Target Information
| Target General Information | Top | |||||
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| Target ID |
T88240
(Former ID: TTDS00237)
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| Target Name |
Bacterial Dihydropteroate synthetase (Bact folP)
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| Synonyms |
folP; H2Pte synthase; Dihydropteroate synthase; Dihydropteroate pyrophosphorylase; DHPS
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| Gene Name |
Bact folP
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 9 Target-related Diseases | + | ||||
| 1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
| 2 | Cystitis [ICD-11: GC00] | |||||
| 3 | Dermatitis herpetiformis [ICD-11: EB44] | |||||
| 4 | Glanders [ICD-11: 1B92] | |||||
| 5 | Gram-positive bacterial infection [ICD-11: 1B74-1F40] | |||||
| 6 | Malaria [ICD-11: 1F40-1F45] | |||||
| 7 | Respiratory infection [ICD-11: CA07-CA4Z] | |||||
| 8 | Rheumatic fever [ICD-11: 1B40] | |||||
| 9 | Urinary tract infection [ICD-11: GC08] | |||||
| Function |
Dhps catalyzes the formation of the immediate precursor of folic acid. It is implicated in resistance to sulfonamide.
Click to Show/Hide
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| BioChemical Class |
Alkyl aryl transferase
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| UniProt ID | ||||||
| EC Number |
EC 2.5.1.15
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| Sequence |
MKLFAQGTSLDLSHPHVMGILNVTPDSFSDGGTHNSLIDAVKHANLMINAGATIIDVGGE
STRPGAAEVSVEEELQRVIPVVEAIAQRFEVWISVDTSKPEVIRESAKVGAHIINDIRSL SEPGALEAAAETGLPVCLMHMQGNPKTMQEAPKYDDVFAEVNRYFIEQIARCEQAGIAKE KLLLDPGFGFGKNLSHNYSLLARLAEFHHFNLPLLVGMSRKSMIGQLLNVGPSERLSGSL ACAVIAAMQGAHIIRVHDVKETVEAMRVVEATLSAKENKRYE Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 22 Approved Drugs | + | ||||
| 1 | Cefozopran | Drug Info | Approved | Gram-positive bacterial infection | [1] | |
| 2 | Chlorhexidine | Drug Info | Approved | Bacterial infection | [2] | |
| 3 | Colistimethate | Drug Info | Approved | Respiratory tract infection | [3], [4] | |
| 4 | Colistin | Drug Info | Approved | Pseudomonas infection | [4] | |
| 5 | Daptomycin | Drug Info | Approved | Bacterial infection | [5] | |
| 6 | Doripenem | Drug Info | Approved | Urinary tract infection | [6], [7] | |
| 7 | Faropenem | Drug Info | Approved | Gram-positive bacterial infection | [1] | |
| 8 | Gramicidin D | Drug Info | Approved | Bacterial infection | [8] | |
| 9 | Oritavancin | Drug Info | Approved | Bacterial infection | [4], [7] | |
| 10 | Polymyxin B Sulfate | Drug Info | Approved | Pseudomonas infection | [4], [9] | |
| 11 | Silver sulfadiazine | Drug Info | Approved | Bacterial infection | [4], [10], [11] | |
| 12 | Sulfacytine | Drug Info | Approved | Cystitis | [12], [4] | |
| 13 | Sulfadiazine | Drug Info | Approved | Rheumatic fever | [4] | |
| 14 | Sulfamerazine | Drug Info | Approved | Bacterial infection | [13] | |
| 15 | Sulfamethazine | Drug Info | Approved | Bacterial infection | [14] | |
| 16 | Sulfamethizole | Drug Info | Approved | Urinary tract infection | [5] | |
| 17 | Sulfamethoxazole | Drug Info | Approved | Bacterial infection | [4], [5] | |
| 18 | Sulfanilamide | Drug Info | Approved | Bacterial infection | [15] | |
| 19 | Sulfapyridine | Drug Info | Approved | Dermatitis herpetiformis | [4], [16] | |
| 20 | Sulfisoxazole | Drug Info | Approved | Urinary tract infection | [4] | |
| 21 | Sulfonamides | Drug Info | Approved | Bacterial infection | [17] | |
| 22 | Sulphadoxine | Drug Info | Approved | Malaria | [18], [19] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Sulfametopyrazine | Drug Info | Withdrawn from market | Urinary tract infection | [20] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 22 Inhibitor drugs | + | ||||
| 1 | Cefozopran | Drug Info | [1] | |||
| 2 | Doripenem | Drug Info | [1] | |||
| 3 | Faropenem | Drug Info | [1] | |||
| 4 | Oritavancin | Drug Info | [1] | |||
| 5 | Sulfacytine | Drug Info | [26] | |||
| 6 | Sulfadiazine | Drug Info | [27] | |||
| 7 | Sulfamerazine | Drug Info | [28] | |||
| 8 | Sulfamethazine | Drug Info | [29] | |||
| 9 | Sulfamethizole | Drug Info | [30] | |||
| 10 | Sulfamethoxazole | Drug Info | [31], [32] | |||
| 11 | Sulfapyridine | Drug Info | [28] | |||
| 12 | Sulfisoxazole | Drug Info | [34] | |||
| 13 | Sulfametopyrazine | Drug Info | [36] | |||
| 14 | 2,6-diamino-5-nitropyrimidin-4(3H)-one | Drug Info | [37] | |||
| 15 | 2,6-diamino-5-nitrosopyrimidin-4(3H)-one | Drug Info | [37] | |||
| 16 | 2-amino-8-methyl-7,8-dihydropteridin-4(3H)-one | Drug Info | [37] | |||
| 17 | 6-Methylamino-5-Nitroisocytosine | Drug Info | [38] | |||
