TKT

Summary

TKT (transketolase, HGNC:11834) is a protein-coding gene on chromosome 3p21.1, encoding Transketolase (P29401). Catalyzes the transfer of a two-carbon ketol group from a ketose donor to an aldose acceptor, via a covalent intermediate with the cofactor thiamine pyrophosphate. It is a selective cancer dependency (DepMap: 38.2% of cell lines).

This gene encodes a thiamine-dependent enzyme which plays a role in the channeling of excess sugar phosphates to glycolysis in the pentose phosphate pathway. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.

Source: NCBI Gene 7086 — RefSeq curated summary.

At a glance

• Gene–disease (curated): transketolase deficiency (Strong, GenCC)
• Clinical variants (ClinVar): 131 total — 2 pathogenic, 2 likely-pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 38.2% of screened cell lines
• MANE Select transcript: NM_001064

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11834
Approved symbol	TKT
Name	transketolase
Location	3p21.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000163931
Ensembl biotype	protein_coding
OMIM	606781
Entrez	7086

Gene structure

Transcript identifiers

Ensembl transcripts: 27 — 17 protein_coding, 6 retained_intron, 3 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000423516, ENST00000423525, ENST00000450814, ENST00000460243, ENST00000460343, ENST00000461139, ENST00000462138, ENST00000466765, ENST00000469678, ENST00000472528, ENST00000483706, ENST00000487660, ENST00000494523, ENST00000869610, ENST00000869611, ENST00000869612, ENST00000869613, ENST00000935658, ENST00000935659, ENST00000935660, ENST00000935661, ENST00000935662, ENST00000935663, ENST00000935664, ENST00000935665, ENST00000971004, ENST00000971005

RefSeq mRNA: 3 — MANE Select: NM_001064 NM_001064, NM_001135055, NM_001258028

CCDS: CCDS2871, CCDS58834

Canonical transcript exons

ENST00000462138 — 14 exons

Exon	Start	End
ENSE00001863311	53224712	53225931
ENSE00002276357	53255836	53256022
ENSE00003481595	53241132	53241245
ENSE00003488544	53229007	53229137
ENSE00003489724	53228276	53228359
ENSE00003491015	53226756	53226878
ENSE00003537400	53228056	53228149
ENSE00003558006	53230457	53230621
ENSE00003563912	53234983	53235174
ENSE00003567663	53229280	53229436
ENSE00003578799	53242125	53242242
ENSE00003579380	53233156	53233274
ENSE00003586584	53231357	53231550
ENSE00003614831	53240251	53240348

Expression profiles

Bgee: expression breadth ubiquitous, 301 present calls, max score 99.54.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 535.1975 / max 3614.5788, expressed in 1828 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
42511	511.9851	1828
42510	21.1277	1799
42507	1.1098	648
42509	0.9749	566

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
monocyte	CL:0000576	99.54	gold quality
mononuclear cell	CL:0000842	99.49	gold quality
leukocyte	CL:0000738	99.47	gold quality
granulocyte	CL:0000094	99.30	gold quality
blood	UBERON:0000178	99.19	gold quality
right lobe of thyroid gland	UBERON:0001119	99.03	gold quality
body of pancreas	UBERON:0001150	98.96	gold quality
bone marrow	UBERON:0002371	98.89	gold quality
left lobe of thyroid gland	UBERON:0001120	98.74	gold quality
left adrenal gland	UBERON:0001234	98.61	gold quality
right adrenal gland cortex	UBERON:0035827	98.57	gold quality
esophagus mucosa	UBERON:0002469	98.54	gold quality
left adrenal gland cortex	UBERON:0035825	98.52	gold quality
right adrenal gland	UBERON:0001233	98.50	gold quality
stromal cell of endometrium	CL:0002255	98.43	gold quality
right lung	UBERON:0002167	98.43	gold quality
thyroid gland	UBERON:0002046	98.40	gold quality
adrenal cortex	UBERON:0001235	98.38	gold quality
upper lobe of lung	UBERON:0008948	98.35	gold quality
upper lobe of left lung	UBERON:0008952	98.35	gold quality
lower esophagus mucosa	UBERON:0035834	98.35	gold quality
esophagus	UBERON:0001043	98.33	gold quality
bone marrow cell	CL:0002092	98.31	gold quality
spleen	UBERON:0002106	98.30	gold quality
gall bladder	UBERON:0002110	98.26	gold quality
cortical plate	UBERON:0005343	98.24	gold quality
embryo	UBERON:0000922	98.22	gold quality
lower esophagus	UBERON:0013473	98.14	gold quality
lower esophagus muscularis layer	UBERON:0035833	98.13	gold quality
bone element	UBERON:0001474	98.08	gold quality

Single-cell (SCXA)

Detected in 21 experiment(s), a significant marker in 18.

