Timeline

Hélène Munier-Lehmann

Group Leader

16 Mar 2024

publication

An equine iPSC-based phenotypic screening platform identifies pro- and anti-viral molecules against West Nile virus.

01 Jan 2024

publication

A journey into the regulatory secrets of the de novo purine nucleotide biosynthesis.

30 Sep 2023

publication

Novel Antiviral Molecules against Ebola Virus Infection.

31 Aug 2023

publication

Modulation of the functional interfaces between retroviral intasomes and the human nucleosome.

20 Jun 2023

publication

Insight into the role of the Bateman domain at the molecular and physiological levels through engineered IMPDHs.

07 Feb 2023

publication

Interaction network among de novo purine nucleotide biosynthesis enzymes in Escherichia coli.

24 Jan 2023

publication

Discovery of Bis-Imidazoline Derivatives as New CXCR4 Ligands.

11 Jan 2023

publication

SigH stress response mediates killing of Mycobacterium tuberculosis by activating nitronaphthofuran prodrugs via induction of Mrx2 expression.

11 Oct 2022

publication

Steroid hormone catabolites activate the pyrin inflammasome through a non-canonical mechanism.

16 Feb 2022

publication

Discovery of bat coronaviruses close to SARS-CoV-2 and infectious for human cells.

12 Feb 2022

publication

Structural basis for the allosteric inhibition of UMP kinase from Gram-positive bacteria, a promising antibacterial target.

05 Dec 2021

publication

Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors.

24 Nov 2021

event

Thesis Defense: “Biosynthèse des nucléotides puriques chez les bactéries : identification d’un métabolon et exploration de la régulation allostérique d’une enzyme-clé de la voie de novo, l’inosine 5’-monophosphate déshydrogénase” – ANTOINE GEDEON – vendredi 17 décembre

21 Jul 2021

publication

SARS-CoV-2 Nsp3 unique domain SUD interacts with guanine quadruplexes and G4-ligands inhibit this interaction.

14 Jan 2021

publication

2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F420)-Dependent Nitroreductase (Ddn).

15 Nov 2020

publication

Endeavors towards transformation of M. tuberculosis thymidylate kinase (MtbTMPK) inhibitors into potential antimycobacterial agents.

11 Sep 2020

publication

Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination.

01 Sep 2020

publication

Synthesis and structure activity relationships of cyanopyridone based anti-tuberculosis agents.

22 Jun 2020

publication

Replication of Equine arteritis virus is efficiently suppressed by purine and pyrimidine biosynthesis inhibitors.

17 Jun 2020

publication

1-(1-Arylethylpiperidin-4-yl)thymine Analogs as Antimycobacterial TMPK Inhibitors.

30 May 2020

publication

A real-time cell-binding assay reveals dynamic features of STxB-Gb3 cointernalization and STxB-mediated cargo delivery into cancer cells.

01 Dec 2019

publication

1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase.

02 Feb 2019

publication

First-in-class allosteric inhibitors of bacterial IMPDHs

02 Jan 2019

publication

Screening and evaluation of antiviral compounds against Equid alpha-herpesviruses using an impedance-based cellular assay

25 May 2018

publication

A Novel Polyaminocarboxylate Compound To Treat Murine Pulmonary Aspergillosis by Interfering with Zinc Metabolism

15 Mar 2018

publication

Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors

18 Jan 2018

publication

Identification of novel leishmanicidal molecules by virtual and biochemical screenings targeting Leishmania eukaryotic translation initiation factor 4A

11 Jan 2018

publication

Synthesis of sulfamide analogues of deoxthymidine monophosphate as potential inhibitors of mycobacterial cell wall biosynthesis

23 Nov 2017

publication

Inhibition of the inflammatory response to stress by targeting interaction between PKR and its cellular activator PACT

28 Aug 2017

publication

Nitazoxanide Analogs Require Nitroreduction for Antimicrobial Activity in Mycobacterium smegmatis

14 Aug 2017

publication

Original chemical series of pyrimidine biosynthesis inhibitors that boost the antiviral interferon response

10 Mar 2017

publication

Tetrahydro-2-furanyl-2,4(1H,3H)-pyrimidinedione derivatives as novel antibacterial compounds against Mycobacterium

24 Aug 2016

publication

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

11 Jul 2016

publication

Administration of zinc chelators improves survival of mice infected with Aspergillus fumigatus both in monotherapy and in combination with caspofungin.

