List of works - Pierre Falson

2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.

scientific article

5-Oxo-hexahydroquinoline derivatives as modulators of P-gp, MRP1 and BCRP transporters to overcome multidrug resistance in cancer cells

scientific article published on 02 November 2018

A hydrophobic filter confers the cation selectivity of Zygosaccharomyces rouxii plasma-membrane Na+/H+ antiporter.

scientific article

A new method for the reconstitution of membrane proteins into giant unilamellar vesicles

scientific article

A template model for studying anticancer drug efflux transporter inhibitors in vitro

scientific article published on 08 August 2012

ABCG2 transports and transfers heme to albumin through its large extracellular loop

scientific article

Alpha subunit of mitochondrial F1-ATPase from the fission yeast. Deduced sequence of the wild type and identification of a mutation that alters apparent negative cooperativity ⬇️

scientific article published on January 5, 1991

An efficient procedure to dialyze volumes in the range of 10-200 microliters.

scientific article published in July 1992

Atomic modelling and systematic mutagenesis identify residues in multiple drug binding sites that are essential for drug resistance in the major Candida transporter Cdr1.

scientific article

Au courant computation of the PDB to audit diffraction anisotropy of soluble and membrane proteins

scientific article published on 19 May 2018

Beta subunit of mitochondrial F1-ATPase from the fission yeast. Deduced sequence of the wild type protein and identification of a mutation that increases nucleotide binding.

scientific article published on August 1991

Cdr1p highlights the role of the non-hydrolytic ATP-binding site in driving drug translocation in asymmetric ABC pumps

scientific article published on 14 November 2019

Characterization of a protease-resistant domain of the cytosolic portion of sarcoplasmic reticulum Ca2+-ATPase. Nucleotide- and metal-binding sites.

scientific article

Chemical modification of thiol groups of mitochondrial F1-ATPase from the yeast Schizosaccharomyces pombe. Involvement of alpha- and gamma-subunits in the enzyme activity

scientific article published on 01 June 1986

Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2

scientific article published on 05 July 2020

Clean Western blots of membrane proteins after yeast heterologous expression following a shortened version of the method of Perini et al

scientific article published on 01 October 2000

Complete removal and exchange of sodium dodecyl sulfate bound to soluble and membrane proteins and restoration of their activities, using ceramic hydroxyapatite chromatography

scientific article published on 01 May 1997

Dicarboxylate-Oside Detergents for Extraction, Overstabilization and Crystallization of Membrane Proteins.

scientific article published on 29 January 2018

Diffraction anisotropy falloff in the direction of the detergent belt for two centered monoclinic crystals of OmpF

scientific article

Directed Mutational Strategies Reveal Drug Binding and Transport by the MDR Transporters of Candida albicans

scientific article

Efficient and stable reconstitution of the ABC transporter BmrA for solid-state NMR studies

scientific article published on 12 June 2014

Expression of the sarcoplasmic reticulum Ca(2+)-ATPase in yeast.

scientific article published on October 1994

Externalized Keratin 8: A Target at the Interface of Microenvironment and Intracellular Signaling in Colorectal Cancer Cells

scientific article published on 16 November 2018

Flavonoid dimers are highly potent killers of multidrug resistant cancer cells overexpressing MRP1.

scientific article published on 28 October 2016

Gradient reconstitution of membrane proteins for solid-state NMR studies

scientific article published on 12 September 2017

Hepatitis C Virus Envelope Glycoprotein E1 Forms Trimers at the Surface of the Virion

scientific article

Identification of pyrrolopyrimidine derivative PP-13 as a novel microtubule-destabilizing agent with promising anticancer properties

scientific article published on 31 August 2017

Involvement of the cytoplasmic loop L6-7 in the entry mechanism for transport of Ca2+ through the sarcoplasmic reticulum Ca2+-ATPase.