Experiment	Marker?	Max mean expression
E-MTAB-11121	yes	2620.68
E-MTAB-10662	yes	1911.08
E-MTAB-6678	yes	1342.40
E-MTAB-6819	yes	1206.06
E-HCAD-4	yes	232.12
E-CURD-122	yes	80.11
E-MTAB-10553	yes	37.79
E-MTAB-6701	yes	36.00
E-HCAD-10	yes	34.36
E-MTAB-9467	yes	33.58
E-MTAB-9221	yes	29.66
E-HCAD-9	yes	25.02
E-CURD-112	yes	24.22
E-GEOD-125970	yes	15.90
E-CURD-88	yes	13.23

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, AR, CEBPB, EGR1, ESR1, FOXN1, FOXO1, JUN, KAT5, KLF4, MAX, MITF, MYC, MYF6, NFE2L2, NFKB, PAX1, PAX6, PDX1, PITX2, PRDM2, SP1, STAT5B, TBP, TCF12, TCF15, THRA, THRB, TP53

miRNA regulators (miRDB)

16 targeting TKT, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-613	99.91	71.50	1710
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-3663-3P	99.84	70.39	798
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-513C-5P	99.50	68.42	1730
HSA-MIR-514B-5P	99.50	68.19	1766
HSA-MIR-4518	98.12	66.82	1030
HSA-MIR-3664-3P	97.85	67.62	1452
HSA-MIR-1266-5P	97.71	66.92	1052
HSA-MIR-3127-5P	97.52	65.24	786
HSA-MIR-3918	96.13	64.65	1300

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 38.2% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 28)

• Almost all multiple sclerosis patients had cerebrospinal fluid IgG directed to isoforms of one of the oligodendroglial molecules, transketolase, 2’,3’-cyclic-nucleotide 3’-phosphodiesterase type I, collapsin response mediator protein 2, and tubulin beta4. (PMID:18676363)
• This protein has been found differentially expressed in the dorsolateral prefrontal cortex from patients with schizophrenia. (PMID:19110265)
• This protein has been found differentially expressed in thalami from patients with schizophrenia. (PMID:20471030)
• The crystal structure of human transketolase and new insights into its mode of action. (PMID:20667822)
• Single Nucleotide Polymorphism in transketolase is associated with diabetic nephropathy. (PMID:20826743)
• TKT is a target gene of the BACH1 transcription factor according to ChIP-seq analysis in HEK 293 cells. (PMID:21555518)
• Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme. (PMID:22645655)
• No transketolase activity of TKTDelta38 can be detected for conversion of physiological sugar substrates thus arguing against an intrinsically encoded enzymatic function of TKTL1 in tumor cell metabolism (PMID:23118983)
• Data indicate that transketolase (hTKT). shares 61% sequence identity with transketolase-like protein (TKTL1). (PMID:23261987)
• TKT rs3736156 identified significant differences in the onset of cardiovascular event in patients having genotypes AG + AA versus GG (PMID:23492569)
• basal TK activity was decreased in cases with diabetic neuropathy (PMID:24114639)
• Akt1 phosphorylates TKT on Thr382, markedly enhancing enzyme activity. (PMID:24981175)
• Transketolase is upregulated in metastatic peritoneal implants and promotes ovarian cancer cell proliferation. (PMID:25895698)
• transketolase (TKT)is required for cancer growth because of its ability to affect the production of NAPDH to counteract oxidative stress. (PMID:26811478)
• The observed associations of genetic variation in transketolase enzyme with neuropathic symptoms and reduced thermal sensation in recent-onset diabetes suggest a role of pathways metabolizing glycolytic intermediates in early diabetic neuropathy. (PMID:27103086)
• Mutations in TKT gene is associated with a Syndrome Including Short Stature, Developmental Delay, and Congenital Heart Defects. (PMID:27259054)
• reduced expression of transketolase in pyrimidine 5’-nucleotidase deficient patients (PMID:27381654)
• Over-expressed and hypo-methylated TKT gene is associated with hepatocellular carcinoma. (PMID:27760737)
• results suggest that SH2D5 is an HBV-induced protein capable of binding to TKT, leading to induction of HCC cell proliferation. (PMID:30659097)
• The regulation of TKT by oxythiamine and/or vitamin B1 may therefore be associated with response to the modulation of NET formation by preventing generation of excessive NETs in inflammatory diseases. (PMID:31415630)
• Transketolase Activity in the Formation of the Azinomycin Azabicycle Moiety (PMID:31424204)
• Erythrocyte transketolase deficiency in patients suffering from Crohn’s disease. (PMID:31646581)
• The nuclear translocation of transketolase inhibits the farnesoid receptor expression by promoting the binding of HDAC3 to FXR promoter in hepatocellular carcinoma cell lines. (PMID:31949131)
• Genetic variants in TKT and DERA in the nicotinamide adenine dinucleotide phosphate pathway predict melanoma survival. (PMID:32659474)
• Untargeted metabolomics as an unbiased approach to the diagnosis of inborn errors of metabolism of the non-oxidative branch of the pentose phosphate pathway. (PMID:32828637)
• QM/MM Study of Human Transketolase: Thiamine Diphosphate Activation Mechanism and Complete Catalytic Cycle. (PMID:34161071)
• Transketolase promotes colorectal cancer metastasis through regulating AKT phosphorylation. (PMID:35110545)
• TKT-PARP1 axis induces radioresistance by promoting DNA double-strand break repair in hepatocellular carcinoma. (PMID:38216672)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	tkta	ENSDARG00000029689
mus_musculus	Tkt	ENSMUSG00000021957
rattus_norvegicus	Tkt	ENSRNOG00000016064

