QTRT1

Summary

QTRT1 (queuine tRNA-ribosyltransferase catalytic subunit 1, HGNC:23797) is a protein-coding gene on chromosome 19p13.3, encoding Queuine tRNA-ribosyltransferase catalytic subunit 1 (Q9BXR0). Catalytic subunit of the queuine tRNA-ribosyltransferase (TGT) that catalyzes the base-exchange of a guanine (G) residue with queuine (Q) at position 34 (anticodon wobble position) in tRNAs with GU(N) anticodons (tRNA-Asp, -Asn, -His and -Tyr), resulting in the hypermodified nuc….

This gene encodes the catalytic subunit of tRNA-guanine transglycosylase. tRNA-guanine transglycosylase is a heterodimeric enzyme complex that plays a critical role in tRNA modification by synthesizing the 7-deazaguanosine queuosine, which is found in tRNAs that code for asparagine, aspartic acid, histidine and tyrosine. A pseudogene of this gene is located on the long arm of chromosome X.

Source: NCBI Gene 81890 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 93 total
• Druggable target: yes
• MANE Select transcript: NM_031209

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23797
Approved symbol	QTRT1
Name	queuine tRNA-ribosyltransferase catalytic subunit 1
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Aliases	TGT
Ensembl gene	ENSG00000213339
Ensembl biotype	protein_coding
OMIM	609615
Entrez	81890

Gene structure

Transcript identifiers

Ensembl transcripts: 19 — 11 protein_coding, 5 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000250237, ENST00000421333, ENST00000585885, ENST00000587500, ENST00000587599, ENST00000587861, ENST00000589488, ENST00000590705, ENST00000591643, ENST00000592254, ENST00000592376, ENST00000592531, ENST00000906542, ENST00000931295, ENST00000931296, ENST00000931297, ENST00000931298, ENST00000931299, ENST00000950801

RefSeq mRNA: 1 — MANE Select: NM_031209 NM_031209

CCDS: CCDS12248

Canonical transcript exons

ENST00000250237 — 10 exons

Exon	Start	End
ENSE00000677420	10712161	10712299
ENSE00001274403	10712553	10712628
ENSE00002740461	10713118	10713365
ENSE00002784706	10701439	10701703
ENSE00003500322	10702116	10702254
ENSE00003538154	10701950	10702018
ENSE00003576710	10712758	10712867
ENSE00003596905	10707302	10707380
ENSE00003598008	10707500	10707615
ENSE00003617591	10712953	10713040

Expression profiles

Bgee: expression breadth ubiquitous, 211 present calls, max score 97.91.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 19.1305 / max 244.6538, expressed in 1801 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
173844	18.9601	1801
173847	0.1047	14
173848	0.0330	6
173846	0.0327	6

Top tissues by expression

266 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
mucosa of transverse colon	UBERON:0004991	97.91	gold quality
body of pancreas	UBERON:0001150	97.89	gold quality
right uterine tube	UBERON:0001302	97.67	gold quality
right hemisphere of cerebellum	UBERON:0014890	97.56	gold quality
cerebellar hemisphere	UBERON:0002245	97.33	gold quality
cerebellar cortex	UBERON:0002129	97.25	gold quality
adenohypophysis	UBERON:0002196	96.52	gold quality
right frontal lobe	UBERON:0002810	96.48	gold quality
left ovary	UBERON:0002119	96.45	gold quality
right lobe of thyroid gland	UBERON:0001119	96.43	gold quality
left lobe of thyroid gland	UBERON:0001120	96.34	gold quality
transverse colon	UBERON:0001157	96.22	gold quality
nucleus accumbens	UBERON:0001882	96.16	gold quality
right ovary	UBERON:0002118	95.92	gold quality
lower esophagus mucosa	UBERON:0035834	95.91	gold quality
metanephros cortex	UBERON:0010533	95.75	gold quality
anterior cingulate cortex	UBERON:0009835	95.70	gold quality
cerebellum	UBERON:0002037	95.63	gold quality
cingulate cortex	UBERON:0003027	95.59	gold quality
endocervix	UBERON:0000458	95.54	gold quality
right adrenal gland	UBERON:0001233	95.40	gold quality
left adrenal gland cortex	UBERON:0035825	95.38	gold quality
tibial nerve	UBERON:0001323	95.35	gold quality
right adrenal gland cortex	UBERON:0035827	95.30	gold quality
pituitary gland	UBERON:0000007	95.29	gold quality
left adrenal gland	UBERON:0001234	95.19	gold quality
amygdala	UBERON:0001876	95.18	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	95.16	gold quality
small intestine Peyer’s patch	UBERON:0003454	95.07	gold quality
thyroid gland	UBERON:0002046	94.92	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 6)