scientific article published on 18 January 2002

Involvement of the cytoplasmic loop L6-7 in the entry mechanism for transport of Ca2+ through the sarcoplasmic reticulum Ca2+-ATPase.

scientific article published in April 2003

Leishmania tarentolae as a Promising Tool for Expressing Polytopic and Multi-Transmembrane Spans Eukaryotic Membrane Proteins: The Case of the ABC Pump ABCG6.

scientific article

Ligand binding to macromolecules or micelles: use of centrifugal ultrafiltration to measure low-affinity binding

scientific article published on 01 November 1998

Localization of putative binding sites for cyclic guanosine monophosphate and the anti-cancer drug 5-fluoro-2'-deoxyuridine-5'-monophosphate on ABCC11 in silico models

scientific article

MRP1-dependent Collateral Sensitivity of Multidrug-resistant Cancer Cells: Identifying Selective Modulators Inducing Cellular Glutathione Depletion.

scientific article published on 18 November 2016

Make azoles active again: chalcones as potent reversal agents of transporters-mediated resistance in Candida albicans

scientific article published on 25 July 2018

Methoxy stilbenes as potent, specific, untransported, and noncytotoxic inhibitors of breast cancer resistance protein

scientific article published on 11 November 2011

Modular construction of quaternary hemiaminal-based inhibitor candidates and their in cellulo assessment with HIV-1 protease.

scientific article published on 14 June 2013

Modulators of the Efflux Pump Cdr1p of Candida albicans: Mechanisms of Action and Chemical Features.

scientific article published on 22 May 2017

Modulators of the human ABCC2: hope from natural sources?

scientific article

Molecular Basis of Substrate Polyspecificity of the Candida albicans Mdr1p Multidrug/H+ Antiporter.

scientific article published on 13 January 2018

Molecular analysis of the massive GSH transport mechanism mediated by the human Multidrug Resistant Protein 1/ABCC1

scientific article published on 06 May 2020

Monoterpene indole alkaloid azine derivatives as MDR reversal agents.

scientific article published on 2 December 2017

Multidrug ABC transporter Cdr1 of Candida albicans harbors specific and overlapping binding sites for human steroid hormones transport.

scientific article

Multidrug resistance ABC transporter structure predictions by homology modeling approaches

scientific article published on March 2011

Optimization of the chromone scaffold through QSAR and docking studies: Identification of potent inhibitors of ABCG2

scientific article published on 10 October 2019

Optimizing the flavanone core toward new selective nitrogen-containing modulators of ABC transporters.

scientific article published on 23 March 2018

Ovarian cancer cells cisplatin sensitization agents selected by mass cytometry target ABCC2 inhibition

scientific article published on 31 May 2018

Overcoming the toxicity of membrane peptide expression in bacteria by upstream insertion of Asp-Pro sequence.

scientific article published in January 2004

Overexpression of SERCA1a Ca2+-ATPase in yeast.

scientific article published on April 2003

PDR-like ABC systems in pathogenic fungi

scientific article published on 25 September 2019

Peroxisomal ATP-binding cassette transporters form mainly tetramers.

scientific article published on 3 March 2017

Polymer "ruthenium-cyclopentadienyl" conjugates - New emerging anti-cancer drugs

scientific article published on 25 February 2019

Potent and fully noncompetitive peptidomimetic inhibitor of multidrug resistance P-glycoprotein.

scientific article

Probing of membrane topology and stability of sarcoplasmic reticulum Ca(2+)-ATPase and Na+,K+ -ATPase with sequence-specific antibodies

scientific article published on 01 November 1997

Purification from a yeast mutant of mitochondrial F1 with modified β-subunit

scientific article published in June 1989

Purification of SERCA1a Ca2+-ATPase mutants expressed in yeast

scientific article published on 01 April 2003

Quantification of Detergents Complexed with Membrane Proteins

scientific article

Quantitative evaluation of the combination between cytotoxic drug and efflux transporter inhibitors based on a tumour growth inhibition model.