15 May 2016

publication

Anti-mycobacterial activity of thymine derivatives bearing boron clusters

01 Jan 2016

publication

Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors

01 Jan 2016

publication

Synthesis and evaluation of original bioisosteres of bacterial type IIA topoisomerases inhibitors

16 Oct 2015

project

AEGIS (Accelerated Early staGe drug dIScovery)

17 Sep 2015

project

Interferon induction, inflammation and stress in HCV infection and stress-related pathologies

10 Sep 2015

event

Workshop on protein-protein interactions: from low to high-throughput investigations

07 Sep 2015

project

FP7 Targeting the Leishmania kinome for the development of novel anti-parasitic strategies (LeishDrug)

03 Sep 2015

project

Inhibitors of Pseudomonas aeruginosa IMPDH

25 Aug 2015

publication

Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation

20 Aug 2015

project

Inhibitors of TMPK from Mycobacterium tuberculosis

28 Jul 2015

project

ATPase inhibitors, the cases of human heat shock protein 90 and bacterial type IIA topoisomerases

28 Jul 2015

project

Alkoxypyrazoles, inhibitors of dihydroorotate dehydrogenase (DHODH)

22 Jul 2015

project

Inosine-5′-monophosphate dehydrogenase

22 Jul 2015

project

Nucleoside monophosphate kinases (NMPKs)

16 Jul 2015

team

Group: Biochemistry and chemobiology

30 Jun 2015

publication

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

06 Jan 2015

publication

Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH)

05 May 2014

publication

High-throughput screening for broad-spectrum chemical inhibitors of RNA viruses

03 Oct 2013

publication

Inhibition of pyrimidine biosynthesis pathway suppresses viral growth through innate immunity

03 Sep 2013

publication

AutomiG, a biosensor to detect alterations in miRNA biogenesis and in small RNA silencing guided by perfect target complementarity

20 Mar 2013

publication

On dihydroorotate dehydrogenases and their inhibitors and uses

01 Feb 2013

publication

Synergy of the antibiotic colistin with echinocandin antifungals in Candida species

05 Nov 2012

publication

Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors

14 Sep 2012

publication

A phenotypic assay to identify Chikungunya virus inhibitors targeting the nonstructural protein nsP2

05 Mar 2012

publication

The composition of the culture medium influences the β-1,3-glucan metabolism of Aspergillus fumigatus and the antifungal activity of inhibitors of β-1,3-glucan synthesis

01 Mar 2012

publication

Synthesis and evaluation of 6-aza-2′-deoxyuridine monophosphate analogs as inhibitors of thymidylate synthases, and as substrates or inhibitors of thymidine monophosphate kinase in Mycobacterium tuberculosis

01 Jan 2012

publication

Drug design and identification of potent leads against mycobacterium tuberculosis thymidine monophosphate kinase

18 Oct 2011

publication

Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase

10 Dec 2010

publication

Structural and functional characterization of the Mycobacterium tuberculosis uridine monophosphate kinase: insights into the allosteric regulation

15 Oct 2010

publication

Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone

23 Jul 2009

publication

Phosphorylation of dGMP analogs by vaccinia virus TMP kinase and human GMP kinase

03 Oct 2008

publication

Metalloprotease vsm is the major determinant of toxicity for extracellular products of Vibrio splendidus

01 Jul 2008

publication

Exploring acyclic nucleoside analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

25 Apr 2008

publication

Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity

01 Apr 2008

publication

Acyclic phosphonate nucleotides and human adenylate kinases: impact of a borano group on alpha-P position

02 Oct 2007

publication

Rational design of 5′-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth

03 Jun 2007

publication

Structural and functional consequences of single amino acid substitutions in the pyrimidine base binding pocket of Escherichia coli CMP kinase

01 Jan 2007

publication

A new family of inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

01 Oct 2006

publication

Synthesis and biological evaluation of bicyclic nucleosides as inhibitors of M. tuberculosis thymidylate kinase

01 Aug 2006

publication

Multiple microfermentor battery: a versatile tool for use with automated parallel cultures of microorganisms producing recombinant proteins and for optimization of cultivation protocols

02 May 2006

publication

The crystal structure of Mycobacterium tuberculosis adenylate kinase in complex with two molecules of ADP and Mg2+ supports an associative mechanism for phosphoryl transfer.

