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Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.
Studies on a series of benzoquinazoline folate analogues as inhibitors of human thymidylate synthase led to the selection of 1843U89 for further evaluation. This compound had a Ki of 90 pM versus… Expand
Cloning, sequencing, and enhanced expression of the dihydropteroate synthase gene of Escherichia coli MC4100.
- W. Dallas, J. Gowen, P. Ray, M. J. Cox, I. Dev
- Biology, Medicine
- Journal of bacteriology
- 1 September 1992
The Escherichia coli gene coding for dihydropteroate synthase (DHPS) has been cloned and sequenced. The protein has 282 amino acids and a compositional molecular mass of 30,314 daltons. Increased… Expand
Inhibition of prolipoprotein signal peptidase by globomycin.
Globomycin inhibits the prolipoprotein-specific signal peptidase activity by binding to the enzyme in a noncompetitive manner (Ki = 36 nM). The Km of prolipoprotein signal peptidase for the… Expand
The effect of anti-VEGF therapy on immature myeloid cell and dendritic cells in cancer patients
- T. Osada, G. Chong, +9 authors M. Morse
- Medicine, Biology
- Cancer Immunology, Immunotherapy
- 10 January 2008
Impairment of dendritic cells (DC), the most effective activators of anticancer immune responses, is one mechanism for defective antitumor immunity, but the causes of DC impairment are incompletely… Expand
Superiority of yeast over bacterial cytosine deaminase for enzyme/prodrug gene therapy in colon cancer xenografts.
The enzyme/prodrug strategy using bacterial cytosine deaminase (bCD) and 5-fluorocytosine (5-FC) is currently under investigation for cancer gene therapy. A major limitation for the use of bCD is… Expand
Rapid assay and purification of a unique signal peptidase that processes the prolipoprotein from Escherichia coli B.
A simple and accurate assay for prolipoprotein signal peptidase activity has been described that is based on the solubility of the signal peptide in 80% acetone. The unprocessed precursor and the… Expand
Sources of one-carbon units in the folate pathway of Escherichia coli.
The anti-human immunodeficiency virus agent 3'-fluorothymidine induces DNA damage and apoptosis in human lymphoblastoid cells.
- R. Sundseth, S. Joyner, J. T. Moore, R. Dornsife, I. Dev
- Biology, Medicine
- Antimicrobial agents and chemotherapy
- 1 February 1996
Patients infected with the human immunodeficiency virus experienced severe hematopoietic toxicity after treatment with the deoxynucleoside analog 3'-fluorothymidine (FLT). Using several methods for… Expand
Minimum substrate sequence for signal peptidase I of Escherichia coli.
The minimum substrate sequence recognized by signal peptidase I (SPase I or leader peptidase) was defined by measuring the kinetic parameters for a set of chemically synthesized peptides… Expand
Mode of binding of folate analogs to thymidylate synthase. Evidence for two asymmetric but interactive substrate binding sites.
- I. Dev, W. Dallas, R. Ferone, M. Hanlon, D. D. McKee, B. B. Yates
- Chemistry, Medicine
- The Journal of biological chemistry
- 21 January 1994
Human thymidylate synthase is a polymeric protein composed of two subunits with identical primary structures. In this study we determined the binding affinities of 5,10-methylene… Expand