scientific article published on 6 February 2013

Revertant of the yeast Schizosaccharomyces pombe with modified α subunits of mitochondrial ATPase-ATPsynthase: Impaired nucleotide interactions with soluble and membrane-bound enzyme

scientific article published in November 1987

Role of the yeast ABC transporter Yor1p in cadmium detoxification

scientific article published in 2006

Spontaneous Suppressors against Debilitating Transmembrane Mutants of <i>Ca</i>Mdr1 Disclose Novel Interdomain Communication via Signature Motifs of the Major Facilitator Superfamily

scientific article published on 22 May 2022

Stoichiometry of the MexA-OprM binding, as investigated by blue native gel electrophoresis.

scientific article published in April 2012

Structural insight into the cooperativity between catalytic and noncatalytic sites of F1-ATPase.

scientific article published in July 2004

Structure-based design and profiling of novel 17β-HSD14 inhibitors

scientific article published on 22 May 2018

Structure-function relationships of mitochondrial ATPase-ATPsynthase using Schizosaccharomyces pombe yeast mutants with altered F1 subunits

scientific article published in August 1989

Structures of P-glycoprotein reveal its conformational flexibility and an epitope on the nucleotide-binding domain

scientific article

Structuring detergents for extracting and stabilizing functional membrane proteins

scientific article

Stubborn contaminants: influence of detergents on the purity of the multidrug ABC transporter BmrA.

scientific article published on 17 December 2014

Synthesis and Anticancer Cytotoxicity of Azaaurones Overcoming Multidrug Resistance

scientific article published on 10 February 2020

Targeting the multidrug ABCG2 transporter with flavonoidic inhibitors: in vitro optimization and in vivo validation.

scientific article published on January 2011

The acridone derivative MBLI-87 sensitizes breast cancer resistance protein-expressing xenografts to irinotecan

scientific article published on 07 January 2011

The cytoplasmic loop between putative transmembrane segments 6 and 7 in sarcoplasmic reticulum Ca2+-ATPase binds Ca2+ and is functionally important

scientific article published on 01 July 1997

The cytoplasmic loop located between transmembrane segments 6 and 7 controls activation by Ca2+ of sarcoplasmic reticulum Ca2+-ATPase.

scientific article

Two different centered monoclinic crystals of the E. coli outer-membrane protein OmpF originate from the same building block

scientific article

Understanding polyspecificity within the substrate-binding cavity of the human multidrug resistance P-glycoprotein

scientific article

Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand

scientific article published on 12 December 2018

Urea reduces the aggregation of membrane proteins on sodium dodecyl sulfate-polyacrylamide gel electrophoresis

scientific article published on 01 May 1996

W1038 near D-loop of NBD2 is a focal point for inter-domain communication in multidrug transporter Cdr1 of Candida albicans

scientific article published on 30 January 2018

X-ray diffraction reveals the intrinsic difference in the physical properties of membrane and soluble proteins.

scientific article published on 5 December 2017

pHluorin enables insights into the transport mechanism of antiporter Mdr1: R215 is critical for drug/H+ antiport.

scientific article published on 18 July 2016

List of works by Pierre Falson

2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.

5-Oxo-hexahydroquinoline derivatives as modulators of P-gp, MRP1 and BCRP transporters to overcome multidrug resistance in cancer cells

A hydrophobic filter confers the cation selectivity of Zygosaccharomyces rouxii plasma-membrane Na+/H+ antiporter.

A new method for the reconstitution of membrane proteins into giant unilamellar vesicles

A template model for studying anticancer drug efflux transporter inhibitors in vitro

ABCG2 transports and transfers heme to albumin through its large extracellular loop

Alpha subunit of mitochondrial F1-ATPase from the fission yeast. Deduced sequence of the wild type and identification of a mutation that alters apparent negative cooperativity ⬇️

An efficient procedure to dialyze volumes in the range of 10-200 microliters.