01 Feb 2006

publication

Unique GMP-binding site in Mycobacterium tuberculosis guanosine monophosphate kinase

01 Apr 2005

publication

LEA3D: a computer-aided ligand design for structure-based drug design

11 Jan 2005

publication

The crystal structure of Mycobacterium tuberculosis thymidylate kinase in complex with 3′-azidodeoxythymidine monophosphate suggests a mechanism for competitive inhibition

01 Dec 2004

publication

Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

01 Dec 2004

publication

High-level production of recombinant sulfide-reactive hemoglobin I from Lucina pectinata in Escherichia coli. High yields of fully functional holoprotein synthesis in the BLi5 E. coli strain

01 Feb 2004

publication

Insight into the activation mechanism of Bordetella pertussis adenylate cyclase by calmodulin using fluorescence spectroscopy

13 Jan 2004

publication

Structural and dynamic studies on ligand-free adenylate kinase from Mycobacterium tuberculosis revealed a closed conformation that can be related to the reduced catalytic activity

15 Sep 2003

publication

Thymidine and thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

28 Aug 2003

publication

3′-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

01 Aug 2003

publication

Comparative study of purine and pyrimidine nucleoside analogues acting on the thymidylate kinases of Mycobacterium tuberculosis and of humans

01 Aug 2003

publication

Mycobacterium tuberculosis thymidine monophosphate kinase inhibitors: Biological evaluation and conformational analysis of 2 ‘- and 3 ‘-modified thymidine analogues

15 Jul 2003

publication

Relationship between bacterial virulence and nucleotide metabolism: a mutation in the adenylate kinase gene renders Yersinia pestis avirulent

01 May 2003

publication

Design of Mycobacterium tuberculosis thymidine monophosphate kinase inhibitors

11 Apr 2003

publication

Mycobacterium tuberculosis thymidylate kinase: structural studies of intermediates along the reaction pathway

01 Apr 2003

publication

Reaction of human UMP-CMP kinase with natural and analog substrates

01 Feb 2003

publication

Enzymatic and structural analysis of inhibitors designed against Mycobacterium tuberculosis thymidylate kinase. New insights into the phosphoryl transfer mechanism

01 Oct 2002

publication

Synthesis and evaluation of thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

01 Jun 2002

publication

Database searching for thymidine and thymidylate kinase inhibitors using three-dimensional structure-based methods

01 Feb 2002

publication

Sugar specificity of bacterial CMP kinases as revealed by crystal structures and mutagenesis of Escherichia coli enzyme

01 Jan 2002

publication

Nucleoside analogues as inhibitors of thymidylate kinases: possible therapeutic applications

01 Aug 2001

publication

X-ray structure of TMP kinase from Mycobacterium tuberculosis complexed with TMP at 1.95 A resolution

01 Jun 2001

publication

Thymidylate kinase of Mycobacterium tuberculosis: a chimera sharing properties common to eukaryotic and bacterial enzymes

01 Jan 2001

publication

1H, 13C and 15N resonance assignment and secondary structure of Mycobacterium tuberculosis adenylate kinase

01 Feb 2000

publication

Crystallization and preliminary X-ray analysis of the thymidylate kinase from Mycobacterium tuberculosis

01 Aug 1999

publication

A new subfamily of short bacterial adenylate kinases with the Mycobacterium tuberculosis enzyme as a model: A predictive and experimental study

21 Jun 1996

publication

Re-expression of the mannose 6-phosphate receptors in receptor-deficient fibroblasts. Complementary function of the two mannose 6-phosphate receptors in lysosomal enzyme targeting.

