Target Information
| Target General Information | Top | |||||
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| Target ID |
T48945
(Former ID: TTDR00459)
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| Target Name |
TERT messenger RNA (TERT mRNA)
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| Synonyms |
Telomerase-associated protein 2 (mRNA); Telomerase catalytic subunit (mRNA); TRT (mRNA); TP2 (mRNA); TCS1 (mRNA); HEST2 (mRNA); EST2 (mRNA)
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| Gene Name |
TERT
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Active in progenitor and cancer cells. Inactive, or very low activity, in normal somatic cells. Catalytic component of the teleromerase holoenzyme complex whose main activity is the elongation of telomeres by acting as a reverse transcriptase that adds simple sequence repeats to chromosome ends by copying a template sequence within the RNA component of the enzyme. Catalyzes the RNA-dependent extension of 3'-chromosomal termini with the 6-nucleotide telomeric repeat unit, 5'-TTAGGG-3'. The catalytic cycle involves primer binding, primer extension and release of product once the template boundary has been reached or nascent product translocation followed by further extension. More active on substrates containing 2 or 3 telomeric repeats. Telomerase activity is regulated by a number of factors including telomerase complex-associated proteins, chaperones and polypeptide modifiers. Modulates Wnt signaling. Plays important roles in aging and antiapoptosis. Telomerase is a ribonucleoprotein enzyme essential for the replication of chromosome termini in most eukaryotes.
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| BioChemical Class |
mRNA target
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| UniProt ID | ||||||
| EC Number |
EC 2.7.7.49
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| Sequence |
MPRAPRCRAVRSLLRSHYREVLPLATFVRRLGPQGWRLVQRGDPAAFRALVAQCLVCVPW
DARPPPAAPSFRQVSCLKELVARVLQRLCERGAKNVLAFGFALLDGARGGPPEAFTTSVR SYLPNTVTDALRGSGAWGLLLRRVGDDVLVHLLARCALFVLVAPSCAYQVCGPPLYQLGA ATQARPPPHASGPRRRLGCERAWNHSVREAGVPLGLPAPGARRRGGSASRSLPLPKRPRR GAAPEPERTPVGQGSWAHPGRTRGPSDRGFCVVSPARPAEEATSLEGALSGTRHSHPSVG RQHHAGPPSTSRPPRPWDTPCPPVYAETKHFLYSSGDKEQLRPSFLLSSLRPSLTGARRL VETIFLGSRPWMPGTPRRLPRLPQRYWQMRPLFLELLGNHAQCPYGVLLKTHCPLRAAVT PAAGVCAREKPQGSVAAPEEEDTDPRRLVQLLRQHSSPWQVYGFVRACLRRLVPPGLWGS RHNERRFLRNTKKFISLGKHAKLSLQELTWKMSVRDCAWLRRSPGVGCVPAAEHRLREEI LAKFLHWLMSVYVVELLRSFFYVTETTFQKNRLFFYRKSVWSKLQSIGIRQHLKRVQLRE LSEAEVRQHREARPALLTSRLRFIPKPDGLRPIVNMDYVVGARTFRREKRAERLTSRVKA LFSVLNYERARRPGLLGASVLGLDDIHRAWRTFVLRVRAQDPPPELYFVKVDVTGAYDTI PQDRLTEVIASIIKPQNTYCVRRYAVVQKAAHGHVRKAFKSHVSTLTDLQPYMRQFVAHL QETSPLRDAVVIEQSSSLNEASSGLFDVFLRFMCHHAVRIRGKSYVQCQGIPQGSILSTL LCSLCYGDMENKLFAGIRRDGLLLRLVDDFLLVTPHLTHAKTFLRTLVRGVPEYGCVVNL RKTVVNFPVEDEALGGTAFVQMPAHGLFPWCGLLLDTRTLEVQSDYSSYARTSIRASLTF NRGFKAGRNMRRKLFGVLRLKCHSLFLDLQVNSLQTVCTNIYKILLLQAYRFHACVLQLP FHQQVWKNPTFFLRVISDTASLCYSILKAKNAGMSLGAKGAAGPLPSEAVQWLCHQAFLL KLTRHRVTYVPLLGSLRTAQTQLSRKLPGTTLTALEAAANPALPSDFKTILD Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Doxorubicin | Drug Info | Approved | Solid tumour/cancer | [2], [3] | |
| 2 | Fluorouracil | Drug Info | Approved | Solid tumour/cancer | [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 51 Inhibitor drugs | + | ||||
| 1 | 1,3-bis(3,4-dihydroxyphenyl)prop-2-en-1-one | Drug Info | [4] | |||
| 2 | 2,3-Dimethylnaphtho[2,3-f]quinoxaline-7,12-dione | Drug Info | [5] | |||
| 3 | 2,7-Bis(3-chloropropionamido)anthraquinone | Drug Info | [6] | |||
| 4 | 2,7-Bis(4-chlorobutyramido)anthraquinone | Drug Info | [6] | |||
| 5 | 2,7-Bis(acetamido)anthraquinone | Drug Info | [6] | |||
| 6 | 2,7-Bis(benzoamido)anthraquinone | Drug Info | [6] | |||
| 7 | 2,7-Bis(butyramido)anthraquinone | Drug Info | [6] | |||
| 8 | 2,7-Bis(chloroacetamido)anthraquinone | Drug Info | [6] | |||
| 9 | 2,7-Bis(cyclohexanecarbonamido)anthraquinone | Drug Info | [6] | |||
| 10 | 2,7-Bis(cyclopentanecarbonamido)anthraquinone | Drug Info | [6] | |||
| 11 | 2,7-Bis(cyclopropanecarbonamido)anthraquinone | Drug Info | [6] | |||
| 12 | 2,7-Bis(phenylacetamido)anthraquinone | Drug Info | [6] | |||
| 13 | 2,7-Bis(phenylpropionamido)anthraquinone | Drug Info | [6] | |||
| 14 | 2,7-Bis(propionamido)anthraquinone | Drug Info | [6] | |||
