List of works - Maria Paola Costi

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1

scientific article

2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes

scientific article published on 30 January 2014

A Peptidic Thymidylate-Synthase Inhibitor Loaded on Pegylated Liposomes Enhances the Antitumour Effect of Chemotherapy Drugs in Human Ovarian Cancer Cells

scientific article published on 23 June 2020

A Primary Pulmonary Artery Chondrosarcoma Manifesting as Acute Pulmonary Embolism

scientific article published on 01 November 2012

A condensed thiadiazolo-pyrimidine as a new efficient fluorophore. Theoretical and experimental investigation of the electronic spectra and photophysics

Alanine mutants of the interface residues of human thymidylate synthase decode key features of the binding mode of allosteric anticancer peptides

scientific article

Antibacterial agent discovery using thymidylate synthase biolibrary screening.

scientific article

Asparagine 229 mutants of thymidylate synthase catalyze the methylation of 3-methyl-2'-deoxyuridine 5'-monophosphate.

scientific article published in April 1996

Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase.

scientific article

Biochemical effects of riluzole on Leishmania parasites

scientific article published on December 2012

Biochemistry: Anchors away

scientific article

Biological evaluation of MR36, a novel non-polyglutamatable thymidylate synthase inhibitor that blocks cell cycle progression in melanoma cell lines

scientific article

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.

scientific article published on 8 March 2017

Collateral sensitivity to novel thymidylate synthase inhibitors correlates with folate cycle enzymes impairment in cisplatin-resistant human ovarian cancer cells

scientific article

Combination of suboptimal doses of inhibitors targeting different domains of LtrMDR1 efficiently overcomes resistance of Leishmania spp. to Miltefosine by inhibiting drug efflux

scientific article

Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case.

scientific article published on 12 July 2016

Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth

scientific article published on 13 August 2018

Conformational analysis of phthalein derivatives acting as thymidylate synthase inhibitors by means of 1H NMR and quantum chemical calculations

scientific article published on 01 October 1996

Constrained dansyl derivatives reveal bacterial specificity of highly conserved thymidylate synthases

scientific article published in March 2008

Corrigendum to “Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction” [J. Mol. Struct. (Theochem) 343 (1995) 1–9]

article

Cyclic Peptides Acting as Allosteric Inhibitors of Human Thymidylate Synthase and Cancer Cell Growth

scientific article published on 26 September 2019

Design and characterization of a mutation outside the active site of human thymidylate synthase that affects ligand binding.

scientific article published on 2 December 2009

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology

scientific article published on 19 February 2020

Dimer-monomer equilibrium of human thymidylate synthase monitored by fluorescence resonance energy transfer

scientific article

Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity

scientific article

Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development

scientific article

Distamycin A and derivatives as synergic drugs in cisplatin-sensitive and -resistant ovarian cancer cells

scientific article

Drug resistance in ovarian cancer: Biomarkers and treatments

scientific article published in May 2010

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections

scientific article published on 09 April 2019

Erratum

scholarly article by M. Paola Costi published May 1998 in Medicinal Research Reviews

Excited-state intramolecular proton transfer in a bioactive flavonoid provides fluorescence observables for recognizing its engagement with target proteins

scientific article published on 22 March 2019

Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting

scientific article published on 12 March 2021

High-resolution crystal structure of Trypanosoma brucei pteridine reductase 1 in complex with an innovative tricyclic-based inhibitor

scientific article published on 29 May 2020

Homodimeric enzymes as drug targets.

scientific article published on January 2010

Hotspots in an obligate homodimeric anticancer target. Structural and functional effects of interfacial mutations in human thymidylate synthase.

