Details of the Target

General Information of Target

Target ID LDTP00420
Target Name Telomerase reverse transcriptase (TERT)
Gene Name TERT
Gene ID 7015
Synonyms
EST2; TCS1; TRT; Telomerase reverse transcriptase; EC 2.7.7.49; HEST2; Telomerase catalytic subunit; Telomerase-associated protein 2; TP2
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPRAPRCRAVRSLLRSHYREVLPLATFVRRLGPQGWRLVQRGDPAAFRALVAQCLVCVPW
DARPPPAAPSFRQVSCLKELVARVLQRLCERGAKNVLAFGFALLDGARGGPPEAFTTSVR
SYLPNTVTDALRGSGAWGLLLRRVGDDVLVHLLARCALFVLVAPSCAYQVCGPPLYQLGA
ATQARPPPHASGPRRRLGCERAWNHSVREAGVPLGLPAPGARRRGGSASRSLPLPKRPRR
GAAPEPERTPVGQGSWAHPGRTRGPSDRGFCVVSPARPAEEATSLEGALSGTRHSHPSVG
RQHHAGPPSTSRPPRPWDTPCPPVYAETKHFLYSSGDKEQLRPSFLLSSLRPSLTGARRL
VETIFLGSRPWMPGTPRRLPRLPQRYWQMRPLFLELLGNHAQCPYGVLLKTHCPLRAAVT
PAAGVCAREKPQGSVAAPEEEDTDPRRLVQLLRQHSSPWQVYGFVRACLRRLVPPGLWGS
RHNERRFLRNTKKFISLGKHAKLSLQELTWKMSVRDCAWLRRSPGVGCVPAAEHRLREEI
LAKFLHWLMSVYVVELLRSFFYVTETTFQKNRLFFYRKSVWSKLQSIGIRQHLKRVQLRE
LSEAEVRQHREARPALLTSRLRFIPKPDGLRPIVNMDYVVGARTFRREKRAERLTSRVKA
LFSVLNYERARRPGLLGASVLGLDDIHRAWRTFVLRVRAQDPPPELYFVKVDVTGAYDTI
PQDRLTEVIASIIKPQNTYCVRRYAVVQKAAHGHVRKAFKSHVSTLTDLQPYMRQFVAHL
QETSPLRDAVVIEQSSSLNEASSGLFDVFLRFMCHHAVRIRGKSYVQCQGIPQGSILSTL
LCSLCYGDMENKLFAGIRRDGLLLRLVDDFLLVTPHLTHAKTFLRTLVRGVPEYGCVVNL
RKTVVNFPVEDEALGGTAFVQMPAHGLFPWCGLLLDTRTLEVQSDYSSYARTSIRASLTF
NRGFKAGRNMRRKLFGVLRLKCHSLFLDLQVNSLQTVCTNIYKILLLQAYRFHACVLQLP
FHQQVWKNPTFFLRVISDTASLCYSILKAKNAGMSLGAKGAAGPLPSEAVQWLCHQAFLL
KLTRHRVTYVPLLGSLRTAQTQLSRKLPGTTLTALEAAANPALPSDFKTILD
Target Type
Successful
Target Bioclass
Enzyme
Family
Reverse transcriptase family, Telomerase subfamily
Subcellular location
Nucleus, nucleolus
Function
Telomerase is a ribonucleoprotein enzyme essential for the replication of chromosome termini in most eukaryotes. 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.
TTD ID
T48945
Uniprot ID
O14746
DrugMap ID
TTUJFD0
Ensemble ID
ENST00000310581.10
HGNC ID
HGNC:11730
ChEMBL ID
CHEMBL2916