• TGT is composed of a catalytic subunit, QTRT1, and QTRTD1, not USP14. QTRTD1 has been implicated as the salvage enzyme that generates free queuine from QMP. (PMID:20354154)
• phylogenetic and kinetic analyses support the conclusion that all tRNA-guanine transglycosylases have divergently evolved to specifically recognize their cognate heterocyclic substrates. (PMID:21131277)
• the inhibition of the human TGT by biopterin, consistent with earlier reports on other eukaryal TGTs, and supportive of the concept that pteridines may regulate eukaryal TGT activity in vivo. (PMID:21640076)
• Homology models of C elegans Tgt and human Tgt suggest that the replacement of Cys158 and Val233 in bacterial Tgt (Zymomonas mobilis) by valine and accordingly glycine in eucaryotic Tgt largely accounts for the different substrate specificities. (PMID:23704982)
• The human tRNA-guanine transglycosylase displays promiscuous nucleobase preference but strict tRNA specificity. (PMID:34009357)
• Structural and functional insights into tRNA recognition by human tRNA guanine transglycosylase. (PMID:38181786)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	qtrt1	ENSDARG00000043105
mus_musculus	Qtrt1	ENSMUSG00000002825
rattus_norvegicus	Qtrt1	ENSRNOG00000007158
drosophila_melanogaster	Tgt	FBGN0031321
caenorhabditis_elegans		WBGENE00006566

Paralogs (1): QTRT2 (ENSG00000151576)

Protein

Protein identifiers

Queuine tRNA-ribosyltransferase catalytic subunit 1 — Q9BXR0 (reviewed: Q9BXR0)

Alternative names: Guanine insertion enzyme, tRNA-guanine transglycosylase

All UniProt accessions (5): Q9BXR0, K7EJ21, K7EL95, K7EPI1, K7ESP6

UniProt curated annotations — full annotation on UniProt →

Function. Catalytic subunit of the queuine tRNA-ribosyltransferase (TGT) that catalyzes the base-exchange of a guanine (G) residue with queuine (Q) at position 34 (anticodon wobble position) in tRNAs with GU(N) anticodons (tRNA-Asp, -Asn, -His and -Tyr), resulting in the hypermodified nucleoside queuosine (7-(((4,5-cis-dihydroxy-2-cyclopenten-1-yl)amino)methyl)-7-deazaguanosine). Catalysis occurs through a double-displacement mechanism. The nucleophile active site attacks the C1’ of nucleotide 34 to detach the guanine base from the RNA, forming a covalent enzyme-RNA intermediate. The proton acceptor active site deprotonates the incoming queuine, allowing a nucleophilic attack on the C1’ of the ribose to form the product. Modification of cytoplasmic tRNAs with queuosine controls the elongation speed of cognate codons, thereby ensuring the correct folding of nascent proteins to maintain proteome integrity.

Subunit / interactions. Heterodimer of a catalytic subunit QTRT1 and an accessory subunit QTRT2.

Subcellular location. Cytoplasm. Mitochondrion outer membrane.