| 18 | Ethylene diamine | Drug Info | [39] | |||
| 19 | HKI-9924129 | Drug Info | [1] | |||
| 20 | Pterin-6-Yl-Methyl-Monophosphate | Drug Info | [40] | |||
| 21 | Pteroic Acid | Drug Info | [41] | |||
| 22 | [Pterin-6-Yl Methanyl]-Phosphonophosphate | Drug Info | [40] | |||
| Breaker | [+] 1 Breaker drugs | + | ||||
| 1 | Chlorhexidine | Drug Info | [21] | |||
| Binder | [+] 8 Binder drugs | + | ||||
| 1 | Colistimethate | Drug Info | [22] | |||
| 2 | Colistin | Drug Info | [22] | |||
| 3 | Daptomycin | Drug Info | [23] | |||
| 4 | Gramicidin D | Drug Info | [24] | |||
| 5 | Polymyxin B Sulfate | Drug Info | [22] | |||
| 6 | Silver sulfadiazine | Drug Info | [25] | |||
| 7 | Sulfonamides | Drug Info | [17] | |||
| 8 | Sulphadoxine | Drug Info | [18], [35] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Sulfanilamide | Drug Info | [33] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Drug Resistance Mutation (DRM) | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019822. | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064216. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73. | |||||
| REF 6 | 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9. | |||||
| REF 7 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
| REF 8 | Drug information of Gramicidin D, 2008. eduDrugs. | |||||
| REF 9 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 064028. | |||||
| REF 10 | URL: 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 11 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019608. | |||||
| REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017569. | |||||
| REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123. | |||||
| REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080123. | |||||
| REF 15 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088718. | |||||
| REF 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 000159. | |||||
| REF 17 | Has nature already identified all useful antibacterial targets Curr Opin Microbiol. 2008 Oct;11(5):387-92. | |||||
| REF 18 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | |||||
| REF 19 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018557. | |||||
| REF 20 | Drug information of Sulfametopyrazine, 2008. eduDrugs. | |||||
| REF 21 | The mechanism of action of chlorhexidine. FEMS Microbiol Lett. 1992 Dec 15;79(1-3):211-5. | |||||
| REF 22 | Polymyxin B sulfate and colistin: old antibiotics for emerging multiresistant gram-negative bacteria. Ann Pharmacother. 1999 Sep;33(9):960-7. | |||||
| REF 23 | Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin. Chem Biol. 2004 Jul;11(7):949-57. | |||||
| REF 24 | Structures of gramicidins A, B, and C incorporated into sodium dodecyl sulfate micelles. Biochemistry. 2001 Oct 2;40(39):11676-86. | |||||
| REF 25 | 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 26 | Sulfacytine in uncomplicated urinary tract infections. Double-blind comparison with sulfisoxazole. Urology. 1976 Mar;7(3):267-71. | |||||
| REF 27 | Sulfadiazine/hydroxypropyl-beta-cyclodextrin host-guest system: Characterization, phase-solubility and molecular modeling. Bioorg Med Chem. 2008 May 15;16(10):5788-94. | |||||
| REF 28 | A confirmatory method for the simultaneous extraction, separation, identification and quantification of Tetracycline, Sulphonamide, Trimethoprim an... J Chromatogr A. 2009 Nov 13;1216(46):8110-6. | |||||
| REF 29 | 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 Oct 23;1216(43):7275-80. | |||||
| REF 30 | Inhibition of bioluminescence in Photobacterium phosphoreum by sulfamethizole and its stimulation by thymine. Biochim Biophys Acta. 1990 Jun 26;1017(3):229-34. | |||||
| REF 31 | In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs. Antimicrob Agents Chemother. 1995 Apr;39(4):948-52. | |||||
| REF 32 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | |||||
| REF 33 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 34 | Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob Agents Chemother. 1995 Aug;39(8):1756-63. | |||||
| REF 35 | 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 36 | 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 37 | Structural studies of pterin-based inhibitors of dihydropteroate synthase. J Med Chem. 2010 Jan 14;53(1):166-77. | |||||
| REF 38 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | |||||
| REF 39 | Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. | |||||
| REF 40 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 41 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
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