Atomic modelling and systematic mutagenesis identify residues in multiple drug binding sites that are essential for drug resistance in the major Candida transporter Cdr1.

Au courant computation of the PDB to audit diffraction anisotropy of soluble and membrane proteins

Beta subunit of mitochondrial F1-ATPase from the fission yeast. Deduced sequence of the wild type protein and identification of a mutation that increases nucleotide binding.

Cdr1p highlights the role of the non-hydrolytic ATP-binding site in driving drug translocation in asymmetric ABC pumps

Characterization of a protease-resistant domain of the cytosolic portion of sarcoplasmic reticulum Ca2+-ATPase. Nucleotide- and metal-binding sites.

Chemical modification of thiol groups of mitochondrial F1-ATPase from the yeast Schizosaccharomyces pombe. Involvement of alpha- and gamma-subunits in the enzyme activity

Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2

Clean Western blots of membrane proteins after yeast heterologous expression following a shortened version of the method of Perini et al

Complete removal and exchange of sodium dodecyl sulfate bound to soluble and membrane proteins and restoration of their activities, using ceramic hydroxyapatite chromatography

Dicarboxylate-Oside Detergents for Extraction, Overstabilization and Crystallization of Membrane Proteins.

Diffraction anisotropy falloff in the direction of the detergent belt for two centered monoclinic crystals of OmpF

Directed Mutational Strategies Reveal Drug Binding and Transport by the MDR Transporters of Candida albicans

Efficient and stable reconstitution of the ABC transporter BmrA for solid-state NMR studies

Expression of the sarcoplasmic reticulum Ca(2+)-ATPase in yeast.

Externalized Keratin 8: A Target at the Interface of Microenvironment and Intracellular Signaling in Colorectal Cancer Cells

Flavonoid dimers are highly potent killers of multidrug resistant cancer cells overexpressing MRP1.

Gradient reconstitution of membrane proteins for solid-state NMR studies

Hepatitis C Virus Envelope Glycoprotein E1 Forms Trimers at the Surface of the Virion

Identification of pyrrolopyrimidine derivative PP-13 as a novel microtubule-destabilizing agent with promising anticancer properties

Involvement of the cytoplasmic loop L6-7 in the entry mechanism for transport of Ca2+ through the sarcoplasmic reticulum Ca2+-ATPase.

Involvement of the cytoplasmic loop L6-7 in the entry mechanism for transport of Ca2+ through the sarcoplasmic reticulum Ca2+-ATPase.

Leishmania tarentolae as a Promising Tool for Expressing Polytopic and Multi-Transmembrane Spans Eukaryotic Membrane Proteins: The Case of the ABC Pump ABCG6.

Ligand binding to macromolecules or micelles: use of centrifugal ultrafiltration to measure low-affinity binding

Localization of putative binding sites for cyclic guanosine monophosphate and the anti-cancer drug 5-fluoro-2'-deoxyuridine-5'-monophosphate on ABCC11 in silico models

MRP1-dependent Collateral Sensitivity of Multidrug-resistant Cancer Cells: Identifying Selective Modulators Inducing Cellular Glutathione Depletion.

Make azoles active again: chalcones as potent reversal agents of transporters-mediated resistance in Candida albicans

Methoxy stilbenes as potent, specific, untransported, and noncytotoxic inhibitors of breast cancer resistance protein

Modular construction of quaternary hemiaminal-based inhibitor candidates and their in cellulo assessment with HIV-1 protease.

Modulators of the Efflux Pump Cdr1p of Candida albicans: Mechanisms of Action and Chemical Features.

Modulators of the human ABCC2: hope from natural sources?

Molecular Basis of Substrate Polyspecificity of the Candida albicans Mdr1p Multidrug/H+ Antiporter.

Molecular analysis of the massive GSH transport mechanism mediated by the human Multidrug Resistant Protein 1/ABCC1

Monoterpene indole alkaloid azine derivatives as MDR reversal agents.