scientific article published on April 2015

Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine

scientific article published in February 2005

Inhibitor of ovarian cancer cells growth by virtual screening: a new thiazole derivative targeting human thymidylate synthase

scientific article

Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase

scientific article

Internalization and Stability of a Thymidylate Synthase Peptide Inhibitor in Ovarian Cancer Cells

article published in 2014

Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors

scientific article published on October 2010

Mass spectrometric/bioinformatic identification of a protein subset that characterizes the cellular activity of anticancer peptides

scientific article published on 29 September 2014

Modulation of the expression of folate cycle enzymes and polyamine metabolism by berberine in cisplatin-sensitive and -resistant human ovarian cancer cells.

scientific article published on 31 July 2013

Naphthalimido derivatives as antifolate thymidylate synthase inhibitors

New Insights into Bioactive Compounds from the Medicinal Plant Spathodea campanulata P. Beauv. and Their Activity against Helicobacter pylori

scientific article published on 15 May 2020

New thymidylate synthase inhibitors induce apoptosis in melanoma cell lines

scientific article published on 6 October 2006

Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs.

scientific article published on September 2010

Opening Opportunities for New Drugs Against Neglected Diseases

scientific article published on 01 March 2008

Optimization of peptides that target human thymidylate synthase to inhibit ovarian cancer cell growth

scientific article published on 12 February 2014

Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy

scientific article

Permeation through the cell membrane of a boron-based β-lactamase inhibitor

scientific article

Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition

scientific article

Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase

scientific article

Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase1,21Escherichia coli thymidylate synthase numbering is used unless otherwise noted.2PDB coordinates have been deposited with the RCSB wi

article published in 2001

Protein-protein interface-binding peptides inhibit the cancer therapy target human thymidylate synthase

scientific article

Quinoxaline chemistry. Part 11. 3-Phenyl-2 [phenoxy- and phenoxymethyl]-6(7) or 6,8-substituted quinoxalines and N-[4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl]benzoylglutamates. Synthesis and evaluation

scientific article published on 01 July 1998

Quinoxaline chemistry. Part 15. 4-[2-Quinoxalylmethylenimino]-benzoylglutamates and -benzoates, 4-[2-quinoxalylmethyl-N-methylamino]-benzoylglutamates as analogues of classical antifolate agents. Synthesis, elucidation of structures and in vitro eva

scientific article published in January 2003

Repurposing of Drugs Targeting YAP-TEAD Functions

article published in 2018

Sequence-based identification of specific drug target regions in the thymidylate synthase enzyme family

scientific article published on March 2008

Sesquiterpene Lactones with Dual Inhibitory Activity against the Trypanosoma brucei Pteridine Reductase 1 and Dihydrofolate Reductase

scientific article published on 28 December 2021

Spermidine/spermine N1-acetyltranferase modulation by novel folate cycle inhibitors in cisplatin-sensitive and -resistant human ovarian cancer cell lines

scientific article

Structural Comparison of Enterococcus faecalis and Human Thymidylate Synthase Complexes with the Substrate dUMP and Its Analogue FdUMP Provides Hints about Enzyme Conformational Variabilities

scientific article published on 31 March 2019

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors

scientific article published on 01 May 2019

Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors

article

Structural study of phenyl boronic acid derivatives as AmpC β-lactamase inhibitors

scientific article

Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase

scientific article

Structure-based design of inhibitors specific for bacterial thymidylate synthase

scientific article

Structure-based discovery and in-parallel optimization of novelcompetitive inhibitors of thymidylate synthase

scientific article published on 01 May 1999

Structure-based optimization of a non-beta-lactam lead results in inhibitors that do not up-regulate beta-lactamase expression in cell culture

scientific article published on April 2005

Structure-based studies on species-specific inhibition of thymidylate synthase

scientific article (publication date: 18 July 2002)

Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities

scientific article published on 18 April 2007

THEORETICAL STUDY OF ELECTRONIC SPECTRA AND PHOTOPHYSICS OF URACIL DERIVATIVES

scientific article published on 01 August 1990

Targeting Class A and C Serine β-Lactamases with a Broad-Spectrum Boronic Acid Derivative

scientific article

Targeting the Trypanosomatidic Enzymes Pteridine Reductase and Dihydrofolate Reductase