Paralogs (4): TKTL1 (ENSG00000007350), BCKDHB (ENSG00000083123), TKTL2 (ENSG00000151005), PDHB (ENSG00000168291)

Protein

Protein identifiers

Transketolase — P29401 (reviewed: P29401)

All UniProt accessions (5): E9PFF2, P29401, F8W888, F8WAX4, V9HWD9

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the transfer of a two-carbon ketol group from a ketose donor to an aldose acceptor, via a covalent intermediate with the cofactor thiamine pyrophosphate.

Subunit / interactions. Homodimer.

Disease relevance. Short stature, developmental delay, and congenital heart defects (SDDHD) [MIM:617044] An autosomal recessive syndrome characterized by short stature, developmental delay, intellectual disability and congenital heart defects including ventricular septal defect, atrial septal defect and patent foramen ovale. Cataract and uveitis are observed in some patients. The disease is caused by variants affecting the gene represented in this entry.

Cofactor. Binds 1 Mg(2+) ion per subunit. Can also utilize other divalent metal cations, such as Ca(2+), Mn(2+) and Co(2+). Binds 1 thiamine pyrophosphate per subunit.

Similarity. Belongs to the transketolase family.

Isoforms (2)

UniProt ID	Names	Canonical?
P29401-1	1	yes
P29401-2	2

RefSeq proteins (3): NP_001055, NP_001128527, NP_001244957 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR005474	Transketolase_N	Domain
IPR005475	Transketolase-like_Pyr-bd	Domain
IPR009014	Transketo_C/PFOR_II	Homologous_superfamily
IPR020826	Transketolase_BS	Binding_site
IPR029061	THDP-binding	Homologous_superfamily
IPR033248	Transketolase_C	Domain
IPR049557	Transketolase_CS	Conserved_site
IPR051424	Transketolase-like	Family

Pfam: PF00456, PF02779, PF02780

Enzyme classification (BRENDA):

• EC 2.2.1.1 — transketolase (BRENDA: 41 organisms, 197 substrates, 77 inhibitors, 215 Km, 72 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
D-XYLULOSE 5-PHOSPHATE	0.0056–4.08	62
D-RIBOSE 5-PHOSPHATE	0.007–7	52
THIAMINE DIPHOSPHATE	0.0003–0.007	14
FRUCTOSE 6-PHOSPHATE	0.0002–11	11
GLYCOLALDEHYDE	0.13–200	8
HYDROXYPYRUVATE	—	7
D-FRUCTOSE 6-PHOSPHATE	0.029–0.72	6
3-FORMYLBENZOIC ACID	1.3–56	5
D-ERYTHROSE 4-PHOSPHATE	0.023–0.36	5
4-FORMYLBENZOIC ACID	13–251	4
XYLULOSE 5-PHOSPHATE	0.0004–0.16	4
3-HYDROXYBENZALDEHYDE	180–390	3
D-RIBOSE-5-PHOSPHATE	0.13–2.75	3
L-ERYTHRULOSE	4.9–8	3
SEDOHEPTULOSE 7-PHOSPHATE	0.031–4	3

Catalyzed reactions (Rhea), 1 shown:

• D-sedoheptulose 7-phosphate + D-glyceraldehyde 3-phosphate = aldehydo-D-ribose 5-phosphate + D-xylulose 5-phosphate (RHEA:10508)

UniProt features (105 total): helix 29, strand 21, binding site 19, modified residue 16, sequence conflict 7, turn 5, site 2, sequence variant 2, chain 1, active site 1, cross-link 1, splice variant 1

Structure

Experimental structures (PDB)

13 structures.

PDB	Method	Resolution (Å)
4KXV	X-RAY DIFFRACTION	0.97
4KXW	X-RAY DIFFRACTION	0.97
4KXU	X-RAY DIFFRACTION	0.98
4KXX	X-RAY DIFFRACTION	1.03
6HAD	X-RAY DIFFRACTION	1.04
6HA3	X-RAY DIFFRACTION	1.08
6RJB	X-RAY DIFFRACTION	1.15
4KXY	X-RAY DIFFRACTION	1.26
8WA8	X-RAY DIFFRACTION	1.48
8WA9	X-RAY DIFFRACTION	1.5
8WAA	X-RAY DIFFRACTION	1.5
3MOS	X-RAY DIFFRACTION	1.75
3OOY	X-RAY DIFFRACTION	2.05

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P29401-F1	97.11	0.97

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 (3): 366 (proton donor); 37 (important for catalytic activity); 258 (important for catalytic activity)

Ligand- & substrate-binding residues (19): 187; 244; 258; 258; 318; 345; 392; 416; 424; 428; 37; 474 …

Post-translational modifications (17): 1, 3, 6, 11, 104, 144, 204, 232, 241, 260, 275, 287, 295, 345, 538, 603, 352

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-163754	Insulin effects increased synthesis of Xylulose-5-Phosphate
R-HSA-71336	Pentose phosphate pathway
R-HSA-9818028	NFE2L2 regulates pentose phosphate pathway genes

MSigDB gene sets: 350 (showing top): GOBP_NADPPLUS_METABOLIC_PROCESS, GOBP_GROWTH, THEILGAARD_NEUTROPHIL_AT_SKIN_WOUND_DN, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, RIZKI_TUMOR_INVASIVENESS_3D_DN, SARRIO_EPITHELIAL_MESENCHYMAL_TRANSITION_DN, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_GLUCOSE_6_PHOSPHATE_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_GENERATION_OF_PRECURSOR_METABOLITES_AND_ENERGY, GOBP_CARBOHYDRATE_DERIVATIVE_BIOSYNTHETIC_PROCESS, ACATTCC_MIR1_MIR206, YAO_TEMPORAL_RESPONSE_TO_PROGESTERONE_CLUSTER_13, GOTZMANN_EPITHELIAL_TO_MESENCHYMAL_TRANSITION_DN

GO Biological Process (6): pentose-phosphate shunt (GO:0006098), pentose-phosphate shunt, non-oxidative branch (GO:0009052), regulation of growth (GO:0040008), glyceraldehyde-3-phosphate biosynthetic process (GO:0046166), D-xylulose 5-phosphate biosynthetic process (GO:1901159), glyceraldehyde-3-phosphate metabolic process (GO:0019682)

GO Molecular Function (9): magnesium ion binding (GO:0000287), transketolase activity (GO:0004802), calcium ion binding (GO:0005509), thiamine pyrophosphate binding (GO:0030976), protein homodimerization activity (GO:0042803), protein binding (GO:0005515), transferase activity (GO:0016740), transketolase or transaldolase activity (GO:0016744), metal ion binding (GO:0046872)

GO Cellular Component (8): nucleoplasm (GO:0005654), peroxisome (GO:0005777), endoplasmic reticulum membrane (GO:0005789), cytosol (GO:0005829), nuclear body (GO:0016604), vesicle (GO:0031982), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Integration of energy metabolism	1
Metabolism of carbohydrates and carbohydrate derivatives	1
Nuclear events mediated by NFE2L2	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
glyceraldehyde-3-phosphate metabolic process	2
organophosphate biosynthetic process	2
carbohydrate derivative biosynthetic process	2
metal ion binding	2
cation binding	2
NADPH regeneration	1
pentose-phosphate shunt, oxidative branch	1
pentose-phosphate shunt, non-oxidative branch	1
glucose 6-phosphate metabolic process	1
D-ribulose-phosphate 3-epimerase activity	1
ribose-5-phosphate isomerase activity	1
transaldolase activity	1
transketolase activity	1
generation of precursor metabolites and energy	1
pentose-phosphate shunt	1
growth	1
regulation of biological process	1
aldehyde biosynthetic process	1
D-xylulose 5-phosphate metabolic process	1
aldehyde metabolic process	1
organophosphate metabolic process	1
carbohydrate derivative metabolic process	1
transketolase or transaldolase activity	1
vitamin binding	1
anion binding	1
quaternary ammonium group binding	1
heterocyclic compound binding	1
sulfur compound binding	1
identical protein binding	1
protein dimerization activity	1
binding	1
catalytic activity	1
transferase activity	1
nuclear lumen	1
microbody	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cytoplasm	1

