Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development
Antonio Cavazzuti Giuseppe Paglietti William N. Hunter Francisco Gamarro Sandra Piras Mario Loriga Sergio Alleca Paola Corona Karen McLuskey Lindsay Tulloch Federica Gibellini Stefania Ferrari Maria Paola Costin
Lindsay Tulloch
Tulloch Lindsay
ORCID: 0000-0001-7223-5106
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Maria Paola Costi
Costi Maria Paola
ORCID: 0000-0002-0443-5402
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Francisco Gamarro
Gamarro Francisco
ORCID: 0000-0003-1347-3440
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Correlation between the affinity of flavonoids binding to the cytosolic site of Leishmania tropica multidrug transporter and their efficiency to revert parasite resistance to daunomycin. 10.1021/bi982455v
Involvement of thiol metabolism in resistance to glucantime in Leishmania tropica. 10.1016/s0006-2952(98)00129-4
A new member of YER057c family in Trypanosoma cruzi is adjacent to an ABC-transporter. 10.1016/s0378-1119(98)00439-9
Altered drug membrane permeability in a multidrug-resistant Leishmania tropica line. 10.1016/s0006-2952(97)00385-7
A pteridine reductase gene ptr1 contiguous to a P-glycoprotein confers resistance to antifolates in Trypanosoma cruzi. 10.1016/s0166-6851(97)00207-7
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Purification of a glycoprotein excreted by Trypanosoma cruzi to increase the permeability of the host-cell membrane. 10.1016/0006-291x(90)90871-j
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Purification of metacyclic forms of Trypanosoma cruzi by Percoll discontinuous gradient centrifugation. 10.1007/bf00926684
Karen McLuskey
McLuskey Karen
ORCID: 0000-0002-9841-4943
PNT1 Is a C11 Cysteine Peptidase Essential for Replication of the Trypanosome Kinetoplast 10.1074/jbc.M116.714972
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Crystal structures of all-alpha type membrane proteins. 10.1007/s00249-009-0546-6
Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development. 10.1073/pnas.0704384105
Crystallization and preliminary x-ray crystallographic analysis of the B800-820 light-harvesting complex from Rhodopseudomonas acidophila strain 7050. 10.1107/s0907444998016059
Comparative structural analysis of the caspase family with other clan CD cysteine peptidases. 10.1042/bj20141324
Purification, characterization, and crystallization of Trypanosoma metacaspases. 10.1007/978-1-4939-0357-3_13
Substrate specificity and the effect of calcium on Trypanosoma brucei metacaspase 2. 10.1111/febs.12248
Crystal structure of a Trypanosoma brucei metacaspase. 10.1073/pnas.1200885109
Oligopeptidase B deficient mutants of Leishmania major. 10.1016/j.molbiopara.2010.09.003
The crystal structure of the periplasmic domain of the type II secretion system protein EpsM from Vibrio cholerae: the simplest version of the ferredoxin fold. 10.1016/j.jmb.2004.01.064
Crystal structure of Leishmania major oligopeptidase B gives insight into the enzymatic properties of a trypanosomatid virulence factor. 10.1074/jbc.m110.156679
Initiating a crystallographic analysis of recombinant (S)-2-hydroxypropylphosphonic acid epoxidase from Streptomyces wedmorensis. 10.1107/s1744309105012376
Insight into the role of Escherichia coli MobB in molybdenum cofactor biosynthesis based on the high resolution crystal structure. 10.1074/jbc.m301485200
Structure and reactivity of hydroxypropylphosphonic acid epoxidase in fosfomycin biosynthesis by a cation- and flavin-dependent mechanism. 10.1073/pnas.0504314102
A protocol for high throughput methods for the expression and purification of inner membrane proteins. 10.1080/09687680802510289
High-throughput identification of purification conditions leads to preliminary crystallization conditions for three inner membrane proteins. 10.3109/09687688.2011.628954
High-throughput methods for the detection of protein overexpression using fluorescence markers. 10.1016/b978-0-12-407239-8.00010-0
Structure and reactivity of Trypanosoma brucei pteridine reductase: inhibition by the archetypal antifolate methotrexate. 10.1111/j.1365-2958.2006.05332.x
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Structural factors which control the position of the Qy absorption band of bacteriochlorophyll a in purple bacterial antenna complexes 10.1023/a:1020995224156
Inhibition ofLeishmania majorpteridine reductase by 2,4,6-triaminoquinazoline: structure of the NADPH ternary complex 10.1107/s0907444904018955
Ranking Metabolite Sets by Their Activity Levels 10.3390/metabo11020103
The crystallographic structure of the B800-820 LH3 light-harvesting complex from the purple bacteria Rhodopseudomonas acidophila strain 7050. 10.1021/bi010309a
