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target has curated data in GtoImmuPdb
Target id: 1353
Nomenclature: CYP5A1
Abbreviated Name: Thromboxane-A synthase
Family: CYP5, CYP7 and CYP8 families, Prostaglandin synthases
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 4 | 533 | 7q34 | TBXAS1 | thromboxane A synthase 1 | |
| Mouse | 4 | 533 | 6 17.85 cM | Tbxas1 | thromboxane A synthase 1, platelet | |
| Rat | 4 | 533 | 4q22 | Tbxas1 | thromboxane A synthase 1 | |
| Previous and Unofficial Names |
| CYP5 | cytochrome P450, family 5, subfamily A, polypeptide 1 | cytochrome P450 5A1 | thromboxane A synthase 1 | thromboxane A synthase 1, platelet | thromboxane A synthase 1 (platelet) |
| Database Links |
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| Alphafold | P24557 (Hs), P36423 (Mm), P49430 (Rn) |
| BRENDA | 5.3.99.5 |
| ChEMBL Target | CHEMBL1835 (Hs), CHEMBL4028 (Rn) |
| DrugBank Target | P24557 (Hs) |
| Ensembl Gene | ENSG00000059377 (Hs), ENSMUSG00000029925 (Mm), ENSRNOG00000007918 (Rn) |
| Entrez Gene | 6916 (Hs), 21391 (Mm), 24886 (Rn) |
| Human Protein Atlas | ENSG00000059377 (Hs) |
| KEGG Enzyme | 5.3.99.5 |
| KEGG Gene | hsa:6916 (Hs), mmu:21391 (Mm), rno:24886 (Rn) |
| OMIM | 274180 (Hs) |
| Pharos | P24557 (Hs) |
| UniProtKB | P24557 (Hs), P36423 (Mm), P49430 (Rn) |
| Wikipedia | TBXAS1 (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| The arachadonic acid-derived inflammtory mediators leukotrienes, prostaglandins, and thromboxanes play important roles in inflammatory and allergic diseases, so the search for inhibitors of their production is a long-standing medicinal chemistry goal [8]. The most well known drug family in this field are the cyclooxygenase (COX) Inhibitors (or nonsteroidal antiinflammatory drugs; NSAIDs) which reduce prostaglandin synthesis, and are widely used for their antiinflammatory action. The clinically approved 5-lipoxygenase (5-LOX) inhibitor zileuton blocks formation of leukotrienes. The thromboxane A2 synthetase function of CYP5A1 is another valid molecular target in this search for novel antiinflammatory drugs. The discovery of inhibitors of thromboxane synthesis may help address those conditions that do not respond to inhibitors of the prostanoid and leukotriene pathways. |
1. Bhagwat SS, Gude C, Boswell C, Contardo N, Cohen DS, Dotson R, Mathis J, Lee W, Furness P, Zoganas H. (1992) Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs. J Med Chem, 35 (23): 4373-83. [PMID:1447738]
2. Faull AW, Brewster AG, Brown GR, Smithers MJ, Jackson R. (1995) Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids. J Med Chem, 38 (4): 686-94. [PMID:7861416]
3. Gorman RR, Johnson RA, Spilman CH, Aiken JW. (1983) Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins, 26 (2): 325-42. [PMID:6316421]
4. Gresele P, Deckmyn H, Arnout J, Nenci GG, Vermylen J. (1989) Characterization of N,N'-bis(3-picolyl)-4-methoxy-isophtalamide (picotamide) as a dual thromboxane synthase inhibitor/thromboxane A2 receptor antagonist in human platelets. Thromb Haemost, 61 (3): 479-84. [PMID:2552606]
5. Gryglewski RJ, Szczeklik A, Korbut R, Swies J, Musiał J, Krzanowski M, Maga P. (1995) The mechanism of anti-thrombotic, thrombolytic and fibrinolytic actions of camonagrel--a new thromboxane synthase inhibitor. Wien Klin Wochenschr, 107 (9): 283-9. [PMID:7778318]
6. Hibi S, Okamoto Y, Tagami K, Numata H, Kobayashi N, Shinoda M, Kawahara T, Harada K, Miyamoto K, Yamatsu I. (1996) Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. J Med Chem, 39 (16): 3148-57. [PMID:8759636]
7. Hiraku S, Taniguchi K, Wakitani K, Omawari N, Kira H, Miyamoto T, Okegawa T, Kawasaki A, Ujiie A. (1986) Pharmacological studies on the TXA2 synthetase inhibitor (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046). Jpn J Pharmacol, 41 (3): 393-401. [PMID:3093741]
8. Khanapure SP, Garvey DS, Janero DR, Letts LG. (2007) Eicosanoids in inflammation: biosynthesis, pharmacology, and therapeutic frontiers. Curr Top Med Chem, 7 (3): 311-40. [PMID:17305573]
9. Randall MJ, Parry MJ, Hawkeswood E, Cross PE, Dickinson RP. (1981) UK-37, 248, a novel, selective thromboxane synthetase inhibitor with platelet anti-aggregatory and anti-thrombotic activity. Thromb Res, 23 (1-2): 145-62. [PMID:6795753]
