Target Information

Target General Infomation
Target ID
T30081
Former ID
TTDR00500
Target Name
Thymidine kinase
Gene Name
TK1
Synonyms
TK; TK1
Target Type
Successful
Disease Adult varicella zoster virus infection [ICD10: B02]
Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Graft-versus-host disease [ICD9: 279.5; ICD10: T86.0]
Prostate cancer [ICD9: 185; ICD10: C61]
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Phosphorylates both thymidine and deoxyuridine.
BioChemical Class
Kinase
Target Validation
T30081
UniProt ID
P04183
EC Number
EC 2.7.1.21
Sequence
MSCINLPTVLPGSPSKTRGQIQVILGPMFSGKSTELMRRVRRFQIAQYKCLVIKYAKDTR
YSSSFCTHDRNTMEALPACLLRDVAQEALGVAVIGIDEGQFFPDIVEFCEAMANAGKTVI
VAALDGTFQRKPFGAILNLVPLAESVVKLTAVCMECFREAAYTKRLGTEKEVEVIGGADK
YHSVCRLCYFKKASGQPAGPDNKENCPVPGKPGEAVAARKLFAPQQILQCSPAN
Drugs and Mode of Action
Drug(s) DEOXYCYTIDINE Drug Info Approved Acute myeloid leukemia [1], [2]
TK-DLI Drug Info Preregistration Graft-versus-host disease [3]
FV-100 Drug Info Phase 3 Adult varicella zoster virus infection [4]
Radiosensitizer gene therapy Drug Info Phase 3 Pancreatic cancer [5]
HQK-1004 Drug Info Phase 2 Solid tumours [6]
Ad-OC-hsvTK/valacyclovir Drug Info Phase 1 Prostate cancer [7]
Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy Drug Info Phase 1 Cancer [8]
Sitimagene ceradenovec Drug Info Discontinued in Phase 3 Brain cancer [9]
Inhibitor (South)-Methanocarba-Thymidine Drug Info [10]
1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine Drug Info [11]
1-[2-(2-triphenylmethoxyethoxy)ethyl]thymine Drug Info [11]
1-[5-(triphenylmethoxy)pentyl]thymine Drug Info [11]
1-[6-(triphenylmethoxy)hexyl]thymine Drug Info [11]
1-[7-(triphenylmethoxy)heptyl]thymine Drug Info [11]
2-phenylamino-9-(4-hydroxy-butyl)-6-oxopurine Drug Info [12]
3'-(1,2,3-Triazol-1-yl)-3'-deoxy-beta-D-thymidine Drug Info [13]
3-(2-propyn-1-yl)thymidine Drug Info [14]
5-Bromothienyldeoxyuridine Drug Info [10]
5-Bromovinyldeoxyuridine Drug Info [15]
5-Iodo-2'-Deoxyuridine-5'-Monophosphate Drug Info [10]
5-Iododeoxyuridine Drug Info [10]
5-propyl-2'-deoxyuridine Drug Info [12]
6-(Dihydroxy-Isobutyl)-Thymine Drug Info [10]
6-Hydroxypropylthymine Drug Info [10]
9-(4-Hydroxy-3-(Hydroxymethyl)but-1-Yl)Guanine Drug Info [10]
9-(4-Hydroxybutyl)-N2-Phenylguanine Drug Info [10]
9-Hydroxypropyladenine, R-Isomer Drug Info [10]
9-Hydroxypropyladenine, S-Isomer Drug Info [10]
Ad-OC-hsvTK/valacyclovir Drug Info [16]
Adenosine-5'-Diphosphate Drug Info [15]
BVDU-MP Drug Info [17]
DEOXYCYTIDINE Drug Info [18]
Deoxythymidine Drug Info [10]
DEOXYURIDINE Drug Info [18]
Edoxudine Drug Info [12]
FV-100 Drug Info [19]
ITdU Drug Info [20]
L-5-(bromovinyl)deoxyuridine Drug Info [12]
L-5-iodo-2'-deoxyuridine Drug Info [12]
MTdU Drug Info [20]
N2-(3-trifluoromethylphenyl)guanine Drug Info [12]
P1-(5'-Adenosyl)P5-(5'-Thymidyl)Pentaphosphate Drug Info [15]
Radiosensitizer gene therapy Drug Info [21]
Thymidine-5'-Phosphate Drug Info [10]
Thymidine-5'-Triphosphate Drug Info [10]
Modulator HQK-1004 Drug Info [22]
Sitimagene ceradenovec Drug Info [23]
Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy Drug Info [24]
TK-DLI Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000912)
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023073)
REF 4ClinicalTrials.gov (NCT02412917) A Comparative Study of FV-100 vs. Valacyclovir for the Prevention of Post-Herpetic Neuralgia. U.S. National Institutes of Health.