Multidrug ABC transporter Cdr1 of Candida albicans harbors specific and overlapping binding sites for human steroid hormones transport.

Multidrug resistance ABC transporter structure predictions by homology modeling approaches

Optimization of the chromone scaffold through QSAR and docking studies: Identification of potent inhibitors of ABCG2

Optimizing the flavanone core toward new selective nitrogen-containing modulators of ABC transporters.

Ovarian cancer cells cisplatin sensitization agents selected by mass cytometry target ABCC2 inhibition

Overcoming the toxicity of membrane peptide expression in bacteria by upstream insertion of Asp-Pro sequence.

Overexpression of SERCA1a Ca2+-ATPase in yeast.

PDR-like ABC systems in pathogenic fungi

Peroxisomal ATP-binding cassette transporters form mainly tetramers.

Polymer "ruthenium-cyclopentadienyl" conjugates - New emerging anti-cancer drugs

Potent and fully noncompetitive peptidomimetic inhibitor of multidrug resistance P-glycoprotein.

Probing of membrane topology and stability of sarcoplasmic reticulum Ca(2+)-ATPase and Na+,K+ -ATPase with sequence-specific antibodies

Purification from a yeast mutant of mitochondrial F1 with modified β-subunit

Purification of SERCA1a Ca2+-ATPase mutants expressed in yeast

Quantification of Detergents Complexed with Membrane Proteins

Quantitative evaluation of the combination between cytotoxic drug and efflux transporter inhibitors based on a tumour growth inhibition model.

Revertant of the yeast Schizosaccharomyces pombe with modified α subunits of mitochondrial ATPase-ATPsynthase: Impaired nucleotide interactions with soluble and membrane-bound enzyme

Role of the yeast ABC transporter Yor1p in cadmium detoxification

Spontaneous Suppressors against Debilitating Transmembrane Mutants of <i>Ca</i>Mdr1 Disclose Novel Interdomain Communication via Signature Motifs of the Major Facilitator Superfamily

Stoichiometry of the MexA-OprM binding, as investigated by blue native gel electrophoresis.

Structural insight into the cooperativity between catalytic and noncatalytic sites of F1-ATPase.

Structure-based design and profiling of novel 17β-HSD14 inhibitors

Structure-function relationships of mitochondrial ATPase-ATPsynthase using Schizosaccharomyces pombe yeast mutants with altered F1 subunits

Structures of P-glycoprotein reveal its conformational flexibility and an epitope on the nucleotide-binding domain

Structuring detergents for extracting and stabilizing functional membrane proteins

Stubborn contaminants: influence of detergents on the purity of the multidrug ABC transporter BmrA.

Synthesis and Anticancer Cytotoxicity of Azaaurones Overcoming Multidrug Resistance

Targeting the multidrug ABCG2 transporter with flavonoidic inhibitors: in vitro optimization and in vivo validation.

The acridone derivative MBLI-87 sensitizes breast cancer resistance protein-expressing xenografts to irinotecan

The cytoplasmic loop between putative transmembrane segments 6 and 7 in sarcoplasmic reticulum Ca2+-ATPase binds Ca2+ and is functionally important

The cytoplasmic loop located between transmembrane segments 6 and 7 controls activation by Ca2+ of sarcoplasmic reticulum Ca2+-ATPase.

Two different centered monoclinic crystals of the E. coli outer-membrane protein OmpF originate from the same building block

Understanding polyspecificity within the substrate-binding cavity of the human multidrug resistance P-glycoprotein

Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand

Urea reduces the aggregation of membrane proteins on sodium dodecyl sulfate-polyacrylamide gel electrophoresis

W1038 near D-loop of NBD2 is a focal point for inter-domain communication in multidrug transporter Cdr1 of Candida albicans

X-ray diffraction reveals the intrinsic difference in the physical properties of membrane and soluble proteins.

pHluorin enables insights into the transport mechanism of antiporter Mdr1: R215 is critical for drug/H+ antiport.