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.D848G .
CAL27 SNV: p.S284F .
COLO792 SNV: p.L769P .
DAOY SNV: p.R972H .
HCT116 SNV: p.E484K .
HDQP1 SNV: p.L520V; p.V746M .
HEC1 SNV: p.R521H .
HEC1B SNV: p.R521H .
HT115 SNV: p.D701G .
ICC3 SNV: p.S165R .
IM95 SNV: p.G926C .
KASUMI1 SNV: p.G192V .
KU1919 SNV: p.G225R .
LNCaP clone FGC SNV: p.R865C .
MCC13 Substitution: p.A801T .
MFE319 SNV: p.A615V .
NCIH716 SNV: p.A98T .
REH SNV: p.T262M .
RL952 SNV: p.V639I .
SKNSH SNV: p.H294P .
SNU1 Deletion: p.E113RfsTer15 .
SW620 Substitution: p.S656K .
TOV21G SNV: p.H17Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
BTD
 Probe Info  		C89(0.79)  LDD2120  [1]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		N.A.  LDD0137  [2]
STS-2
 Probe Info  		N.A.  LDD0138  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C89(0.79)  LDD2120  [1]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C89(0.90)  LDD2128  [1]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C89(0.58)  LDD2143  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Regulator of nonsense transcripts 1 (UPF1) DNA2/NAM7 helicase family Q92900
Telomerase reverse transcriptase (TERT) Reverse transcriptase family O14746
RuvB-like 1 (RUVBL1) RuvB family Q9Y265
Transcription activator BRG1 (SMARCA4) SNF2/RAD54 helicase family P51532
Guanine nucleotide-binding protein-like 3 (GNL3) TRAFAC class YlqF/YawG GTPase family Q9BVP2
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Catenin beta-1 (CTNNB1) Beta-catenin family P35222
Nucleophosmin (NPM1) Nucleoplasmin family P06748
PIN2/TERF1-interacting telomerase inhibitor 1 (PINX1) PINX1 family Q96BK5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Doxorubicin Small molecular drug D07VLY
Fluorouracil Small molecular drug D05LEO
Zidovudine Small molecular drug DB00495
Investigative
Click To Hide/Show 54 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cantide + Cisplatin Combination drug (Antisense drug) D08ZRW
1,3-bis(3,4-dihydroxyphenyl)Prop-2-en-1-one Small molecular drug D0Y2RR
2,3-dimethylnaphtho[2,3-f]Quinoxaline-7,12-dione Small molecular drug D04LTV
2,7-bis(3-chloropropionamido)Anthraquinone Small molecular drug D05IBW
2,7-bis(4-chlorobutyramido)Anthraquinone Small molecular drug D0F5MA
2,7-bis(Acetamido)Anthraquinone Small molecular drug D00EWP
2,7-bis(Benzoamido)Anthraquinone Small molecular drug D0S6JQ
2,7-bis(Butyramido)Anthraquinone Small molecular drug D0WJ5T
2,7-bis(Chloroacetamido)Anthraquinone Small molecular drug D07ZRU
2,7-bis(Cyclohexanecarbonamido)Anthraquinone Small molecular drug D00FCF
2,7-bis(Cyclopentanecarbonamido)Anthraquinone Small molecular drug D0T2JN
2,7-bis(Cyclopropanecarbonamido)Anthraquinone Small molecular drug D01MWX
2,7-bis(Phenylacetamido)Anthraquinone Small molecular drug D01TRI
2,7-bis(Phenylpropionamido)Anthraquinone Small molecular drug D0KQ6U
2,7-bis(Propionamido)Anthraquinone Small molecular drug D0D0OX
2,7-bis[2-(Butylamino)Acetamido]Anthraquinone Small molecular drug D02ZIO
2,7-bis[2-(Diethylamino)Acetamido]Anthraquinone Small molecular drug D0G6CD
2,7-bis[2-(Dimethylamino)Acetamido]Anthraquinone Small molecular drug D0VR4A
2,7-bis[2-(Ethylamino)Acetamido]Anthraquinone Small molecular drug D0Y5IW
2,7-bis[2-(Isobutylamino)Acetamido]Anthraquinone Small molecular drug D0C9HB
2,7-bis[2-(Isopropylamino)Acetamido]Anthraquinone Small molecular drug D00SLR
2,7-bis[2-(Piperazino)Acetamido]Anthraquinone Small molecular drug D05RCG
2,7-bis[2-(Piperidino)Acetamido]Anthraquinone Small molecular drug D0B2YF
2,7-bis[2-(Propylamino)Acetamido]Anthraquinone Small molecular drug D0Z5AO
2,7-bis[2-(Pyrrolidino)Acetamido]Anthraquinone Small molecular drug D0IT1P
2,7-bis[3-(Butylamino)Propionamido]Anthraquinone Small molecular drug D06GHM
2,7-bis[3-(Ethylamino)Propionamido]Anthraquinone Small molecular drug D04SKW
2,7-bis[3-(Piperazino)Propionamido]Anthraquinone Small molecular drug D0C0TI
2,7-bis[3-(Piperidino)Propionamido]Anthraquinone Small molecular drug D01BAK
2,7-bis[3-(Propylamino)Propionamido]Anthraquinone Small molecular drug D06TSI
2,7-bis[3-(Pyrrolidino)Propionamido]Anthraquinone Small molecular drug D04KDW
2,7-diaminoanthraquinone Small molecular drug D0G7NE
2,7-dinitroantraquinone Small molecular drug D07DAX
2-butyl-1(3)H-anthra[1,2-d]Imidazole-6,11-dione Small molecular drug D0EB4X
2-heptyl-1(3)H-anthra[1,2-d]Imidazole-6,11-dione Small molecular drug D0JR3Y
2-methyl-1(3)H-anthrasimidazole-6,11-dione Small molecular drug D03SFB
7,8,3',4'-tetrahydroxyflavone Small molecular drug D0X5LN
Aurasperone A Small molecular drug D09PHV
Hoe-33258 Small molecular drug D0E8ZH
Lividomycin A Small molecular drug D07SQW
Nsc-745794 Small molecular drug D09VFQ
Nsc-745795 Small molecular drug D0P7KL
Nsc-745796 Small molecular drug D0M7VY
Nsc-745797 Small molecular drug D0Q8SP
Nsc-745798 Small molecular drug D04STF
Nsc-745799 Small molecular drug D0M6GY
Nsc-745883 Small molecular drug D0T1ZM
Nsc-745884 Small molecular drug D01AAD
Nsc-745885 Small molecular drug D0I6UM
Nsc-745886 Small molecular drug D09IJN
Nsc-745887 Small molecular drug D02CSC
Nsc-745888 Small molecular drug D0I0CU
Grn163l . DB05036
Tertomotide . DB12747

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
2 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.