Target Information
Target General Infomation | |||||
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Target ID |
T40111
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Former ID |
TTDS00062
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Target Name |
Inosine-5'-monophosphate dehydrogenase
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Synonyms |
IMP dehydrogenase; IMPD; IMPDH; Inosine dehydrogenase; NAD-dependent inosine monophosphate dehydrogenase; Probable inosine-5'-monophosphate dehydrogenase IMD1; SOI12; Superoxide-inducible protein 12
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Target Type |
Successful
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Disease | Acute lymphoblastic leukemia [ICD9: 204.0, 556; ICD10: C91.0] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Hyperuricemia; Transplant rejection [ICD9:790.6, 279.5, 996; ICD10: E79.0, D89.8, T86] | |||||
Hepatitis virus infection [ICD9: 573.3; ICD10: K75.9] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Function |
Catalyzes the conversion of inosine 5'-phosphate (IMP) to xanthosine 5'-phosphate (XMP), the first committed and rate- limiting step in the de novo synthesis of guaninenucleotides, and therefore plays an important role in the regulation of cell growth. Essential for mouse infection by tick bite and critical for the survival in environments that appear to lack sufficient amounts of guanine, guanosine, and/or deoxyguanosine to support spirochete growth, such as mammalian host tissues.
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BioChemical Class |
Short-chain dehydrogenases reductases
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Target Validation |
T40111
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EC Number |
EC 1.1.1.205
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Drugs and Mode of Action | |||||
Drug(s) | Mercaptopurine | Drug Info | Approved | Acute lymphoblastic leukemia | [537297], [542241] |
Mizoribine | Drug Info | Approved | Hyperuricemia; Transplant rejection | [536361], [551871] | |
Ribavirin | Drug Info | Approved | HCV infection | [538312], [541922] | |
Tiazofurin | Drug Info | Approved | Cancer | [535786] | |
Viramidine | Drug Info | Phase 3 | HCV infection | [530252] | |
VX-148 | Drug Info | Discontinued in Phase 2 | Psoriasis | [547204] | |
VX-497 | Drug Info | Discontinued in Phase 2 | Hepatitis virus infection | [546443] | |
Inhibitor | 6-Cl-IMP | Drug Info | [537838] | ||
Imidazo[4,5-e][1,4]diazapine nucleotide (I) | Drug Info | [538123] | |||
Inosinic Acid | Drug Info | [551393] | |||
Mercaptopurine | Drug Info | [536724] | |||
Mizoribine | Drug Info | [535145], [535945] | |||
Ribavirin | Drug Info | [536140], [536154] | |||
Selenazofurin | Drug Info | [538118] | |||
TAD | Drug Info | [535593] | |||
Tiazofurin | Drug Info | [537700], [537883], [538118] | |||
Viramidine | Drug Info | [536317] | |||
VX-148 | Drug Info | [535538] | |||
VX-497 | Drug Info | [535145] | |||
References | |||||
Ref 530252 | A phase III study of the safety and efficacy of viramidine versus ribavirin in treatment-na?ve patients with chronic hepatitis C: ViSER1 results. Hepatology. 2009 Sep;50(3):717-26. | ||||
Ref 535786 | De novo synthesis of two new cytotoxic tiazofurin analogues with modified sugar moieties. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3167-70. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 537297 | S-adenosylmethionine regulates thiopurine methyltransferase activity and decreases 6-mercaptopurine cytotoxicity in MOLT lymphoblasts. Biochem Pharmacol. 2009 Jun 15;77(12):1845-53. Epub 2009 Mar 19. | ||||
Ref 538312 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076192. | ||||
Ref 541922 | (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: 6842). | ||||
Ref 542241 | (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: 7226). | ||||
Ref 546443 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008158) | ||||
Ref 535145 | VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent. J Pharm Sci. 2001 May;90(5):625-37. | ||||
Ref 535538 | Characterization of pharmacological efficacy of VX-148, a new, potent immunosuppressive inosine 5'-monophosphate dehydrogenase inhibitor. J Pharmacol Exp Ther. 2002 Sep;302(3):1272-7. | ||||
Ref 535593 | Crystal structure of a ternary complex of Tritrichomonas foetus inosine 5'-monophosphate dehydrogenase: NAD+ orients the active site loop for catalysis. Biochemistry. 2002 Nov 5;41(44):13309-17. | ||||
Ref 535945 | Cofactor mimics as selective inhibitors of NAD-dependent inosine monophosphate dehydrogenase (IMPDH)--the major therapeutic target. Curr Med Chem. 2004 Apr;11(7):887-900. | ||||
Ref 536140 | A randomized, double-blind, placebo-controlled dose-escalation trial of merimepodib (VX-497) and interferon-alpha in previously untreated patients with chronic hepatitis C. Antivir Ther. 2005;10(5):635-43. | ||||
Ref 536154 | Treating HCV with ribavirin analogues and ribavirin-like molecules. J Antimicrob Chemother. 2006 Jan;57(1):8-13. Epub 2005 Nov 17. | ||||
Ref 536317 | Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25. | ||||
Ref 536724 | Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67. Epub 2008 May 28. | ||||
Ref 537700 | Relationships between the cytotoxicity of tiazofurin and its metabolism by cultured human lung cancer cells. J Clin Invest. 1985 Jan;75(1):175-82. | ||||
Ref 537838 | Identification of the IMP binding site in the IMP dehydrogenase from Tritrichomonas foetus. Biochemistry. 1995 Oct 24;34(42):13889-94. | ||||
Ref 537883 | Sequential impact of tiazofurin and ribavirin on the enzymic program of the bone marrow. Cancer Res. 1993 Dec 15;53(24):5982-6. | ||||
Ref 538118 | In vitro and in vivo antiproliferative activity of IPCAR, a new pyrazole nucleoside analog. Anticancer Res. 1998 Jul-Aug;18(4A):2623-30. |
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