Target Information

Target General Infomation
Target ID
T30081 (Former ID: TTDR00500)
Target Name
Thymidine kinase 1 (TK1)
Synonyms
Thymidine kinase, cytosolic
Gene Name
TK1
Target Type
Successful target
 [1]
Disease [+] 2 Target-related Diseases +
1 Acute myeloid leukaemia [ICD-11: 2A60]
2 Human immunodeficiency virus disease [ICD-11: 1C60-1C62]
Function
cytosol, identical protein binding, thymidine kinase activity, zinc ion binding, DNA metabolic process, nucleobase-containing compound metabolic process, protein homotetramerization, pyrimidine nucleoside salvage, thymidine metabolic process
BioChemical Class
Kinase
UniProt ID
KITH_HUMAN
EC Number
EC 2.7.1.21
Sequence
MSCINLPTVLPGSPSKTRGQIQVILGPMFSGKSTELMRRVRRFQIAQYKCLVIKYAKDTR
YSSSFCTHDRNTMEALPACLLRDVAQEALGVAVIGIDEGQFFPDIVEFCEAMANAGKTVI
VAALDGTFQRKPFGAILNLVPLAESVVKLTAVCMECFREAAYTKRLGTEKEVEVIGGADK
YHSVCRLCYFKKASGQPAGPDNKENCPVPGKPGEAVAARKLFAPQQILQCSPAN
Drugs and Modes of Action
Approved Drug(s) [+] 2 Approved Drugs +
1 DEOXYCYTIDINE Drug Info Approved Acute myeloid leukaemia [2], [3]
2 Penciclovir Drug Info Approved Human immunodeficiency virus infection [2], [4]
Clinical Trial Drug(s) [+] 7 Clinical Trial Drugs +
1 TK-DLI Drug Info Preregistration Graft-versus-host disease [5]
2 FV-100 Drug Info Phase 3 Varicella zoster virus infection [6]
3 Radiosensitizer gene therapy Drug Info Phase 3 Pancreatic cancer [7]
4 HQK-1004 Drug Info Phase 2 Solid tumour/cancer [8]
5 Ad-OC-hsvTK/valacyclovir Drug Info Phase 1 Prostate cancer [9]
6 Rilapladib Drug Info Phase 1 Cardiovascular disease [10]
7 Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy Drug Info Phase 1 Solid tumour/cancer [11]
Discontinued Drug(s) [+] 1 Discontinued Drugs +
1 Sitimagene ceradenovec Drug Info Discontinued in Phase 3 Brain cancer [12]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 37 Inhibitor drugs +
1 DEOXYCYTIDINE Drug Info [13]
2 Penciclovir Drug Info [1]
3 FV-100 Drug Info [15]
4 Radiosensitizer gene therapy Drug Info [16]
5 Rilapladib Drug Info [18]
6 Ad-OC-hsvTK/valacyclovir Drug Info [19]
7 (South)-Methanocarba-Thymidine Drug Info [1]
8 1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine Drug Info [22]
9 1-[2-(2-triphenylmethoxyethoxy)ethyl]thymine Drug Info [22]
10 1-[5-(triphenylmethoxy)pentyl]thymine Drug Info [22]
11 1-[6-(triphenylmethoxy)hexyl]thymine Drug Info [22]
12 1-[7-(triphenylmethoxy)heptyl]thymine Drug Info [22]
13 2'-deoxythymidine triphosphate Drug Info [1]
14 2'-Deoxyuridine Drug Info [13]
15 2-phenylamino-9-(4-hydroxy-butyl)-6-oxopurine Drug Info [23]
16 3'-(1,2,3-Triazol-1-yl)-3'-deoxy-beta-D-thymidine Drug Info [24]
17 3-(2-propyn-1-yl)thymidine Drug Info [25]
18 5-Bromothienyldeoxyuridine Drug Info [1]
19 5-Bromovinyldeoxyuridine Drug Info [26]
20 5-Iodo-2'-Deoxyuridine-5'-Monophosphate Drug Info [1]
21 5-Iododeoxyuridine Drug Info [1]
22 5-propyl-2'-deoxyuridine Drug Info [23]
23 6-(Dihydroxy-Isobutyl)-Thymine Drug Info [1]
24 6-Hydroxypropylthymine Drug Info [1]
25 9-(4-Hydroxybutyl)-N2-Phenylguanine Drug Info [1]
26 9-Hydroxypropyladenine, R-Isomer Drug Info [1]
27 9-Hydroxypropyladenine, S-Isomer Drug Info [1]
28 Adenosine-5'-Diphosphate Drug Info [26]
29 BVDU-MP Drug Info [27]
30 Deoxythymidine Drug Info [1]
31 Edoxudine Drug Info [23]
32 ITdU Drug Info [18]
33 L-5-(bromovinyl)deoxyuridine Drug Info [23]
34 L-5-iodo-2'-deoxyuridine Drug Info [23]
35 N2-(3-trifluoromethylphenyl)guanine Drug Info [23]
36 P1-(5'-Adenosyl)P5-(5'-Thymidyl)Pentaphosphate Drug Info [26]
37 Thymidine-5'-Phosphate Drug Info [1]
Modulator [+] 4 Modulator drugs +
1 TK-DLI Drug Info [14]
2 HQK-1004 Drug Info [17]
3 Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy Drug Info [20]
4 Sitimagene ceradenovec Drug Info [21]
Target Regulators
Target-regulating Transcription Factors
Target-regulating Transcription Factors Info 
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Expression Profile Info 
Target-Related Models and Studies
Target Validation
Target Validation Info 
Target QSAR Model
Target QSAR Model 
References
REF 1 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000912)
REF 4 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
REF 5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023073)
REF 6 ClinicalTrials.gov (NCT02412917) A Comparative Study of FV-100 vs. Valacyclovir for the Prevention of Post-Herpetic Neuralgia. U.S. National Institutes of Health.
REF 7 Clinical pipeline report, company report or official report of Advantagene.
REF 8 ClinicalTrials.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 9 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007778)
REF 10 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018454)
REF 11 ClinicalTrials.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 12 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015264)
REF 13 Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes. J Med Chem. 1982 Jun;25(6):644-9.
REF 14 Company report (Takara Bio)
REF 15 Specific 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 16 Pronounced antitumor effects and tumor radiosensitization of double suicide gene therapy. Clin Cancer Res. 1997 Nov;3(11):2081-8.
REF 17 Induction 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 18 Trichomonas vaginalis thymidine kinase: purification, characterization and search for inhibitors. Biochem J. 1998 Aug 15;334 ( Pt 1):15-22.
REF 19 Phase 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 20 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 21 Sitimagene ceradenovec: a gene-based drug for the treatment of operable high-grade glioma. Future Oncol. 2010 Nov;6(11):1691-710.
REF 22 N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors. J Med Chem. 2006 Dec 28;49(26):7766-73.
REF 23 Sensitivity of monkey B virus (Cercopithecine herpesvirus 1) to antiviral drugs: role of thymidine kinase in antiviral activities of substrate anal... Antimicrob Agents Chemother. 2007 Jun;51(6):2028-34.
REF 24 3'-[4-Aryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues as potent and selective inhibitors of human mitochondrial thymidine kinase. J Med Chem. 2010 Apr 8;53(7):2902-12.
REF 25 Synthesis, in vitro, and in silico evaluation of organometallic technetium and rhenium thymidine complexes with retained substrate activity toward ... J Med Chem. 2008 Nov 13;51(21):6689-98.
REF 26 DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
REF 27 Crystal structure of varicella zoster virus thymidine kinase. J Biol Chem. 2003 Jul 4;278(27):24680-7.

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