65 articles for thisTarget
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Article Title
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Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
University of Dundee
New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.
University of Dundee
Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity.
University of Dundee
Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities.
University of Dundee
Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.
University of Dundee
The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.
University of Dundee
Discovery ofβ2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
University of Dundee
Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase.
University of Dundee
Synthesis and evaluation ofa-thymidine analogues as novel antimalarials.
University of Dundee
Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase.
University of Dundee
Structure-based design of pteridine reductase inhibitors targeting African sleeping sickness and the leishmaniases.
University of Dundee
Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.
University of Dundee
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
University of Dundee
Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography.
University of Dundee
β-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.
University of Dundee
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
University of Dundee
Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds.
University of Dundee
Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif.
University of Dundee
Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase.
University of Dundee
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
University of Dundee
Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.
University of Dundee
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity.
University of Dundee
Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.
University of Dundee
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7.
University of Dundee
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
University of Dundee
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
University of Dundee
An efficient synthesis of argifin: a natural product chitinase inhibitor with chemotherapeutic potential.
University of Dundee
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
University of Dundee
Estimating the cooperativity of PROTAC-induced ternary complexes using
University of Dundee
Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins.
University of Dundee
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.
University of Dundee
Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1).
University of Dundee
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
University of Dundee
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent
University of Dundee
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.
University of Dundee
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.
University of Dundee
Drug discovery for neglected diseases: molecular target-based and phenotypic approaches.
University of Dundee
Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1.
University of Dundee
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.
University of Dundee
2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.
University of Dundee
Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.
University of Dundee
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.
University of Dundee
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrroli
University of Dundee
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.
University of Dundee
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
University of Dundee
Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.
University of Dundee
BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.
University of Dundee
5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
Galapagos
Quinazoline heterocyclic compound as EGFR kinase inhibitor and preparation and application thereof
Beijing Scitech-Mq Pharmaceuticals
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.
National Cancer Institute-Frederick
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.
Nagoya Institute of Technology
Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition.
University of North Carolina at Chapel Hill
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.
Nerviano Medical Sciences
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
Universidad Central De Venezuela
SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C.
Sphinx Laboratories