The 1,10-Phenanthroline Ligand Enhances the Antiproliferative Activity of DNA-Intercalating Thiourea-Pd(II) and -Pt(II) Complexes Against Cisplatin-Sensitive and -Resistant Human Ovarian Cancer Cell Lines ⬇️

scientific article published on 04 December 2019

The inhibition of extended spectrum β-lactamases: hits and leads

scientific article published on January 2014

The structural roles of conserved Pro196, Pro197 and His199 in the mechanism of thymidylate synthase

scientific article published in August 2003

The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition

scientific article published on 28 September 2005

The structure of Enterococcus faecalis thymidylate synthase provides clues about folate bacterial metabolism

scientific article

Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction

article

Thymidylate synthase structure, function and implication in drug discovery.

scientific article

Translational repression of thymidylate synthase by targeting its mRNA.

scientific article

Update on antifolate drugs targets

scientific article

ortho-Halogen naphthaleins as specific inhibitors of Lactobacillus casei thymidylate synthase. Conformational properties and biological activity

scientific article

List of works by Maria Paola Costi

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1

2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes

A Peptidic Thymidylate-Synthase Inhibitor Loaded on Pegylated Liposomes Enhances the Antitumour Effect of Chemotherapy Drugs in Human Ovarian Cancer Cells

A Primary Pulmonary Artery Chondrosarcoma Manifesting as Acute Pulmonary Embolism

A condensed thiadiazolo-pyrimidine as a new efficient fluorophore. Theoretical and experimental investigation of the electronic spectra and photophysics

Alanine mutants of the interface residues of human thymidylate synthase decode key features of the binding mode of allosteric anticancer peptides

Antibacterial agent discovery using thymidylate synthase biolibrary screening.

Asparagine 229 mutants of thymidylate synthase catalyze the methylation of 3-methyl-2'-deoxyuridine 5'-monophosphate.

Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase.

Biochemical effects of riluzole on Leishmania parasites

Biochemistry: Anchors away

Biological evaluation of MR36, a novel non-polyglutamatable thymidylate synthase inhibitor that blocks cell cycle progression in melanoma cell lines

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.

Collateral sensitivity to novel thymidylate synthase inhibitors correlates with folate cycle enzymes impairment in cisplatin-resistant human ovarian cancer cells

Combination of suboptimal doses of inhibitors targeting different domains of LtrMDR1 efficiently overcomes resistance of Leishmania spp. to Miltefosine by inhibiting drug efflux

Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case.

Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth

Conformational analysis of phthalein derivatives acting as thymidylate synthase inhibitors by means of 1H NMR and quantum chemical calculations

Constrained dansyl derivatives reveal bacterial specificity of highly conserved thymidylate synthases

Corrigendum to “Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction” [J. Mol. Struct. (Theochem) 343 (1995) 1–9]

Cyclic Peptides Acting as Allosteric Inhibitors of Human Thymidylate Synthase and Cancer Cell Growth

Design and characterization of a mutation outside the active site of human thymidylate synthase that affects ligand binding.

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology

Dimer-monomer equilibrium of human thymidylate synthase monitored by fluorescence resonance energy transfer

Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity

Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development

Distamycin A and derivatives as synergic drugs in cisplatin-sensitive and -resistant ovarian cancer cells

Drug resistance in ovarian cancer: Biomarkers and treatments

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections

Erratum

Excited-state intramolecular proton transfer in a bioactive flavonoid provides fluorescence observables for recognizing its engagement with target proteins

Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting

High-resolution crystal structure of Trypanosoma brucei pteridine reductase 1 in complex with an innovative tricyclic-based inhibitor

Homodimeric enzymes as drug targets.

Hotspots in an obligate homodimeric anticancer target. Structural and functional effects of interfacial mutations in human thymidylate synthase.

Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine

Inhibitor of ovarian cancer cells growth by virtual screening: a new thiazole derivative targeting human thymidylate synthase

Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase

Internalization and Stability of a Thymidylate Synthase Peptide Inhibitor in Ovarian Cancer Cells

Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors

Mass spectrometric/bioinformatic identification of a protein subset that characterizes the cellular activity of anticancer peptides

Modulation of the expression of folate cycle enzymes and polyamine metabolism by berberine in cisplatin-sensitive and -resistant human ovarian cancer cells.

Naphthalimido derivatives as antifolate thymidylate synthase inhibitors

New Insights into Bioactive Compounds from the Medicinal Plant Spathodea campanulata P. Beauv. and Their Activity against Helicobacter pylori

New thymidylate synthase inhibitors induce apoptosis in melanoma cell lines

Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs.

Opening Opportunities for New Drugs Against Neglected Diseases

Optimization of peptides that target human thymidylate synthase to inhibit ovarian cancer cell growth

Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy

Permeation through the cell membrane of a boron-based β-lactamase inhibitor

Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition

Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase

Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase1,21Escherichia coli thymidylate synthase numbering is used unless otherwise noted.2PDB coordinates have been deposited with the RCSB wi

Protein-protein interface-binding peptides inhibit the cancer therapy target human thymidylate synthase

Quinoxaline chemistry. Part 11. 3-Phenyl-2 [phenoxy- and phenoxymethyl]-6(7) or 6,8-substituted quinoxalines and N-[4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl]benzoylglutamates. Synthesis and evaluation

Quinoxaline chemistry. Part 15. 4-[2-Quinoxalylmethylenimino]-benzoylglutamates and -benzoates, 4-[2-quinoxalylmethyl-N-methylamino]-benzoylglutamates as analogues of classical antifolate agents. Synthesis, elucidation of structures and in vitro eva

Repurposing of Drugs Targeting YAP-TEAD Functions

Sequence-based identification of specific drug target regions in the thymidylate synthase enzyme family

Sesquiterpene Lactones with Dual Inhibitory Activity against the Trypanosoma brucei Pteridine Reductase 1 and Dihydrofolate Reductase

Spermidine/spermine N1-acetyltranferase modulation by novel folate cycle inhibitors in cisplatin-sensitive and -resistant human ovarian cancer cell lines

Structural Comparison of Enterococcus faecalis and Human Thymidylate Synthase Complexes with the Substrate dUMP and Its Analogue FdUMP Provides Hints about Enzyme Conformational Variabilities

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors

Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors

Structural study of phenyl boronic acid derivatives as AmpC β-lactamase inhibitors

Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase

Structure-based design of inhibitors specific for bacterial thymidylate synthase

Structure-based discovery and in-parallel optimization of novelcompetitive inhibitors of thymidylate synthase

Structure-based optimization of a non-beta-lactam lead results in inhibitors that do not up-regulate beta-lactamase expression in cell culture

Structure-based studies on species-specific inhibition of thymidylate synthase

Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities

THEORETICAL STUDY OF ELECTRONIC SPECTRA AND PHOTOPHYSICS OF URACIL DERIVATIVES

Targeting Class A and C Serine β-Lactamases with a Broad-Spectrum Boronic Acid Derivative

Targeting the Trypanosomatidic Enzymes Pteridine Reductase and Dihydrofolate Reductase

The 1,10-Phenanthroline Ligand Enhances the Antiproliferative Activity of DNA-Intercalating Thiourea-Pd(II) and -Pt(II) Complexes Against Cisplatin-Sensitive and -Resistant Human Ovarian Cancer Cell Lines ⬇️

The inhibition of extended spectrum β-lactamases: hits and leads

The structural roles of conserved Pro196, Pro197 and His199 in the mechanism of thymidylate synthase

The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition

The structure of Enterococcus faecalis thymidylate synthase provides clues about folate bacterial metabolism

Theoretical analysis of the addition of hydroxylamine to uracil and 5-fluorouracil as a model for the thymidylate synthase reaction