Target Information
Target General Infomation | |||||
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Target ID |
T88240
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Former ID |
TTDS00237
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Target Name |
Dihydropteroate synthetase
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Gene Name |
folP
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Synonyms |
DHPS; Dihydropteroate pyrophosphorylase; Dihydropteroate synthase; H2Pte synthase; folP
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Target Type |
Successful
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Disease | Bacterial respiratory tract infection [ICD10: J13, J15] | ||||
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99] | |||||
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; Meningococcal meningitis; Acute otitis media [ICD10: N39] | |||||
Urinary tract infections [ICD9: 599; ICD10: N39.0] | |||||
Urinary tract infections; Cystitis [ICD9:599; ICD10: N39.0, N30] | |||||
Function |
Dhps catalyzes the formation of the immediate precursor of folic acid. It is implicated in resistance to sulfonamide.
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BioChemical Class |
Alkyl aryl transferase
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Target Validation |
T88240
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UniProt ID | |||||
EC Number |
EC 2.5.1.15
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Sequence |
MKLFAQGTSLDLSHPHVMGILNVTPDSFSDGGTHNSLIDAVKHANLMINAGATIIDVGGE
STRPGAAEVSVEEELQRVIPVVEAIAQRFEVWISVDTSKPEVIRESAKVGAHIINDIRSL SEPGALEAAAETGLPVCLMHMQGNPKTMQEAPKYDDVFAEVNRYFIEQIARCEQAGIAKE KLLLDPGFGFGKNLSHNYSLLARLAEFHHFNLPLLVGMSRKSMIGQLLNVGPSERLSGSL ACAVIAAMQGAHIIRVHDVKETVEAMRVVEATLSAKENKRYE |
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Structure |
1AJ0; 1AJ2; 1AJZ
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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 521417 | ClinicalTrials.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 536094 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
Ref 536602 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | ||||
Ref 536773 | How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30. | ||||
Ref 536854 | Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6. | ||||
Ref 538210 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064028. | ||||
Ref 538213 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064216. | ||||
Ref 538336 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123. | ||||
Ref 538337 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123. | ||||
Ref 538372 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088718. | ||||
Ref 538383 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 000159. | ||||
Ref 538490 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017569. | ||||
Ref 538509 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018557. | ||||
Ref 538527 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019608. | ||||
Ref 530506 | J Med Chem. 2010 Jan 14;53(1):166-77.Structural studies of pterin-based inhibitors of dihydropteroate synthase. | ||||
Ref 534902 | Polymyxin B sulfate and colistin: old antibiotics for emerging multiresistant gram-negative bacteria. Ann Pharmacother. 1999 Sep;33(9):960-7. | ||||
Ref 535268 | Structures of gramicidins A, B, and C incorporated into sodium dodecyl sulfate micelles. Biochemistry. 2001 Oct 2;40(39):11676-86. | ||||
Ref 535512 | Plasmodium 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 535992 | Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin. Chem Biol. 2004 Jul;11(7):949-57. | ||||
Ref 536094 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
Ref 536135 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | ||||
Ref 536263 | Comparative 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 536472 | Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. | ||||
Ref 536602 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | ||||
Ref 536658 | Geographical 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 536696 | Sulfadiazine/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 536854 | Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6. | ||||
Ref 537438 | A 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 537591 | A 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 537676 | Inhibition of bioluminescence in Photobacterium phosphoreum by sulfamethizole and its stimulation by thymine. Biochim Biophys Acta. 1990 Jun 26;1017(3):229-34. | ||||
Ref 537826 | Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63. | ||||
Ref 537854 | Sulfacytine in uncomplicated urinary tract infections. Double-blind comparison with sulfisoxazole. Urology. 1976 Mar;7(3):267-71. | ||||
Ref 537865 | In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs. Antimicrob Agents Chemother. 1995 Apr;39(4):948-52. |
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