All Stories

  1. Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future
  2. Unpacking boxes: identification of novel inhibitors of malaria parasite invasion
  3. Formation of the moving junction is the nexus for host cytoskeletal remodelling during Plasmodium falciparum invasion of human erythrocytes
  4. Genome-wide reconstruction of the intrinsic apoptosis pathway in Haemonchus contortus
  5. MK-7602: a potent multi-stage dual-targeting antimalarial
  6. Exploration and Characterization of the Antimalarial Activity of Pyrimidine‐2,4‐Diamines for which Resistance is Mediated by the ABCI3 Transporter
  7. Deconvolution of the On-Target Activity of Plasmepsin V Peptidomimetics in Plasmodium falciparum Parasites
  8. Characterizing the quick-killing mechanism of action of azithromycin analogs against malaria parasites
  9. Optimization and Characterization of the Antimalarial Activity of N-Aryl Acetamides that are Susceptible to Mutations in ROM8 and CSC1
  10. A review of natural products as a source of next-generation drugs against apicomplexan parasites
  11. Advances in Anthelmintic Target Identification
  12. Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4
  13. Prediction and Prioritisation of Novel Anthelmintic Candidates from Public Databases Using Deep Learning and Available Bioactivity Data Sets
  14. Structure–activity analysis of imino‐pyrimidinone‐fused pyrrolidines aids the development of dual plasmepsin V and plasmepsin X inhibitors
  15. Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b
  16. Lactam Truncation Yields a Dihydroquinazolinone Scaffold with Potent Antimalarial Activity that Targets PfATP4
  17. An adaptable, fit-for-purpose screening approach with high-throughput capability to determine speed of action and stage specificity of anti-malarial compounds
  18. Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3
  19. Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4
  20. Comparative structure activity and target exploration of 1,2-diphenylethynes in Haemonchus contortus and Caenorhabditis elegans
  21. Aryl amino acetamides prevent Plasmodium falciparum ring development via targeting the lipid-transfer protein PfSTART1
  22. Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein
  23. Structure-activity relationship and target investigation of 2-aryl quinolines with nematocidal activity
  24. A phenotypic screen of the Global Health Priority Box identifies an insecticide with anthelmintic activity
  25. BNC210, a negative allosteric modulator of the alpha 7 nicotinic acetylcholine receptor, demonstrates anxiolytic- and antidepressant-like effects in rodents
  26. Novel aroyl guanidine anti-trypanosomal compounds that exert opposing effects on parasite energy metabolism
  27. Structure activity relationship and target prediction for ABX464 analogues in Caenorhabditis elegans
  28. Sequence elements within the PEXEL motif and its downstream region modulate PTEX‐dependent protein export in Plasmodium falciparum
  29. A Pyridyl-Furan Series Developed from the Open Global Health Library Block Red Blood Cell Invasion and Protein Trafficking in Plasmodium falciparum through Potential Inhibition of the Parasite’s PI4KIIIB Enzyme
  30. Chemo‐proteomics in antimalarial target identification and engagement
  31. Sulfonylpiperazine compounds prevent Plasmodium falciparum invasion of red blood cells through interference with actin-1/profilin dynamics
  32. Sequence elements within the PEXEL motif and its downstream region modulate PTEX dependent protein export in Plasmodium falciparum .
  33. 7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc1 Complex
  34. Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4
  35. Design and characterization of a heterobifunctional degrader of KEAP1
  36. Targeting malaria parasites with novel derivatives of azithromycin
  37. Thermal proteome profiling reveals Haemonchus orphan protein HCO_011565 as a target of the nematocidal small molecule UMW-868
  38. The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria
  39. Australian chemistry and drug discovery towards the development of antimalarials
  40. Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity
  41. The Medicines for Malaria Venture Malaria Box contains inhibitors of protein secretion in Plasmodium falciparum blood stage parasites
  42. Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax
  43. A revised mechanism for how Plasmodium falciparum recruits and exports proteins into its erythrocytic host cell
  44. A High-Throughput Phenotypic Screen of the ‘Pandemic Response Box’ Identifies a Quinoline Derivative with Significant Anthelmintic Activity
  45. Optimization of Phosphotyrosine Peptides that Target the SH2 Domain of SOCS1 and Block Substrate Ubiquitination
  46. Hydroxychloroquine inhibits the mitochondrial antioxidant system in activated T cells
  47. Property activity refinement of 2-anilino 4-amino substituted quinazolines as antimalarials with fast acting asexual parasite activity
  48. Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity
  49. A revised mechanism for how Plasmodium falciparum recruits and exports proteins into its erythrocytic host cell
  50. High-Throughput Phenotypic Assay to Screen for Anthelmintic Activity on Haemonchus contortus
  51. Late Stage Phosphotyrosine Mimetic Functionalization of Peptides Employing Metallaphotoredox Catalysis
  52. Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity against Haemonchus contortus In Vitro
  53. Development of an automated assay for accelerated in vitro detection of DNA adduct-inducing and crosslinking agents
  54. Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion
  55. Optimization of Benzothiazole and Thiazole Hydrazones as Inhibitors of Schistosome BCL-2
  56. Advances in the discovery and development of anthelmintics by harnessing natural product scaffolds
  57. Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction
  58. Development and application of a high-throughput screening assay for identification of small molecule inhibitors of the P. falciparum reticulocyte binding-like homologue 5 protein
  59. Retargeting azithromycin analogues to have dual-modality antimalarial activity
  60. Optimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents
  61. Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro
  62. Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle
  63. Screening the Medicines for Malaria Venture Pathogen Box for invasion and egress inhibitors of the blood stage of Plasmodium falciparum reveals several inhibitory compounds
  64. Formaldehyde-activated WEHI-150 induces DNA interstrand crosslinks with unique structural features
  65. Inhibition of Plasmepsin V Activity Blocks Plasmodium falciparum Gametocytogenesis and Transmission to Mosquitoes
  66. Screening the Medicines for Malaria Venture Pathogen Box for invasion and egress inhibitors of the blood stage of Plasmodium falciparum reveals several inhibitory compounds
  67. The Development Process for Discovery and Clinical Advancement of Modern Antimalarials
  68. An appraisal of natural products active against parasitic nematodes of animals
  69. Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models
  70. Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria
  71. Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P 2 position of PEXEL peptidomimetics
  72. Conversion of Bim-BH3 from Activator to Inhibitor of Bak through Structure-Based Design
  73. Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery
  74. Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis
  75. Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity
  76. Analysis of Ca2 + mediated signaling regulating Toxoplasma infectivity reveals complex relationships between key molecules
  77. Exploration of the P 3 region of PEXEL peptidomimetics leads to a potent inhibitor of the Plasmodium protease, plasmepsin V
  78. Synthesis of amino heterocycle aspartyl protease inhibitors
  79. Reversible and formaldehyde-mediated covalent binding of a bis-amino mitoxantrone analogue to DNA
  80. Isolation and structural analysis of the covalent adduct formed between a bis-amino mitoxantrone analogue and DNA: a pathway to major–minor groove cross-linked adducts
  81. An aspartyl protease defines a novel pathway for export of Toxoplasma proteins into the host cell
  82. HIV-1 and Human PEG10 Frameshift Elements Are Functionally Distinct and Distinguished by Novel Small Molecule Modulators
  83. Mitoxantrone, More than Just Another Topoisomerase II Poison
  84. Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes
  85. Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum
  86. The effect of N-methylation on transition state mimetic inhibitors of the Plasmodium protease, plasmepsin V
  87. Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides
  88. Discovery of a Potent and Selective BCL-X L Inhibitor with in Vivo Activity
  89. Transition State Mimetics of the Plasmodium Export Element Are Potent Inhibitors of Plasmepsin V from P. falciparum and P. vivax
  90. Inhibition of Plasmepsin V Activity Demonstrates Its Essential Role in Protein Export, PfEMP1 Display, and Survival of Malaria Parasites
  91. Structure-Guided Rescaffolding of Selective Antagonists of BCL-X L
  92. Stereoselective Synthesis and Application of β-Amino Ketones
  93. Discovery of Potent and Selective Benzothiazole Hydrazone Inhibitors of Bcl-X L
  94. Diastereoselective synthesis of cyclic β2,3-amino acids utilizing 4-substituted-1,3-oxazinan-6-ones
  95. Structure-guided design of a selective BCL-XL inhibitor
  96. Synthesis of N-Cbz-Substituted β3-Amino Ketones Utilizing 4-Substituted 1,3-Oxazinan-6-ones
  97. A Mild Multistep Conversion of N-Protected α-Amino Acids into N-Protected β3-Amino Acids Utilizing the Nef Reaction
  98. Role of Plasmepsin V in Export of Diverse Protein Families from the Plasmodium falciparum Exportome
  99. Corrigendum to “Diastereoselective synthesis of highly functionalized β2,2,3-substituted amino acids from 4-substituted-1,3-oxazinan-6-ones” [Tetrahedron 68 (2012) 4745–4756]
  100. Diastereoselective synthesis of highly functionalized β2,2,3-substituted amino acids from 4-substituted-1,3-oxazinan-6-ones
  101. Corrigendum to “Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors” [Bioorg. Med. Chem. Lett. 21 (2011) 5992–5994]
  102. M2, a novel anthracenedione, elicits a potent DNA damage response that can be subverted through checkpoint kinase inhibition to generate mitotic catastrophe
  103. Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors
  104. Quinazoline Sulfonamides as Dual Binders of the Proteins B-Cell Lymphoma 2 and B-Cell Lymphoma Extra Long with Potent Proapoptotic Cell-Based Activity
  105. Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
  106. Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
  107. New Anthracenedione Derivatives with Improved Biological Activity by Virtue of Stable Drug−DNA Adduct Formation
  108. De Novo Synthesis of a Potent LIMK1 Inhibitor
  109. Recent Advances in Stereoselective Synthesis and Application of β-Amino Acids
  110. Conformational Changes in Bcl-2 Pro-survival Proteins Determine Their Capacity to Bind Ligands
  111. Studies of 2-Substituted 1,3-Oxazolidin-5-ones and 1,3-Oxazinan-6-ones as Precursors for the Synthesis ofN-Alkyl-β-Amino Acids
  112. Exploitation of the Arndt-Eistert Homologation of N-Methyl-�-Amino Acids for Concomitant Ester and N-Methyl Peptide Formation
  113. Diastereoselective Synthesis of α-Methyl and α-Hydroxy-β-Amino Acids via 4-Substituted-1,3-Oxazinan-6-ones
  114. Effective Methods for the Synthesis ofN-Methylβ-Amino Acids from All Twenty Commonα-Amino Acids Using 1,3-Oxazolidin-5-ones and 1,3-Oxazinan-6-ones
  115. Synthesis of New β-Amino Acids via 5-Oxazolidinones and the Arndt–Eistert Procedure