47 results on '"Hol, Wim G. J."'
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2. From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis
3. Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis
4. 5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors
5. SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1
6. Potent and Selective Inhibitors of CDPK1 from T. gondii and C. parvum Based on a 5-Aminopyrazole-4-carboxamide Scaffold
7. Urea-Based Inhibitors of Trypanosoma brucei Methionyl-tRNA Synthetase: Selectivity and in Vivo Characterization
8. Multiple Determinants for Selective Inhibition of Apicomplexan Calcium-Dependent Protein Kinase CDPK1
9. Crystal Structures, Metal Activation, and DNA-Binding Properties of Two-Domain IdeR from Mycobacterium tuberculosis,
10. Using Fragment Cocktail Crystallography To Assist Inhibitor Design of Trypanosoma brucei Nucleoside 2-Deoxyribosyltransferase
11. Protein Heterodimerization through Ligand-Bridged Multivalent Pre-organization: Enhancing Ligand Binding toward Both Protein Targets
12. Large Cyclic Peptides as Cores of Multivalent Ligands: Application to Inhibitors of Receptor Binding by Cholera Toxin
13. Solution- and Solid-Phase Syntheses of Guanidine-Bridged, Water-Soluble Linkers for Multivalent Ligand Design
14. Crystal Structures of an Intrinsically Active Cholera Toxin Mutant Yield Insight into the Toxin Activation Mechanism,
15. Explorations of Peptide and Oligonucleotide Binding Sites of Tyrosyl-DNA Phosphodiesterase Using Vanadate Complexes
16. Structures of Enterococcal Glycerol Kinase in the Absence and Presence of Glycerol: Correlation of Conformation to Substrate Binding and a Mechanism of Activation by Phosphorylation
17. Analysis of the Sequence Motifs Responsible for the Interactions of Peroxins 14 and 5, Which Are Involved in Glycosome Biogenesis in Trypanosoma brucei
18. Structure-Based Design of a Macrocyclic Inhibitor for Peptide Deformylase
19. Solution and Crystallographic Studies of Branched Multivalent Ligands that Inhibit the Receptor-Binding of Cholera Toxin
20. Characterization and Crystal Structure of a High-Affinity Pentavalent Receptor-Binding Inhibitor for Cholera Toxin and E. coli Heat-Labile Enterotoxin
21. Adenosine Analogues as Selective Inhibitors of Glyceraldehyde-3-phosphate Dehydrogenase of Trypanosomatidae via Structure-Based Drug Design
22. Solid-Phase Synthesis of N-Acyl-N‘-Alkyl/Aryl Disubstituted Guanidines
23. Adenosine Analogues as Inhibitors of Trypanosoma brucei Phosphoglycerate Kinase: Elucidation of a Novel Binding Mode for a 2-Amino-N6-Substituted Adenosine
24. Novel Insights into Catalytic Mechanism from a Crystal Structure of Human Topoisomerase I in Complex with DNA
25. High-Affinity Pentavalent Ligands of Escherichia coli Heat-Labile Enterotoxin by Modular Structure-Based Design
26. The Role of Waters in Docking Strategies with Incremental Flexibility for Carbohydrate Derivatives: Heat-Labile Enterotoxin, a Multivalent Test Case
27. Structure-Based Exploration of the Ganglioside GM1 Binding Sites ofEscherichia coliHeat-Labile Enterotoxin and Cholera Toxin for the Discovery of Receptor Antagonists
28. Selective Tight Binding Inhibitors of Trypanosomal Glyceraldehyde-3-phosphate Dehydrogenase via Structure-Based Drug Design
29. Crystal Structure of Fructose-1,6-bisphosphate Aldolase from the Human Malaria Parasite Plasmodium falciparum,
30. Crystal Structures of Substrates and Products Bound to the Phosphoglycerate Kinase Active Site Reveal the Catalytic Mechanism
31. Structure of the Native Cysteine-Sulfenic Acid Redox Center of Enterococcal NADH Peroxidase Refined at 2.8 Å Resolution,
32. Stabilization of Human Triosephosphate Isomerase by Improvement of the Stability of Individual α-Helices in Dimeric as well as Monomeric Forms of the Protein
33. High-Resolution Structure of the Diphtheria Toxin Repressor Complexed with Cobalt and Manganese Reveals an SH3-like Third Domain and Suggests a Possible Role of Phosphate as Co-corepressor,
34. Crystal Structure of Glycosomal Glyceraldehyde-3-phosphate Dehydrogenase from Leishmania mexicana: Implications for Structure-Based Drug Design and a New Position for the Inorganic Phosphate Binding Site
35. The Arg7Lys Mutant of Heat-Labile Enterotoxin Exhibits Great Flexibility of Active Site Loop 47-56 of the A Subunit
36. Synthesis and Structure-Activity Relationships of Analogs of 2'-Deoxy-2'-(3-methoxybenzamido)adenosine, a Selective Inhibitor of Trypanosomal Glycosomal Glyceraldehyde-3-phosphate Dehydrogenase
37. Crystallographic Analyses of NADH Peroxidase Cys42Ala and Cys42Ser Mutants: Active Site Structures, Mechanistic Implications, and an Unusual Environment of Arg 303
38. An L40C Mutation Converts the Cysteine-Sulfenic Acid Redox Center in Enterococcal NADH Peroxidase to a Disulfide
39. Crystallographic and Enzymic Investigations on the Role of Ser558, His610, and Asn614 in the Catalytic Mechanism of Azotobacter vinelandii Dihydrolipoamide Acetyltransferase (E2p)
40. Selective Inhibition of Trypanosomal Glyceraldehyde-3-phosphate Dehydrogenase by Protein Structure-Based Design: Toward New Drugs for the Treatment of Sleeping Sickness
41. Crystal Structures of Wild-Type p-Hydroxybenzoate Hydroxylase Complexed with 4-Aminobenzoate, 2,4-Dihydroxybenzoate, and 2-Hydroxy-4-aminobenzoate and of the Tyr222Ala Mutant Complexed with 2-Hydroxy-4-aminobenzoate. Evidence for a Proton Channel and a New Binding Mode of the Flavin Ring
42. Comparison of the B-pentamers of heat-labile enterotoxin and verotoxin-1: two structures with remarkable similarity and dissimilarity
43. Active site structure of methylamine dehydrogenase: hydrazines identify C6 as the reactive site of the tryptophan-derived quinone cofactor
44. Crystallographic and molecular modeling studies on trypanosomal triosephosphate isomerase: a critical assessment of the predicted and observed structures of the complex with 2-phosphoglycerate
45. Analysis of the active site of the flavoprotein p-hydroxybenzoate hydroxylase and some ideas with respect to its reaction mechanism
46. Interaction of pyrophosphate moieties with .alpha.-helixes in dinucleotide-binding proteins
47. The coenzyme analog adenosine 5-diphosphoribose displaces FAD in the active site of p-hydroxybenzoate hydroxylase. An x-ray crystallographic investigation
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