REF 5Clinical pipeline report, company report or official report of Advantagene.
REF 6ClinicalTrials.gov (NCT00992732) Study of HQK-1004 and Valganciclovir to Treat Epstein-Barr Virus (EBV) - Positive Lymphoid Malignancies or Lymphoproliferative Disorders. U.S. National Institutes of Health.
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007778)
REF 8ClinicalTrials.gov (NCT00964756) A Study of an Infectivity Enhanced Suicide Gene Expressing Adenovirus for Ovarian Cancer in Patients With Recurrent Ovarian and Other Selected Gynecologic Cancers. U.S. National Institutes of Health.
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015264)
REF 10How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 11J Med Chem. 2006 Dec 28;49(26):7766-73.N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
REF 12Antimicrob Agents Chemother. 2007 Jun;51(6):2028-34. Epub 2007 Apr 16.Sensitivity of monkey B virus (Cercopithecine herpesvirus 1) to antiviral drugs: role of thymidine kinase in antiviral activities of substrate analogs and acyclonucleosides.
REF 13J Med Chem. 2010 Apr 8;53(7):2902-12.3'-[4-Aryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues as potent and selective inhibitors of human mitochondrial thymidine kinase.
REF 14J Med Chem. 2008 Nov 13;51(21):6689-98. Epub 2008 Oct 7.Synthesis, in vitro, and in silico evaluation of organometallic technetium and rhenium thymidine complexes with retained substrate activity toward human thymidine kinase type 1.
REF 15DrugBank 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 16Phase I dose escalation clinical trial of adenovirus vector carrying osteocalcin promoter-driven herpes simplex virus thymidine kinase in localized and metastatic hormone-refractory prostate cancer. Hum Gene Ther. 2003 Feb 10;14(3):227-41.
REF 17Crystal structure of varicella zoster virus thymidine kinase. J Biol Chem. 2003 Jul 4;278(27):24680-7. Epub 2003 Apr 9.
REF 18J Med Chem. 1982 Jun;25(6):644-9.Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes.
REF 19Specific recognition of the bicyclic pyrimidine nucleoside analogs, a new class of highly potent and selective inhibitors of varicella-zoster virus (VZV), by the VZV-encoded thymidine kinase. Mol Pharmacol. 2002 Feb;61(2):249-54.
REF 20Trichomonas vaginalis thymidine kinase: purification, characterization and search for inhibitors. Biochem J. 1998 Aug 15;334 ( Pt 1):15-22.
REF 21Pronounced antitumor effects and tumor radiosensitization of double suicide gene therapy. Clin Cancer Res. 1997 Nov;3(11):2081-8.
REF 22Induction of the Epstein-Barr virus thymidine kinase gene with concomitant nucleoside antivirals as a therapeutic strategy for Epstein-Barr virus-associated malignancies. Curr Opin Oncol. 2001 Sep;13(5):360-7.
REF 23Sitimagene ceradenovec: a gene-based drug for the treatment of operable high-grade glioma. Future Oncol. 2010 Nov;6(11):1691-710.
REF 24Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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