List of works - Lari Lehtiö

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors

scientific article

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10

scientific article published on 20 June 2018

A Trimetal Site and Substrate Distortion in a Family II Inorganic Pyrophosphatase

scientific article published in Journal of Biological Chemistry

Activity-Based Screening Assay for Mono-ADP-Ribosylhydrolases

scientific article published on 12 June 2020

Activity-based assay for human mono-ADP-ribosyltransferases ARTD7/PARP15 and ARTD10/PARP10 aimed at screening and profiling inhibitors.

scientific article published on 26 February 2013

Adenosine analogs bearing phosphate isosteres as human MDO1 ligands

scientific article published on 13 February 2018

An Evolutionary Perspective on the Origin, Conservation and Binding Partner Acquisition of Tankyrases

scientific article published in 2022

Characterization of the DNA dependent activation of human ARTD2/PARP2.

scientific article

Comparative structural analysis of lipid binding START domains

scientific article published in 2011

Completing the family portrait of the anti-apoptotic Bcl-2 proteins: crystal structure of human Bfl-1 in complex with Bim

scientific article

Crystal Structures of the ATPase Domains of Four Human Hsp70 Isoforms: HSPA1L/Hsp70-hom, HSPA2/Hsp70-2, HSPA6/Hsp70B', and HSPA5/BiP/GRP78

scientific article

Crystal structure of a glycyl radical enzyme from Archaeoglobus fulgidus

scientific article published on 3 January 2006

Crystal structure of the N-terminal NC4 domain of collagen IX, a zinc binding member of the laminin-neurexin-sex hormone binding globulin (LNS) domain family

scientific article

Crystallization and preliminary crystallographic analysis of two Streptococcus agalactiae proteins: the family II inorganic pyrophosphatase and the serine/threonine phosphatase

scientific article published on 11 August 2006

Development and structural analysis of adenosine site binding tankyrase inhibitors

scientific article

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

scientific article published on 08 December 2021

Development of an Inhibitor Screening Assay for Mono-ADP-Ribosyl Hydrolyzing Macrodomains Using AlphaScreen Technology

article

Discovery of Compounds Inhibiting the ADP-Ribosyltransferase Activity of Pertussis Toxin

scientific article published on 13 January 2020

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

scientific article published on 20 November 2017

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics

scientific article

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity

scientific article

Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei

scientific article published on 23 March 2016

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

scientific article published on 07 January 2019

Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors

scientific article

Exploration of the nicotinamide-binding site of the tankyrases, identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro

scientific article

FMN-dependent oligomerization of putative lactate oxidase from Pediococcus acidilactici

scientific article published on 24 February 2020

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.

scientific article published on 16 December 2016

Homogeneous screening assay for human tankyrase.

scientific article

Inhibition of poly(ADP-ribose) polymerase interferes with Trypanosoma cruzi infection and proliferation of the parasite

scientific article published in 2012

Inhibitor screening assay for neurexin-LRRTM adhesion protein interaction involved in synaptic maintenance and neurological disorders

scientific article published on 28 September 2019

Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules

scientific article published in 2022

Multiple crystal forms of human MacroD2

scientific article published on 15 September 2020

Oligomerization mediated by the D2 domain of DTX3L is critical for DTX3L‐PARP9 reading function of mono‐ADP‐ribosylated androgen receptor

scientific article published in 2024

PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA

scientific article

PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA.: FIGURE 2

scientific article published in Journal of Biological Chemistry

Proximal ADP-ribose Hydrolysis in Trypanosomatids is Catalyzed by a Macrodomain

scientific article published on 11 April 2016

Screening and structural analysis of flavones inhibiting tankyrases

scientific article

Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.

scientific article published on 22 September 2016

Small-Molecule Screening Assay for Mono-ADP-Ribosyltransferases

scientific article published on 01 January 2018

Structural Basis for Regulation of the Human Acetyl-CoA Thioesterase 12 and Interactions with the Steroidogenic Acute Regulatory Protein-related Lipid Transfer (START) Domain

scientific article

Structural Determination of Functional Domains in Early B-cell Factor (EBF) Family of Transcription Factors Reveals Similarities to Rel DNA-binding Proteins and a Novel Dimerization Motif

scientific article

Structural and Biochemical Characterization of Poly-ADP-ribose Polymerase from Trypanosoma brucei

scientific article published on 16 June 2017

Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4

scientific article

Structural basis for DNA break recognition by ARTD2/PARP2

article

Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3

scientific article

Structural basis of selective inhibition of human tankyrases

scientific article

Structural studies of metal ions in family II pyrophosphatases: the requirement for a Janus ion.

scientific article

Structural studies of tri-functional human GART

scientific article

Structure and function of the 3-carboxy-cis,cis-muconate lactonizing enzyme from the protocatechuate degradative pathway of Agrobacterium radiobacter S2.