Similarity. Belongs to the queuine tRNA-ribosyltransferase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9BXR0-1	1	yes
Q9BXR0-2	2

RefSeq proteins (1): NP_112486* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002616	tRNA_ribo_trans-like	Domain
IPR004803	TGT	Family
IPR036511	TGT-like_sf	Homologous_superfamily

Pfam: PF01702

Enzyme classification (BRENDA):

• EC 2.4.2.29 — tRNA-guanosine34 preQ1 transglycosylase (BRENDA: 15 organisms, 100 substrates, 94 inhibitors, 36 Km, 29 kcat entries)
• EC 2.4.2.64 — tRNA-guanosine34 queuine transglycosylase (BRENDA: 15 organisms, 38 substrates, 46 inhibitors, 29 Km, 21 kcat entries)

Substrate kinetics (BRENDA)

23 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
GUANINE	0.0001–0.105	12
GUANINE	0.0001–0.0063	11
QUEUINE	0.0003–0.0023	5
TRNA	0.0001–0.0005	4
[TRNATYR]7-AMINOMETHYL-7-CARBAGUANINE	0.001–0.0022	3
XANTHINE	0.0026–0.224	3
PRE-QUEUINE 0	0.0005–0.0009	2
PRE-QUEUINE 1	0.0007–0.032	2
TRNA GUANINE	0.0009–0.001	2
TRNA(TYR)	0.0003–0.0097	2
[TRNA]-GUANINE	0.0004–0.001	2
7-AMINOMETHYL-7-CARBAGUANINE	0.0223–0.132	2
GUANINE34 IN TRNA	0.0004–0.001	2
HYPOXANTHINE	0.49–1.55	2
2-AMINO-5-(FLUOROMETHYL)PYRROLO[2,3-D]PYRIMIDIN-	0.152	1

Catalyzed reactions (Rhea), 1 shown:

• guanosine(34) in tRNA + queuine = queuosine(34) in tRNA + guanine (RHEA:16633)

UniProt features (60 total): strand 22, helix 18, binding site 8, modified residue 2, splice variant 2, region of interest 2, active site 2, initiator methionine 1, chain 1, mutagenesis site 1, turn 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
6H45	X-RAY DIFFRACTION	2.4
6H42	X-RAY DIFFRACTION	2.45
7NQ4	X-RAY DIFFRACTION	2.88
8OMR	ELECTRON MICROSCOPY	3.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9BXR0-F1	94.07	0.87

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (2): 105 (proton acceptor); 279 (nucleophile)

Ligand- & substrate-binding residues (8): 317; 319; 322; 348; 105; 159; 202; 229

Post-translational modifications (2): 2, 139

Mutagenesis-validated functional residues (1):

Position	Phenotype
279	loss of transglycosylase activity.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-6782315	tRNA modification in the nucleus and cytosol
R-HSA-72306	tRNA processing
R-HSA-8953854	Metabolism of RNA

MSigDB gene sets: 152 (showing top): GOBP_TRNA_METABOLIC_PROCESS, GOBP_RNA_MODIFICATION, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1, MYCMAX_01, GOCC_MITOCHONDRIAL_ENVELOPE, RFX1_02, GOBP_TRNA_PROCESSING, REACTOME_METABOLISM_OF_RNA, GOBP_TRNA_MODIFICATION, GOCC_CYTOPLASMIC_SIDE_OF_MEMBRANE, GINESTIER_BREAST_CANCER_ZNF217_AMPLIFIED_DN, GOCC_TRANSFERASE_COMPLEX, GOCC_SIDE_OF_MEMBRANE, SANSOM_APC_MYC_TARGETS, SANSOM_APC_TARGETS_REQUIRE_MYC

GO Biological Process (4): tRNA wobble guanine modification (GO:0002099), tRNA modification (GO:0006400), tRNA processing (GO:0008033), obsolete tRNA-guanine transglycosylation (GO:0101030)

GO Molecular Function (7): tRNA-guanosine(34) queuine transglycosylase activity (GO:0008479), metal ion binding (GO:0046872), protein binding (GO:0005515), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757), protein homodimerization activity (GO:0042803), protein heterodimerization activity (GO:0046982)

