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Comparative in vitro and in vivo activities of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase, CI-972 and PD 141955.
TLDR
An in-parallel comparison is presented of the in vitro and in vivo properties of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase (PNP) and PD 141955, with PD considerably more potent and active in all systems studied. Expand
Inhibitors of human purine nucleoside phosphorylase. Synthesis and biological activities of 8-amino-3-benzylhypoxanthine and related analogues.
TLDR
2,8-Diamino-3-substituted hypoxanthines (16a-d) represent a novel structural type hitherto unreported in the literature, and efficient methodologies for their synthesis were developed in the present studies. Expand
Structure-Activity Analysis of N-Type Calcium Channel Inhibitor SO-3.
TLDR
The replacement of some amino acid residues ofSO-3 in loop 1 with the corresponding residues of CVID and GVIA improved the inhibitory activity of SO-3, and provided a new strategy for improving the potency of Cav2.2 inhibitors. Expand
The biochemistry and pharmacology of PD 116124 (8-amino-2'-nordeoxyguanosine), an inhibitor of purine nucleoside phosphorylase (PNP).
TLDR
PD 116124 produced marked and statistically significant elevation of both inosine and guanosine and was only weakly inhibitory in human mixed lymphocyte cultures, but in the presence of 10 microM dGuo, the IC50 for PD 116124 was reduced to 108.7 microM. Expand
Selective in vitro inhibition of human MOLT-4 T lymphoblasts by the novel purine nucleoside phosphorylase inhibitor, CI-972.
TLDR
Inhibition of MOLT-4 growth was associated with an increase in dGTP that was dependent on CI-972 concentration and inhibited by 2'-deoxycytidine, and growth could not be restored by hypoxanthine or adenine. Expand
CHARACTERIZATION OF ANTIGENIC SITES OF HUMAN PROSTATIC ACID PHOSPHATASE
TLDR
Two approaches are adopted: one involving structural studies by peptide mapping, and the other involving topological mapping through the use of uniquely defined antibodies, which exhibited a remarkably specific binding to PAP, particularly to the Sp-1 fragment, without binding to other acid phosphatase preparations. Expand
Double-antibody immunoenzyme assay for human prostatic acid phosphatase.
TLDR
Results showed that the double-antibody radioimmunoassay (RIA) and immunoenzyme assay (IEA) for measuring the concentration of prostatic acid phosphatase in human serum was highly correlated and 3-10% false positives were seen. Expand
Antibody restores catalytic activity of a small molecular weight fragment of human prostatic acid phosphatase.
TLDR
In the presence of specific antibodies directed against human prostatic acid phosphatase, both the subunit polypeptides and one of the cyanogen bromide-derived peptides (C5) regained catalytic activity. Expand
Inhibitors of human purine nucleoside phosphorylase. Synthesis, purine nucleoside phosphorylase inhibition, and T-cell cytotoxicity of 2,5-diaminothiazolo[5,4-d]pyrimidin-7(6H)-one and
TLDR
Two thio isosteres of 8-aminoguanine were synthesized and evaluated for their inhibitory activity against PNP and were found to be weak inhibitors of P NP and to be noncytotoxic for MOLT-4 T-cells in culture. Expand
Biochemical and pharmacological properties of CI-972, a novel 9-deazaguanine analog purine nucleoside phosphorylase (PNP) inhibitor.
TLDR
2'-Deoxycytidine (10 microM), but not hypoxanthine or adenine, restored MOLT-4 cell growth, and inhibition of 3H-thymidine uptake in MOLt-4 cells correlated with accumulation of dGTP, while alterations in guanine nucleotides were not observed. Expand
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