26 Jan 1996

publication

A casein kinase II phosphorylation site in the cytoplasmic domain of the cation-dependent mannose 6-phosphate receptor determines the high affinity interaction of the AP-1 Golgi assembly proteins with membranes.

01 Aug 1994

publication

Differential sorting of lysosomal enzymes in mannose 6-phosphate receptor-deficient fibroblasts.

15 Dec 1993

publication

Structural and physico-chemical characteristics of Bordetella pertussis adenylate kinase, a tryptophan-containing enzyme.

15 Oct 1993

publication

Structural flexibility of the calmodulin-binding locus in Bordetella pertussis adenylate cyclase. Reconstitution of catalytically active species from fragments or inactive forms of the enzyme.

25 Jan 1993

publication

Characterization of a synthetic calmodulin-binding peptide derived from Bacillus anthracis adenylate cyclase.

25 Jan 1993

publication

Cooperative phenomena in binding and activation of Bordetella pertussis adenylate cyclase by calmodulin.

15 May 1992

publication

The role of histidine 63 in the catalytic mechanism of Bordetella pertussis adenylate cyclase.

14 Jan 1992

publication

1H and 15N NMR characterization of free and bound states of an amphiphilic peptide interacting with calmodulin.

01 Jul 1991

publication

Functional consequences of single amino acid substitutions in calmodulin-activated adenylate cyclase of Bordetella pertussis.

14 Mar 1991

publication

Isolation and characterization of catalytic and calmodulin-binding domains of Bordetella pertussis adenylate cyclase.

04 Sep 1990

publication

A little guide for advanced search:

An equine iPSC-based phenotypic screening platform identifies pro- and anti-viral molecules against West Nile virus.

A journey into the regulatory secrets of the de novo purine nucleotide biosynthesis.

Novel Antiviral Molecules against Ebola Virus Infection.

Modulation of the functional interfaces between retroviral intasomes and the human nucleosome.

Insight into the role of the Bateman domain at the molecular and physiological levels through engineered IMPDHs.

Interaction network among de novo purine nucleotide biosynthesis enzymes in Escherichia coli.

Discovery of Bis-Imidazoline Derivatives as New CXCR4 Ligands.

SigH stress response mediates killing of Mycobacterium tuberculosis by activating nitronaphthofuran prodrugs via induction of Mrx2 expression.

Steroid hormone catabolites activate the pyrin inflammasome through a non-canonical mechanism.

Discovery of bat coronaviruses close to SARS-CoV-2 and infectious for human cells.

Structural basis for the allosteric inhibition of UMP kinase from Gram-positive bacteria, a promising antibacterial target.

Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors.

Thesis Defense: “Biosynthèse des nucléotides puriques chez les bactéries : identification d’un métabolon et exploration de la régulation allostérique d’une enzyme-clé de la voie de novo, l’inosine 5’-monophosphate déshydrogénase” – ANTOINE GEDEON – vendredi 17 décembre

SARS-CoV-2 Nsp3 unique domain SUD interacts with guanine quadruplexes and G4-ligands inhibit this interaction.

2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F420)-Dependent Nitroreductase (Ddn).

Endeavors towards transformation of M. tuberculosis thymidylate kinase (MtbTMPK) inhibitors into potential antimycobacterial agents.

Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination.

Synthesis and structure activity relationships of cyanopyridone based anti-tuberculosis agents.

Replication of Equine arteritis virus is efficiently suppressed by purine and pyrimidine biosynthesis inhibitors.

1-(1-Arylethylpiperidin-4-yl)thymine Analogs as Antimycobacterial TMPK Inhibitors.

A real-time cell-binding assay reveals dynamic features of STxB-Gb3 cointernalization and STxB-mediated cargo delivery into cancer cells.

1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase.