GO Cellular Component (9): nucleus (GO:0005634), cytoplasm (GO:0005737), mitochondrion (GO:0005739), mitochondrial outer membrane (GO:0005741), cytoplasmic side of mitochondrial outer membrane (GO:0032473), tRNA-guanine transglycosylase complex (GO:0120507), transferase complex (GO:1990234), membrane (GO:0016020), protein-containing complex (GO:0032991)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
tRNA processing	1
Metabolism of RNA	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein dimerization activity	2
intracellular membrane-bounded organelle	2
cellular anatomical structure	2
tRNA wobble base modification	1
tRNA processing	1
RNA modification	1
RNA processing	1
tRNA metabolic process	1
pentosyltransferase activity	1
catalytic activity, acting on a tRNA	1
cation binding	1
binding	1
catalytic activity	1
transferase activity	1
identical protein binding	1
intracellular anatomical structure	1
cytoplasm	1
mitochondrial membrane	1
organelle outer membrane	1
mitochondrial outer membrane	1
cytoplasmic side of membrane	1
transferase complex	1
catalytic complex	1
cellular_component	1

Protein interactions and networks

STRING

1506 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
QTRT1	USP14	P54578	962
QTRT1	QTRT2	Q9H974	894
QTRT1	USP8	P40818	769
QTRT1	USP6	P35125	768
QTRT1	TRDMT1	O14717	679
QTRT1	TRMT5	Q32P41	563
QTRT1	NSUN2	Q08J23	553
QTRT1	GTPBP3	Q969Y2	540
QTRT1	TRIT1	Q9H3H1	528
QTRT1	METTL1	Q9UBP6	528
QTRT1	ADAT3	Q96EY9	506
QTRT1	NTAQ1	Q96HA8	492
QTRT1	PUS1	Q9Y606	489
QTRT1	TRUB1	Q8WWH5	488
QTRT1	TRMT10A	Q8TBZ6	478

IntAct

27 interactions, top by confidence:

A	B	Type	Score
QTRT2	QTRT1	psi-mi:“MI:0407”(direct interaction)	0.560
THUMPD1	YBX1	psi-mi:“MI:0914”(association)	0.530
CLEC11A	VWA8	psi-mi:“MI:0914”(association)	0.530
PA	QTRT1	psi-mi:“MI:0915”(physical association)	0.370
CLEC11A	VWA8	psi-mi:“MI:0914”(association)	0.350
QTRT1	APBB1	psi-mi:“MI:0914”(association)	0.350
ORF4a	MPHOSPH10	psi-mi:“MI:0914”(association)	0.350
TAS1R2	UPK3BL1	psi-mi:“MI:0914”(association)	0.350
NOG	TCAF2	psi-mi:“MI:0914”(association)	0.350
ISCA1	BACH1	psi-mi:“MI:0914”(association)	0.350
QTRT1	ACSL4	psi-mi:“MI:0914”(association)	0.350
THUMPD1	H2AX	psi-mi:“MI:0914”(association)	0.350
ILF3	ESYT2	psi-mi:“MI:2364”(proximity)	0.270
SMNDC1	SMCHD1	psi-mi:“MI:2364”(proximity)	0.270
ARF6	QTRT1	psi-mi:“MI:0915”(physical association)	0.000
LCOR	QTRT1	psi-mi:“MI:0915”(physical association)	0.000
QTRT1	COPS6	psi-mi:“MI:0915”(physical association)	0.000
QTRT1	SETDB1	psi-mi:“MI:0915”(physical association)	0.000
QTRT1	SH3GL3	psi-mi:“MI:0915”(physical association)	0.000
QTRT1	UNC119	psi-mi:“MI:0915”(physical association)	0.000
QTRT1	ZBTB16	psi-mi:“MI:0915”(physical association)	0.000
NDUFA4L2	QTRT1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (57): PLS1 (Affinity Capture-MS), PRAME (Affinity Capture-MS), HSPD1 (Affinity Capture-MS), APBB2 (Affinity Capture-MS), APBB1 (Affinity Capture-MS), POLE4 (Affinity Capture-MS), QTRT1 (Affinity Capture-MS), QTRT1 (Affinity Capture-MS), QTRT1 (Co-fractionation), QTRT1 (Reconstituted Complex), QTRT1 (Affinity Capture-MS), APBB2 (Affinity Capture-MS), PRAME (Affinity Capture-MS), APBB1 (Affinity Capture-MS), PLS1 (Affinity Capture-MS)

