Target Information

Target General Infomation
Target ID
T88240
Former ID
TTDS00237
Target Name
Dihydropteroate synthetase
Gene Name
folP
Synonyms
DHPS; Dihydropteroate pyrophosphorylase; Dihydropteroate synthase; H2Pte synthase; folP
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Bacterial respiratory tract infection [ICD10: J13, J15]
Dermatitis herpetiformis [ICD9: 694; ICD10: L12.2, L13]
Gram-positive bacterial infection [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104]
Gram-positive bacterial infection [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104]
Infections by gram-negative bacilli particularly Pseudomonas aeruginosa [ICD10: B96.5]
Infection of P. falciparum [ICD9: 84; ICD10: B50-B54]
Malaria [ICD10: B54]
Pseudomonas aeruginosa infection [ICD9: 001-139; ICD10: B96.5]
Rheumatic fever; Meningococcal meningitis [ICD10: R50.9]
Tuberculosis [ICD9: 010-018; ICD10: A15-A19]
Urinary tract infections [ICD9: 599; ICD10: N39.0]
Urinary tract infections; Cystitis [ICD9:599; ICD10: N39.0, N30]
Urinary tract infections; Meningococcal meningitis; Acute otitis media [ICD10: N39]
Function
Dhps catalyzes the formation of the immediate precursor of folic acid. It is implicated in resistance to sulfonamide.
BioChemical Class
Alkyl aryl transferase
Target Validation
T88240
UniProt ID
P0AC13
EC Number
EC 2.5.1.15
Sequence
MKLFAQGTSLDLSHPHVMGILNVTPDSFSDGGTHNSLIDAVKHANLMINAGATIIDVGGE
STRPGAAEVSVEEELQRVIPVVEAIAQRFEVWISVDTSKPEVIRESAKVGAHIINDIRSL
SEPGALEAAAETGLPVCLMHMQGNPKTMQEAPKYDDVFAEVNRYFIEQIARCEQAGIAKE
KLLLDPGFGFGKNLSHNYSLLARLAEFHHFNLPLLVGMSRKSMIGQLLNVGPSERLSGSL
ACAVIAAMQGAHIIRVHDVKETVEAMRVVEATLSAKENKRYE
Structure
1AJ0; 1AJ2; 1AJZ
Drugs and Mode of Action
Drug(s) Cefozopran Drug Info Approved Gram-positive bacterial infection [536094]
Chlorhexidine Drug Info Approved Bacterial infections [538533]
Colistimethate Drug Info Approved Bacterial respiratory tract infection [538213], [551871]
Colistin Drug Info Approved Infections by gram-negative bacilli particularly Pseudomonas aeruginosa [551871]
Daptomycin Drug Info Approved Bacterial infections [536773]
Doripenem Drug Info Approved Urinary tract infections [529282], [533123]
Faropenem Drug Info Approved Gram-positive bacterial infection [536094]
Gramicidin D Drug Info Approved Bacterial infections [550737]
Oritavancin Drug Info Approved Bacterial infections [533123], [551871]
Polymyxin B Sulfate Drug Info Approved Pseudomonas aeruginosa infection [538210], [551871]
Silver sulfadiazine Drug Info Approved Bacterial infections [467470], [538527], [551871]
Sulfacytine Drug Info Approved Urinary tract infections; Cystitis [538490], [551871]
Sulfadiazine Drug Info Approved Rheumatic fever; Meningococcal meningitis [551871]
Sulfadoxine Drug Info Approved Malaria [538509]
Sulfamerazine Drug Info Approved Bacterial infections [538336]
Sulfamethazine Drug Info Approved Bacterial infections [538337]
Sulfamethizole Drug Info Approved Urinary tract infections [536773]
Sulfamethoxazole Drug Info Approved Bacterial infections [536773], [551871]
Sulfanilamide Drug Info Approved Bacterial infections [538372]
Sulfapyridine Drug Info Approved Dermatitis herpetiformis [538383], [551871]
Sulfisoxazole Drug Info Approved Urinary tract infections; Meningococcal meningitis; Acute otitis media [551871]
Sulfonamides Drug Info Approved Bacterial infections [536854]
Sulphadoxine Drug Info Approved Malaria [536602]
Doripenem Drug Info Phase 3 Gram-positive bacterial infection [536094]
Sulfonamide Drug Info Phase 3 Discovery agent [521417]
Sulfametopyrazine Drug Info Withdrawn from market Urinary tract infections [550724]
Oritavancin Drug Info Terminated Gram-positive bacterial infection [536773]
Inhibitor 2,6-diamino-5-nitropyrimidin-4(3H)-one Drug Info [530506]
2,6-diamino-5-nitrosopyrimidin-4(3H)-one Drug Info [530506]
2-amino-8-methyl-7,8-dihydropteridin-4(3H)-one Drug Info [530506]
6-Methylamino-5-Nitroisocytosine Drug Info [551391]
Cefozopran Drug Info [536094]
Doripenem Drug Info [536094]
Ethylene diamine Drug Info [536472]
Faropenem Drug Info [536094]
HKI-9924129 Drug Info [536094]
Oritavancin Drug Info [536094]
Pterin-6-Yl-Methyl-Monophosphate Drug Info [551393]
Pteroic Acid Drug Info [551374]
Sulfacytine Drug Info [537854]
Sulfadiazine Drug Info [536696]
Sulfadoxine Drug Info [536658]
Sulfamerazine Drug Info [537591]
Sulfamethazine Drug Info [537438]
Sulfamethizole Drug Info [537676]
Sulfamethoxazole Drug Info [537865]
Sulfametopyrazine Drug Info [535512]
Sulfapyridine Drug Info [537591]
Sulfisoxazole Drug Info [537826]
[Pterin-6-Yl Methanyl]-Phosphonophosphate Drug Info [551393]
Breaker Chlorhexidine Drug Info [535808]
Binder Colistimethate Drug Info [534902]
Colistin Drug Info [534902]
Daptomycin Drug Info [535992]
Gramicidin D Drug Info [535268]
Polymyxin B Sulfate Drug Info [534902]
Silver sulfadiazine Drug Info [536263]
Sulfonamide Drug Info [535199]
Sulfonamides Drug Info [536854]
Sulphadoxine Drug Info [536602]
Sulphameth oxazole Drug Info [536135]
Modulator Sulfanilamide Drug Info [556264]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
References
Ref 467470(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4126).
