-dihydropyridines potentiate mutant cystic fibrosis transmembrane conductance regulator (CFTR).

Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain

Binding site of activators of the cystic fibrosis transmembrane conductance regulator in the nucleotide binding domains.

Biophysical Characteristics of Swelling-Activated Cl − Channels in Human Tracheal 9HTEo-Cells ⬇️

Block of CFTR-dependent chloride currents by inhibitors of multidrug resistance-associated proteins.

CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds

CFTR chloride channel drug discovery--inhibitors as antidiarrheals and activators for therapy of cystic fibrosis

CFTR pharmacology.

Ca2+-activated Cl- channels

Cell-based imaging of sodium iodide symporter activity with the yellow fluorescent protein variant YFP-H148Q/I152L.

Characterization of the human gene coding for the swelling-dependent chloride channel ICln at position 11q13.5-14.1 (CLNS1A) and further characterization of the chromosome 6 (CLNS1B) localization.

Chloride channels as drug targets

Chromosomal localization of the genes (CLNS1A and CLNS1B) coding for the swelling-dependent chloride channel ICln

Cl- currents activated by extracellular nucleotides in human bronchial cells

Contribution of CFTR to apical-basolateral fluid transport in cultured human alveolar epithelial type II cells

Correction of G551D-CFTR transport defect in epithelial monolayers by genistein but not by CPX or MPB-07.

Correction: High-throughput screening for modulators of ACVR1 transcription: discovery of potential therapeutics for fibrodysplasia ossificans progressiva

Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines.

DOG1 regulates growth and IGFBP5 in gastrointestinal stromal tumors.

Development of substituted Benzo[c]quinolizinium compounds as novel activators of the cystic fibrosis chloride channel.

Development of the Olfactory Epithelium and Nasal Glands in TMEM16A-/- and TMEM16A+/+ Mice

Discovery of a picomolar potency pharmacological corrector of the mutant CFTR chloride channel

Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy

Double mechanism for apical tryptophan depletion in polarized human bronchial epithelium

Dual activity of aminoarylthiazoles on the trafficking and gating defects of the cystic fibrosis transmembrane conductance regulator chloride channel caused by cystic fibrosis mutations.

Effect of inflammatory stimuli on airway ion transport.

Epithelial sodium channel inhibition in primary human bronchial epithelia by transfected siRNA.

Epithelial sodium channel silencing as a strategy to correct the airway surface fluid deficit in cystic fibrosis

Esculentin-1a-Derived Peptides Promote Clearance of Pseudomonas aeruginosa Internalized in Bronchial Cells of Cystic Fibrosis Patients and Lung Cell Migration: Biochemical Properties and a Plausible Mode of Action

Evaluation of a systems biology approach to identify pharmacological correctors of the mutant CFTR chloride channel

Evidence against the rescue of defective DeltaF508-CFTR cellular processing by curcumin in cell culture and mouse models.

Evidence for direct CFTR inhibition by CFTR(inh)-172 based on Arg347 mutagenesis.

Finding new drugs to enhance anion secretion in cystic fibrosis: Toward suitable systems for better drug screening. Report on the pre-conference meeting to the 12th ECFS Basic Science Conference, Albufeira, 25-28 March 2015.

Functional analysis of acid-activated Cl⁻ channels: properties and mechanisms of regulation.

Functional analysis of mutations in the putative binding site for cystic fibrosis transmembrane conductance regulator potentiators. Interaction between activation and inhibition

Gelsolin Secretion in Interleukin-4–treated Bronchial Epithelia and in Asthmatic Airways

Genetic Inhibition Of The Ubiquitin Ligase Rnf5 Attenuates Phenotypes Associated To F508del Cystic Fibrosis Mutation.

Goblet Cell Hyperplasia Requires High Bicarbonate Transport To Support Mucin Release

High-affinity activators of cystic fibrosis transmembrane conductance regulator (CFTR) chloride conductance identified by high-throughput screening

High-throughput screening for modulators of ACVR1 transcription: discovery of potential therapeutics for fibrodysplasia ossificans progressiva

High-throughput screening identifies FAU protein as a regulator of mutant cystic fibrosis transmembrane conductance regulator channel.

High-throughput screening of libraries of compounds to identify CFTR modulators.

IL-4 is a potent modulator of ion transport in the human bronchial epithelium in vitro

Identification and characterization of a novel promoter for the human ANO1 gene regulated by the transcription factor signal transducer and activator of transcription 6 (STAT6)

Identification of CFTR activators and inhibitors: chance or design?

Increased expression of ATP12A proton pump in cystic fibrosis airways

Influence of cell background on pharmacological rescue of mutant CFTR.

Intermolecular Interactions in the TMEM16A Dimer Controlling Channel Activity

Ion channel and lipid scramblase activity associated with expression of TMEM16F/ANO6 isoforms.

KCNE1-like gene is deleted in AMME contiguous gene syndrome: identification and characterization of the human and mouse homologs.

Lectin conjugates as potent, nonabsorbable CFTR inhibitors for reducing intestinal fluid secretion in cholera.

Ligand-based design, in silico ADME-Tox filtering, synthesis and biological evaluation to discover new soluble 1,4-DHP-based CFTR activators ⬇️

Low Ca2+-sensitive maxi-K+ channels in human cultured fibroblasts

Managing the Underlying Cause of Cystic Fibrosis: A Future Role for Potentiators and Correctors ⬇️

Modulation of cystic fibrosis transmembrane conductance regulator (CFTR) activity and genistein binding by cytosolic pH.

Molecular cloning and functional characterization of a GABA/betaine transporter from human kidney

Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators.

Nanomolar CFTR inhibition by pore-occluding divalent polyethylene glycol-malonic acid hydrazides

Nanomolar affinity small molecule correctors of defective Delta F508-CFTR chloride channel gating.

New pulmonary therapies directed at targets other than CFTR.

Non-canonical translation start sites in the TMEM16A chloride channel

Novel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.

Peripheral localization of the epithelial sodium channel in the apical membrane of bronchial epithelial cells