ESM2 similar proteins: A2YII8, A8X0P0, O35567, O59736, O74940, O80585, O82191, O94460, P12628, P23368, P29696, P31335, P31939, P37222, P37223, P38795, P43279, P51615, P79023, Q01637, Q09755, Q0D8D4, Q0VCK0, Q19360, Q23623, Q25479, Q4QQY7, Q54ML1, Q54V77, Q5R5C2, Q6FXK9, Q6NUA1, Q754E7, Q7SYK1, Q84WV8, Q8RWM2, Q93714, Q941T1, Q945K7, Q99KE1

Diamond homologs: A0AIX9, A0LFR2, A0RJ24, A2SM97, A3DE13, A4IRA9, A4J541, A4VW51, A4W2F8, A5D3G6, A5EW66, A5ITG3, A6QHI1, A6U2A7, A7GT99, A7X354, A7Z766, A8FFQ9, A8X0P0, A8Z2G7, A9VIP3, B0K0M1, B0K959, B1HVA1, B1I9B4, B2A5K8, B5F9Y3, B6EK65, B7GFN1, B7HE51, B7HQH6, B7IIS9, B7JQ03, B8CXG0, B8DHL8, B8E2N5, B8FQV2, B8GTQ4, B8HX02, B9DNG7

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

93 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	72
Likely benign	3
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

1527 predictions. Top by Δscore:

Variant	Effect	Δscore
19:10701692:GGTC:G	donor_gain	1.0000
19:10702250:GCTGG:G	donor_gain	1.0000
19:10702253:GG:G	donor_gain	1.0000
19:10702254:GG:G	donor_gain	1.0000
19:10702255:G:GG	donor_gain	1.0000
19:10702256:T:A	donor_loss	1.0000
19:10702298:G:GT	donor_gain	1.0000
19:10707300:A:AG	acceptor_gain	1.0000
19:10707301:G:GG	acceptor_gain	1.0000
19:10707378:CAG:C	donor_gain	1.0000
19:10707381:G:GG	donor_gain	1.0000
19:10712271:G:GT	donor_gain	1.0000
19:10712753:CACA:C	acceptor_loss	1.0000
19:10712756:A:AG	acceptor_gain	1.0000
19:10712756:AGC:A	acceptor_gain	1.0000
19:10712757:G:GG	acceptor_gain	1.0000
19:10712757:GC:G	acceptor_gain	1.0000
19:10712757:GCG:G	acceptor_gain	1.0000
19:10712757:GCGC:G	acceptor_gain	1.0000
19:10712757:GCGCT:G	acceptor_gain	1.0000
19:10712841:G:GT	donor_gain	1.0000
19:10712864:AAAAG:A	donor_loss	1.0000
19:10712865:AAA:A	donor_gain	1.0000
19:10712866:AA:A	donor_gain	1.0000
19:10712868:G:C	donor_loss	1.0000
19:10712868:G:GG	donor_gain	1.0000
19:10712869:T:A	donor_loss	1.0000
19:10712876:G:GT	donor_gain	1.0000
19:10712948:TACA:T	acceptor_loss	1.0000
19:10712950:CA:C	acceptor_loss	1.0000