Ref 521417ClinicalTrials.gov (NCT00000802) A Randomized, Comparative Study of Daily Dapsone and Daily Atovaquone for Prophylaxis Against PCP in HIV-Infected Patients Who Are Intolerant of Trimethoprim and/or Sulfonamides. U.S. National Institutes of Health.
Ref 5292822007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536094Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
Ref 536602The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 538210FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064028.
Ref 538213FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064216.
Ref 538336FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123.
Ref 538337FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123.
Ref 538372FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088718.
Ref 538383FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 000159.
Ref 538490FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017569.
Ref 538509FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018557.
Ref 538527FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019608.
Ref 538533FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019822.
Ref 550724Drug information of Sulfametopyrazine, 2008. eduDrugs.
Ref 550737Drug information of Gramicidin D, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 530506J Med Chem. 2010 Jan 14;53(1):166-77.Structural studies of pterin-based inhibitors of dihydropteroate synthase.
Ref 534902Polymyxin B sulfate and colistin: old antibiotics for emerging multiresistant gram-negative bacteria. Ann Pharmacother. 1999 Sep;33(9):960-7.
Ref 535199Resistance to trimethoprim and sulfonamides. Vet Res. 2001 May-Aug;32(3-4):261-73.
Ref 535268Structures of gramicidins A, B, and C incorporated into sodium dodecyl sulfate micelles. Biochemistry. 2001 Oct 2;40(39):11676-86.
Ref 535512Plasmodium falciparum dihydrofolate reductase Val-16 and Thr-108 mutation associated with in vivo resistance to antifolate drug: a case study. Indian J Malariol. 2001 Sep-Dec;38(3-4):76-83.
Ref 535808The mechanism of action of chlorhexidine. FEMS Microbiol Lett. 1992 Dec 15;79(1-3):211-5.
Ref 535992Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin. Chem Biol. 2004 Jul;11(7):949-57.
Ref 536094Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 536263Comparative evaluation of transdermal formulations of norfloxacin with silver sulfadiazine cream, USP, for burn wound healing property. J Burns Wounds. 2006 Jun 7;5:e4.
Ref 536472Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.
Ref 536602The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.
Ref 536658Geographical distribution of amino acid mutations in Plasmodium vivax DHFR and DHPS from malaria endemic areas of Thailand. Am J Trop Med Hyg. 2008 Mar;78(3):462-7.
Ref 536696Sulfadiazine/hydroxypropyl-beta-cyclodextrin host-guest system: Characterization, phase-solubility and molecular modeling. Bioorg Med Chem. 2008 May 15;16(10):5788-94. Epub 2008 Mar 27.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 537438A new and simple method to determine trace levels of sulfonamides in honey by high performance liquid chromatography with fluorescence detection. J Chromatogr A. 2009 May 29.
Ref 537591A confirmatory method for the simultaneous extraction, separation, identification and quantification of Tetracycline, Sulphonamide, Trimethoprim and Dapsone residues in muscle by ultra-high-performance liquid chromatography-tandem mass spectrometry according to Commission Decision 2002/657/EC. J Chromatogr A. 2009 Jun 9.
Ref 537676Inhibition of bioluminescence in Photobacterium phosphoreum by sulfamethizole and its stimulation by thymine. Biochim Biophys Acta. 1990 Jun 26;1017(3):229-34.
Ref 537826Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63.
Ref 537854Sulfacytine in uncomplicated urinary tract infections. Double-blind comparison with sulfisoxazole. Urology. 1976 Mar;7(3):267-71.
Ref 537865In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs. Antimicrob Agents Chemother. 1995 Apr;39(4):948-52.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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