Stefania Ferrari
Ferrari Stefania
ORCID: 0000-0003-1149-5953
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells 10.1021/jm501397h
2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes 10.1016/j.ejmech.2014.01.048
Optimization of peptides that target human thymidylate synthase to inhibit ovarian cancer cell growth 10.1021/jm401574p
2′-deoxyuridine 5′-monophosphate substrate displacement in thymidylate synthase through 6-Hydroxy-2 H -naphtho[1,8- bc ]furan-2-one derivatives 10.1021/jm4014086
Modulation of the expression of folate cycle enzymes and polyamine metabolism by berberine in cisplatin-sensitive and-resistant human ovarian cancer cells 10.3892/ijo.2013.2045
Targeting the Trypanosomatidic Enzymes Pteridine Reductase and Dihydrofolate Reductase 10.1002/9783527670383.ch24
Biochemical effects of riluzole on Leishmania parasites 10.1016/j.exppara.2012.11.013
Ligand-based discovery of N-(1,3-dioxo-1H,3H-benzo[de]isochromen-5-yl)- carboxamide and sulfonamide derivatives as thymidylate synthase A inhibitors 10.1016/j.bmcl.2012.11.117
Inhibitor of ovarian cancer cells growth by virtual screening: A new thiazole derivative targeting human thymidylate synthase 10.1021/jm300850v
Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors 10.1021/jm300563f
The structure of Enterococcus faecalis thymidylate synthase provides clues about folate bacterial metabolism 10.1107/S0907444912026236
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Protein-protein interface-binding peptides inhibit the cancer therapy target human thymidylate synthase 10.1073/pnas.1104829108
Identification of the binding modes of N-phenylphthalimides inhibiting bacterial thymidylate synthase through X-ray crystallography screening 10.1021/jm2005018
Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase 10.1021/jm1010572
Dimer-monomer equilibrium of human thymidylate synthase monitored by fluorescence resonance energy transfer 10.1002/pro.379
Homodimeric enzymes as drug targets 10.2174/092986710790712156
Design and characterization of a mutation outside the active site of human thymidylate synthase that affects ligand binding 10.1093/protein/gzp075
Anchors away 10.1038/458840a
Constrained dansyl derivatives reveal bacterial specificity of high conserved thymidylate synthases 10.1002/cbic.200700524
Sequence-based identification of specific drug target regions in the thymidylate synthase enzyme family 10.1002/cmdc.200700215
Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development 10.1073/pnas.0704384105
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 10.1016/j.ejmech.2007.03.035
Antibacterial agent discovery using thymidylate synthase biolibrary screening 10.1021/jm051187d
Novel 3-benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents 10.1002/jhet.5570430304
The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition 10.1107/S0907444905022638
Thymidylate synthase structure, function and implication in drug discovery 10.2174/0929867054864868
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine 10.1021/jm0491445
Aza-boronic acids as non-β-lactam inhibitors of AmpC-β-lactamase 10.1016/j.bmcl.2004.05.054
Inhibitor Specificity via Protein Dynamics: Insights from the Design of Antibacterial Agents Targeted Against Thymidylate Synthase 10.1016/j.chembiol.2003.11.012
Update on antifolate drugs targets 10.2174/1389450013348669
Hotspots in an obligate homodimeric anticancer target. Structural and functional effects of interfacial mutations in human thymidylate synthase 10.1021/acs.jmedchem.5b00137
Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case 10.1002/cmdc.201600121
X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors 10.1016/j.ejmech.2016.07.066
Inside the biochemical pathways of thymidylate synthase perturbed by anticancer drugs: Novel strategies to overcome cancer chemoresistance 10.1016/j.drup.2015.10.003
2-carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1 10.1021/cb5007163
The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment 10.1021/jm501615v
Protein-protein interaction inhibitors: Case studies on small molecules and natural compounds 10.1007/978-3-642-37999-4_2
Profiling of flavonol derivatives for the development of antitrypanosomatidic drugs 10.1021/acs.jmedchem.6b00698
Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity 10.3390/molecules22030426
Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth 10.1021/acs.jmedchem.7b01699
SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-Trypanosoma brucei Agent 10.1021/acsmedchemlett.8b00565
Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors 10.3390/molecules24071362