AlphaMissense

2622 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:10702117:A:T	D105V	1.000
19:10702128:T:C	F109L	1.000
19:10702130:C:A	F109L	1.000
19:10702130:C:G	F109L	1.000
19:10701679:T:A	N73K	0.999
19:10701679:T:G	N73K	0.999
19:10702116:G:C	D105H	0.999
19:10702117:A:C	D105A	0.999
19:10702117:A:G	D105G	0.999
19:10702118:C:A	D105E	0.999
19:10702118:C:G	D105E	0.999
19:10702133:G:C	Q110H	0.999
19:10702133:G:T	Q110H	0.999
19:10707326:A:T	D159V	0.999
19:10707510:T:A	W181R	0.999
19:10707510:T:C	W181R	0.999
19:10712290:T:C	M259T	0.999
19:10712291:G:A	M259I	0.999
19:10712291:G:C	M259I	0.999
19:10712291:G:T	M259I	0.999
19:10712292:G:A	G260R	0.999
19:10712292:G:C	G260R	0.999
19:10712603:A:T	D279V	0.999
19:10712604:C:A	D279E	0.999
19:10712604:C:G	D279E	0.999
19:10713226:T:A	W390R	0.999
19:10713226:T:C	W390R	0.999
19:10701686:C:G	H76D	0.998
19:10702116:G:T	D105Y	0.998
19:10702119:A:C	S106R	0.998

dbSNP variants (sampled 300 via entrez): RS1000521237 (19:10702605 A>G), RS1000553750 (19:10702389 CG>C,CGG), RS1000772615 (19:10709574 G>A,C,T), RS1000888700 (19:10713766 T>C), RS1000919915 (19:10713480 C>T), RS1000971534 (19:10704373 A>C), RS1001097548 (19:10710200 A>G), RS1001188011 (19:10707892 G>A,C,T), RS1001408719 (19:10700803 G>T), RS1001482353 (19:10700523 T>A,C), RS1001513383 (19:10700159 G>A), RS1001835615 (19:10707769 T>G), RS1001844848 (19:10701487 C>G,T), RS1001990775 (19:10707297 A>C,G), RS1002002262 (19:10705744 C>A,T)

Disease associations

OMIM: gene MIM:609615 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST002740_61	Inflammatory skin disease	1.000000e-10
GCST002874_22	Psoriasis	2.000000e-06
GCST007429_90	Lung function (FVC)	3.000000e-06
GCST007432_100	FEV1	8.000000e-11
GCST008103_119	Bipolar disorder	5.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004312	vital capacity
EFO:0004314	forced expiratory volume

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6004 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.68	Ki	2100	nM	CHEMBL6993
5.43	Ki	3700	nM	CHEMBL487739

PubChem BioAssay actives

2 with measured affinity, of 2 total; 2 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2-amino-3H-quinazolin-4-one	405522: Inhibition of TGT	ki	2.1000	uM
6-amino-4-[2-(4-methoxyphenyl)ethyl]-1,7-dihydroimidazo[4,5-g]quinazolin-8-one	405522: Inhibition of TGT	ki	3.7000	uM

CTD chemical–gene interactions

28 total (human), top 28 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases abundance, increases expression, decreases expression, affects cotreatment	3
Arsenic	increases abundance, increases expression, affects methylation, affects cotreatment	2
Valproic Acid	affects expression, increases methylation	2
pirinixic acid	affects binding, decreases expression, increases activity	1
beta-lapachone	decreases expression, increases expression	1
di-n-butylphosphoric acid	affects expression	1
abrine	increases expression	1
(+)-JQ1 compound	decreases expression	1
Resveratrol	affects cotreatment, increases expression	1
Arsenic Trioxide	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Benzo(a)pyrene	decreases methylation	1
Carbamazepine	affects expression	1
Doxorubicin	increases expression	1
Ivermectin	decreases expression	1
Plant Extracts	affects cotreatment, increases expression	1
Ribonucleotides	affects binding	1
Rotenone	decreases expression	1
Selenium	increases expression, affects cotreatment	1
Smoke	decreases expression	1
Tretinoin	decreases expression	1
Urethane	decreases expression	1
Vitamin E	affects cotreatment, increases expression	1
Cyclosporine	decreases expression	1
Okadaic Acid	decreases expression	1
Copper Sulfate	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL958734	Binding	Inhibition of TGT	Recent developments in fragment-based drug discovery. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B2CZ	Abcam HeLa QTRT1 KO	Cancer cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.