| 15 | 2,7-Bis[2-(butylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 16 | 2,7-Bis[2-(diethylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 17 | 2,7-Bis[2-(dimethylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 18 | 2,7-Bis[2-(ethylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 19 | 2,7-Bis[2-(isobutylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 20 | 2,7-Bis[2-(isopropylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 21 | 2,7-Bis[2-(piperazino)acetamido]anthraquinone | Drug Info | [6] | |||
| 22 | 2,7-Bis[2-(piperidino)acetamido]anthraquinone | Drug Info | [6] | |||
| 23 | 2,7-Bis[2-(propylamino)acetamido]anthraquinone | Drug Info | [6] | |||
| 24 | 2,7-Bis[2-(pyrrolidino)acetamido]anthraquinone | Drug Info | [6] | |||
| 25 | 2,7-Bis[3-(butylamino)propionamido]anthraquinone | Drug Info | [6] | |||
| 26 | 2,7-Bis[3-(ethylamino)propionamido]anthraquinone | Drug Info | [6] | |||
| 27 | 2,7-Bis[3-(piperazino)propionamido]anthraquinone | Drug Info | [6] | |||
| 28 | 2,7-Bis[3-(piperidino)propionamido]anthraquinone | Drug Info | [6] | |||
| 29 | 2,7-Bis[3-(propylamino)propionamido]anthraquinone | Drug Info | [6] | |||
| 30 | 2,7-Bis[3-(pyrrolidino)propionamido]anthraquinone | Drug Info | [6] | |||
| 31 | 2,7-diaminoanthraquinone | Drug Info | [6] | |||
| 32 | 2,7-Dinitroantraquinone | Drug Info | [6] | |||
| 33 | 2-Butyl-1(3)H-anthra[1,2-d]imidazole-6,11-dione | Drug Info | [5] | |||
| 34 | 2-Heptyl-1(3)H-anthra[1,2-d]imidazole-6,11-dione | Drug Info | [5] | |||
| 35 | 2-Methyl-1(3)H-anthrasimidazole-6,11-dione | Drug Info | [5] | |||
| 36 | 7,8,3',4'-tetrahydroxyflavone | Drug Info | [4] | |||
| 37 | AURASPERONE A | Drug Info | [7] | |||
| 38 | HOE-33258 | Drug Info | [8] | |||
| 39 | LIVIDOMYCIN A | Drug Info | [8] | |||
| 40 | NSC-745794 | Drug Info | [5] | |||
| 41 | NSC-745795 | Drug Info | [5] | |||
| 42 | NSC-745796 | Drug Info | [5] | |||
| 43 | NSC-745797 | Drug Info | [5] | |||
| 44 | NSC-745798 | Drug Info | [5] | |||
| 45 | NSC-745799 | Drug Info | [5] | |||
| 46 | NSC-745883 | Drug Info | [5] | |||
| 47 | NSC-745884 | Drug Info | [5] | |||
| 48 | NSC-745885 | Drug Info | [5] | |||
| 49 | NSC-745886 | Drug Info | [5] | |||
| 50 | NSC-745887 | Drug Info | [5] | |||
| 51 | NSC-745888 | Drug Info | [5] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Property Profile of Target | Top | |
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| (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 Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | HTLV-I infection | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | IL2 Signaling Pathway | |||||
| PID Pathway | [+] 5 PID Pathways | + | ||||
| 1 | Validated targets of C-MYC transcriptional activation | |||||
| 2 | Regulation of Telomerase | |||||
| 3 | IL2 signaling events mediated by PI3K | |||||
| 4 | Regulation of nuclear beta catenin signaling and target gene transcription | |||||
| 5 | HIF-1-alpha transcription factor network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Formation of the beta-catenin:TCF transactivating complex | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | TGF beta Signaling Pathway | |||||
| 2 | miR-targeted genes in lymphocytes - TarBase | |||||
| 3 | miR-targeted genes in epithelium - TarBase | |||||
| 4 | Telomere Maintenance | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207. | |||||
| REF 2 | 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: 7069). | |||||
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | Catecholic flavonoids acting as telomerase inhibitors. J Med Chem. 2004 Dec 16;47(26):6466-75. | |||||
| REF 5 | Synthesis, cytotoxicity and human telomerase inhibition activities of a series of 1,2-heteroannelated anthraquinones and anthra[1,2-d]imidazole-6,1... Bioorg Med Chem. 2009 Nov 1;17(21):7418-28. | |||||
| REF 6 | Synthesis, human telomerase inhibition and anti-proliferative studies of a series of 2,7-bis-substituted amido-anthraquinone derivatives. Bioorg Med Chem. 2008 Jul 15;16(14):6976-86. | |||||
| REF 7 | New dimeric naphthopyrones from Aspergillus niger. J Nat Prod. 2003 Jan;66(1):136-9. | |||||
| REF 8 | Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3467-71. | |||||
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