First-in-class allosteric inhibitors of bacterial IMPDHs

Screening and evaluation of antiviral compounds against Equid alpha-herpesviruses using an impedance-based cellular assay

A Novel Polyaminocarboxylate Compound To Treat Murine Pulmonary Aspergillosis by Interfering with Zinc Metabolism

Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors

Identification of novel leishmanicidal molecules by virtual and biochemical screenings targeting Leishmania eukaryotic translation initiation factor 4A

Synthesis of sulfamide analogues of deoxthymidine monophosphate as potential inhibitors of mycobacterial cell wall biosynthesis

Inhibition of the inflammatory response to stress by targeting interaction between PKR and its cellular activator PACT

Nitazoxanide Analogs Require Nitroreduction for Antimicrobial Activity in Mycobacterium smegmatis

Original chemical series of pyrimidine biosynthesis inhibitors that boost the antiviral interferon response

Tetrahydro-2-furanyl-2,4(1H,3H)-pyrimidinedione derivatives as novel antibacterial compounds against Mycobacterium

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

Administration of zinc chelators improves survival of mice infected with Aspergillus fumigatus both in monotherapy and in combination with caspofungin.

Anti-mycobacterial activity of thymine derivatives bearing boron clusters

Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors

Synthesis and evaluation of original bioisosteres of bacterial type IIA topoisomerases inhibitors

AEGIS (Accelerated Early staGe drug dIScovery)

Interferon induction, inflammation and stress in HCV infection and stress-related pathologies

Workshop on protein-protein interactions: from low to high-throughput investigations

FP7 Targeting the Leishmania kinome for the development of novel anti-parasitic strategies (LeishDrug)

Inhibitors of Pseudomonas aeruginosa IMPDH

Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation

Inhibitors of TMPK from Mycobacterium tuberculosis

ATPase inhibitors, the cases of human heat shock protein 90 and bacterial type IIA topoisomerases

Alkoxypyrazoles, inhibitors of dihydroorotate dehydrogenase (DHODH)

Inosine-5′-monophosphate dehydrogenase

Nucleoside monophosphate kinases (NMPKs)

Group: Biochemistry and chemobiology

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH)

High-throughput screening for broad-spectrum chemical inhibitors of RNA viruses

Inhibition of pyrimidine biosynthesis pathway suppresses viral growth through innate immunity

AutomiG, a biosensor to detect alterations in miRNA biogenesis and in small RNA silencing guided by perfect target complementarity

On dihydroorotate dehydrogenases and their inhibitors and uses

Synergy of the antibiotic colistin with echinocandin antifungals in Candida species

Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors

A phenotypic assay to identify Chikungunya virus inhibitors targeting the nonstructural protein nsP2

The composition of the culture medium influences the β-1,3-glucan metabolism of Aspergillus fumigatus and the antifungal activity of inhibitors of β-1,3-glucan synthesis

Synthesis and evaluation of 6-aza-2′-deoxyuridine monophosphate analogs as inhibitors of thymidylate synthases, and as substrates or inhibitors of thymidine monophosphate kinase in Mycobacterium tuberculosis

Drug design and identification of potent leads against mycobacterium tuberculosis thymidine monophosphate kinase

Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase

Structural and functional characterization of the Mycobacterium tuberculosis uridine monophosphate kinase: insights into the allosteric regulation

Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone

Phosphorylation of dGMP analogs by vaccinia virus TMP kinase and human GMP kinase

Metalloprotease vsm is the major determinant of toxicity for extracellular products of Vibrio splendidus

Exploring acyclic nucleoside analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity

Acyclic phosphonate nucleotides and human adenylate kinases: impact of a borano group on alpha-P position

Rational design of 5′-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth

Structural and functional consequences of single amino acid substitutions in the pyrimidine base binding pocket of Escherichia coli CMP kinase

A new family of inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

Synthesis and biological evaluation of bicyclic nucleosides as inhibitors of M. tuberculosis thymidylate kinase

Multiple microfermentor battery: a versatile tool for use with automated parallel cultures of microorganisms producing recombinant proteins and for optimization of cultivation protocols

The crystal structure of Mycobacterium tuberculosis adenylate kinase in complex with two molecules of ADP and Mg2+ supports an associative mechanism for phosphoryl transfer.

Unique GMP-binding site in Mycobacterium tuberculosis guanosine monophosphate kinase

LEA3D: a computer-aided ligand design for structure-based drug design

The crystal structure of Mycobacterium tuberculosis thymidylate kinase in complex with 3′-azidodeoxythymidine monophosphate suggests a mechanism for competitive inhibition

Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase