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Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.
A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3, and derivatives of this compound that contain an OH group at the 4' position of the phenyl ring may provide the new treatment strategies for the design of childhood treatment strategies.
Crystal Structure of Bruton's Tyrosine Kinase Domain Suggests a Novel Pathway for Activation and Provides Insights into the Molecular Basis of X-linked Agammaglobulinemia*
The x-ray crystal structure of the Bruton's tyrosine kinase kinase domain in its unphosphorylated state to a 2.1 Å resolution is determined and a comparison with the structures of other tyosine kinases is provided.
Expression of dominant-negative Ikaros isoforms in T-cell acute lymphoblastic leukemia.
  • L. Sun, M. Crotty, +10 authors F. Uckun
  • Biology, Medicine
    Clinical cancer research : an official journal of…
  • 1 August 1999
Children with T-ALL express high levels of dysfunctional dominant-negative Ikaros isoforms, including Ik-4, Ik-7, and Ik-8 that lack critical NH2-terminal zinc fingers.
Binding Interactions between the Active Center Cleft of Recombinant Pokeweed Antiviral Protein and the α-Sarcin/Ricin Stem Loop of Ribosomal RNA*
Experimental evidence is provided that besides the catalytic site, the active center cleft also participates in the binding of PAP to the target tetraloop structure of rRNA, providing experimental evidence that the residues of the activecenter cleft could, via electrostatic interactions, contribute to both the correct orientation and stable binding of the substrates in PAP active site pocket.
Spleen tyrosine kinase (Syk) deficiency in childhood pro-B cell acute lymphoblastic leukemia
These findings link for the first time specific molecular defects involving the Syk gene to an immunophenotypically distinct category of childhood ALL and are the first discovery of a specific tyrosine kinase deficiency in a human hematologic malignancy.
Active center cleft residues of pokeweed antiviral protein mediate its high-affinity binding to the ribosomal protein L3.
Unprecedented evidence is provided that the active center cleft of PAP is important for its in vitro binding to ribosomes via the L3 protein, which may account for their inability to efficiently inactivate ribosome.
Effect of stereochemistry on the anti-HIV activity of chiral thiourea compounds.
Experimental evidence is provided that the stereochemistry as well as regiochemistry of NNRTI can profoundly affect their anti-HIV activity.
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
HI-236 was highly effective against the multidrug-resistant HIV-1 strain RT-MDR with multiple mutations involving the RT residues 74V, 41L, 106A, and 215Y and twice as effective as the recently reported lead compound N-[2-fluorophenethyl]-N'-[2-(5-bromopyridyl)]-thiourea.
Structure-Based Design and Engineering of a Nontoxic Recombinant Pokeweed Antiviral Protein with Potent Anti-Human Immunodeficiency Virus Activity
Rationally engineered nontoxic recombinant PAPs such as FLP-102 andFLP-105 may provide the basis for effective salvage therapies for patients harboring highly drug-resistant strains of HIV-1 and warrant the further development of these promising new biotherapeutic agents.
Structure-Based Design of Novel Dihydroalkoxybenzyloxopyrimidine Derivatives as Potent Nonnucleoside Inhibitors of the Human Immunodeficiency Virus Reverse Transcriptase
ABSTRACT Two highly potent dihydroalkoxybenzyloxopyrimidine (DABO) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of human immunodeficiency virus (HIV) reverse transcriptase