Target Validation Information
Target ID T88240
Target Name Dihydropteroate synthetase
Target Type
Successful
Drug Potency against Target Sulfonamides Drug Info IC50 = 13 nM [537826]
Dapsone Drug Info IC50 = 150 nM [537826]
Sulfamethoxazole Drug Info IC50 = 23 nM [537826]
Sulfapyridine Drug Info IC50 = 180 nM [537826]
Sulphadoxine Drug Info IC50 = 740 nM [537826]
Sulfamerazine Drug Info IC50 = 78 nM [537826]
2,6-diamino-5-nitrosopyrimidin-4(3H)-one Drug Info IC50 = 8000 nM [530506]
Oritavancin Drug Info MIC50 = 0.5 ug/ml [552333]
Sulfisoxazole Drug Info IC50 = 40 nM [537826]
Sulfadiazine Drug Info IC50 = 190 nM [537826]
Sulfamethazine Drug Info IC50 = 5700 nM [553105]
Daptomycin Drug Info MIC90 = 2 ug/ml [552333]
Sulfadoxine Drug Info IC50 = 740 nM [537826]
Sulfamethizole Drug Info IC50 = 7500 nM [553105]
Action against Disease Model Sulfadiazine Following 72 h of exposure, the 50% inhibitory concentration of rBPI21 for T. gondii was 2.6 micrograms/ml, whereas only slight cytotoxicity for HFF cells was observed at the concentrations tested. Subsequent mathematical analyses revealed that the combination of rBPI21 with sulfadiazine yielded slight to moderate synergistic effects against T. gondii in vitro. Infection of mice orally with C56 cysts or intraperitoneally (i.p.) with RH tachyzoites resulted in 100% mortality, whereas prolongation of the time to death or significant survival (P = 0.002) was noted for thoseanimals treated with 5 to 20 mg of rBPI21 per kg of body weight per day. Treatment with rBPI21 in combination with sulfadiazine resulted in significant (P = 0.0001) survival of mice infected i.p. with tachyzoites but not of mice infected orally with T. gondii cysts. These results indicate that rBPI21 is active in vitro and in vivo against T. gondii and that its activity is significantly enhanced when it is used in combination with sulfadiazine. [552180] Drug Info
Dapsone IC50 for Plasmodi uM falcipar uM isolates from Entosopia, Kenya: 28 ng/mL [552454] Drug Info
References
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 552180Recombinant bactericidal/permeability-increasing protein (rBPI21) in combination with sulfadiazine is active against Toxoplasma gondii. Antimicrob Agents Chemother. 1999 Apr;43(4):758-62.
Ref 552454Drug susceptibility and genetic evaluation of Plasmodium falciparum isolates obtained in four distinct geographical regions of Kenya. Antimicrob Agents Chemother. 2004 Sep;48(9):3598-601.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 530506J Med Chem. 2010 Jan 14;53(1):166-77.Structural studies of pterin-based inhibitors of dihydropteroate synthase.
Ref 552333Novel antibacterial agents for the treatment of serious Gram-positive infections. Expert Opin Investig Drugs. 2003 Mar;12(3):379-99.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 553105Interaction of sulfonamide and sulfone compounds with Toxoplasma gondii dihydropteroate synthase. J Clin Invest. 1990 Feb;85(2):371-9.
Ref 552333Novel antibacterial agents for the treatment of serious Gram-positive infections. Expert Opin Investig Drugs. 2003 Mar;12(3):379-99.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 553105Interaction of sulfonamide and sulfone compounds with Toxoplasma gondii dihydropteroate synthase. J Clin Invest. 1990 Feb;85(2):371-9.

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