scientific article

Structure of Escherichia coli pyruvate formate-lyase with pyruvate

scientific article

Structure of Streptococcus agalactiae serine/threonine phosphatase

scientific article

Structure of theStreptococcus agalactiaefamily II inorganic pyrophosphatase at 2.80 Å resolution

scientific article

Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases

scientific article

Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases

scientific article

Substrate specificity and oligomerization of human GMP synthetase

scientific article

Tankyrases as drug targets

scientific article published on 18 June 2013

Tankyrases: structure, function and therapeutic implications in cancer

scientific article published on January 2014

The DEXD/H-box RNA Helicase DDX19 Is Regulated by an -Helical Switch

scientific article

The crystal structure of the Dachshund domain of human SnoN reveals flexibility in the putative protein interaction surface

scientific article

The pyruvate formate lyase family: sequences, structures and activation

scientific article

The structure ofPseudomonasP51 Cl-muconate lactonizing enzyme: Co-evolution of structure and dynamics with the dehalogenation function ⬇️

scientific article published in September 2003

The zinc-binding motif in tankyrases is required for the structural integrity of the catalytic ADP-ribosyltransferase domain

scientific article published on 23 March 2022

Unusual twinning in an acetyl coenzyme A synthetase (ADP-forming) from Pyrococcus furiosus

scientific article published on 24 February 2005

Zinc binding catalytic domain of human tankyrase 1

scientific article

para-Substituted 2-phenyl-3,4-dihydroquinazolin-4-ones as potent and selective tankyrase inhibitors

scientific article

List of works by Lari Lehtiö

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10

A Trimetal Site and Substrate Distortion in a Family II Inorganic Pyrophosphatase

Activity-Based Screening Assay for Mono-ADP-Ribosylhydrolases

Activity-based assay for human mono-ADP-ribosyltransferases ARTD7/PARP15 and ARTD10/PARP10 aimed at screening and profiling inhibitors.

Adenosine analogs bearing phosphate isosteres as human MDO1 ligands

An Evolutionary Perspective on the Origin, Conservation and Binding Partner Acquisition of Tankyrases

Characterization of the DNA dependent activation of human ARTD2/PARP2.

Comparative structural analysis of lipid binding START domains

Completing the family portrait of the anti-apoptotic Bcl-2 proteins: crystal structure of human Bfl-1 in complex with Bim

Crystal Structures of the ATPase Domains of Four Human Hsp70 Isoforms: HSPA1L/Hsp70-hom, HSPA2/Hsp70-2, HSPA6/Hsp70B', and HSPA5/BiP/GRP78

Crystal structure of a glycyl radical enzyme from Archaeoglobus fulgidus

Crystal structure of the N-terminal NC4 domain of collagen IX, a zinc binding member of the laminin-neurexin-sex hormone binding globulin (LNS) domain family

Crystallization and preliminary crystallographic analysis of two Streptococcus agalactiae proteins: the family II inorganic pyrophosphatase and the serine/threonine phosphatase

Development and structural analysis of adenosine site binding tankyrase inhibitors

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

Development of an Inhibitor Screening Assay for Mono-ADP-Ribosyl Hydrolyzing Macrodomains Using AlphaScreen Technology

Discovery of Compounds Inhibiting the ADP-Ribosyltransferase Activity of Pertussis Toxin

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity

Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors

Exploration of the nicotinamide-binding site of the tankyrases, identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro

FMN-dependent oligomerization of putative lactate oxidase from Pediococcus acidilactici

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.

Homogeneous screening assay for human tankyrase.

Inhibition of poly(ADP-ribose) polymerase interferes with Trypanosoma cruzi infection and proliferation of the parasite

Inhibitor screening assay for neurexin-LRRTM adhesion protein interaction involved in synaptic maintenance and neurological disorders

Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules

Multiple crystal forms of human MacroD2

Oligomerization mediated by the D2 domain of DTX3L is critical for DTX3L‐PARP9 reading function of mono‐ADP‐ribosylated androgen receptor

PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA

PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA.: FIGURE 2

Proximal ADP-ribose Hydrolysis in Trypanosomatids is Catalyzed by a Macrodomain

Screening and structural analysis of flavones inhibiting tankyrases

Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.

Small-Molecule Screening Assay for Mono-ADP-Ribosyltransferases

Structural Basis for Regulation of the Human Acetyl-CoA Thioesterase 12 and Interactions with the Steroidogenic Acute Regulatory Protein-related Lipid Transfer (START) Domain

Structural Determination of Functional Domains in Early B-cell Factor (EBF) Family of Transcription Factors Reveals Similarities to Rel DNA-binding Proteins and a Novel Dimerization Motif

Structural and Biochemical Characterization of Poly-ADP-ribose Polymerase from Trypanosoma brucei

Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4

Structural basis for DNA break recognition by ARTD2/PARP2

Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3

Structural basis of selective inhibition of human tankyrases

Structural studies of metal ions in family II pyrophosphatases: the requirement for a Janus ion.

Structural studies of tri-functional human GART

Structure and function of the 3-carboxy-cis,cis-muconate lactonizing enzyme from the protocatechuate degradative pathway of Agrobacterium radiobacter S2.

Structure of Escherichia coli pyruvate formate-lyase with pyruvate

Structure of Streptococcus agalactiae serine/threonine phosphatase

Structure of theStreptococcus agalactiaefamily II inorganic pyrophosphatase at 2.80 Å resolution

Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases

Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases

Substrate specificity and oligomerization of human GMP synthetase

Tankyrases as drug targets

Tankyrases: structure, function and therapeutic implications in cancer

The DEXD/H-box RNA Helicase DDX19 Is Regulated by an -Helical Switch

The crystal structure of the Dachshund domain of human SnoN reveals flexibility in the putative protein interaction surface

The pyruvate formate lyase family: sequences, structures and activation

The structure ofPseudomonasP51 Cl-muconate lactonizing enzyme: Co-evolution of structure and dynamics with the dehalogenation function ⬇️

The zinc-binding motif in tankyrases is required for the structural integrity of the catalytic ADP-ribosyltransferase domain

Unusual twinning in an acetyl coenzyme A synthetase (ADP-forming) from Pyrococcus furiosus

Zinc binding catalytic domain of human tankyrase 1

para-Substituted 2-phenyl-3,4-dihydroquinazolin-4-ones as potent and selective tankyrase inhibitors