Protein interactions and networks

STRING

3733 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TKT	TPK1	Q9H3S4	964
TKT	TALDO1	P37837	943
TKT	PGD	P52209	847
TKT	H6PD	O95479	847
TKT	RPIA	P49247	840
TKT	RPE	Q96AT9	822
TKT	G6PD	P11413	819
TKT	RPEL1	Q2QD12	783
TKT	TPI1	P00938	781
TKT	GPI	P06744	760
TKT	PC	P11498	722
TKT	GAPDH	P00354	706
TKT	XYLB	O75191	702
TKT	PGLS	O95336	701
TKT	ENO1	P06733	660

IntAct

119 interactions, top by confidence:

A	B	Type	Score
ATG5	ATG12	psi-mi:“MI:0914”(association)	0.800
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
TUBA1B	TXNDC9	psi-mi:“MI:0914”(association)	0.640
CFTR	HAX1	psi-mi:“MI:0914”(association)	0.610
TKT	POTEF	psi-mi:“MI:0914”(association)	0.530
DMWD	GAK	psi-mi:“MI:0914”(association)	0.530
ATG2B	TKT	psi-mi:“MI:0914”(association)	0.530
SV2A	EXTL3	psi-mi:“MI:0914”(association)	0.530
TKT	TERF1	psi-mi:“MI:0915”(physical association)	0.510
Csnk1e		psi-mi:“MI:0915”(physical association)	0.400
Bles03		psi-mi:“MI:0915”(physical association)	0.400
	GNAT3	psi-mi:“MI:0915”(physical association)	0.400
	TK2	psi-mi:“MI:0915”(physical association)	0.400
YWHAZ	TKT	psi-mi:“MI:0915”(physical association)	0.400
MAPK8	TCP1	psi-mi:“MI:0914”(association)	0.350
Strn3	STK24	psi-mi:“MI:0914”(association)	0.350
EXOSC9	MPHOSPH6	psi-mi:“MI:0914”(association)	0.350
PRKCD	TRAPPC13	psi-mi:“MI:0914”(association)	0.350
JUN	TPM3	psi-mi:“MI:0914”(association)	0.350
PHOSPHO1	DDX39A	psi-mi:“MI:0914”(association)	0.350
BCAR1	PSMD11	psi-mi:“MI:0914”(association)	0.350
BCAR1	MYO1C	psi-mi:“MI:0914”(association)	0.350

BioGRID (425): TKT (Affinity Capture-MS), TKT (Affinity Capture-MS), ACAA2 (Co-fractionation), ACP1 (Co-fractionation), AKR1A1 (Co-fractionation), AKR1B1 (Co-fractionation), AKR1B15 (Co-fractionation), LOC101930400 (Co-fractionation), AKR1C2 (Co-fractionation), ALDH4A1 (Co-fractionation), ALDOA (Co-fractionation), CALR (Co-fractionation), COX17 (Co-fractionation), DUT (Co-fractionation), ENO1 (Co-fractionation)

ESM2 similar proteins: A0A223HDI5, A3QK15, O00097, P00333, P00504, P04181, P04182, P07754, P08843, P0C0Y4, P0C0Y5, P12863, P14219, P14673, P14674, P14675, P25141, P28032, P29401, P29758, P33097, P34937, P37769, P40142, P41177, P41747, P46226, P48491, P48493, P48494, P48495, P49724, P50137, Q05528, Q07264, Q0II68, Q29RZ0, Q2R8Z5, Q2U919, Q3ZCF5

Diamond homologs: A0AIG6, A1K4R0, A1W4U9, A2C220, A2C9X1, A4SDG1, A5D2Z6, A5N7J2, A6KXB3, A6VKQ3, A7Z6J5, A8FF11, A8FYL0, A9VGD1, B0C8J3, B0JL88, B0TEJ5, B1I3J6, B1WWM7, B1Z1G2, B2A526, B2J5P1, B2V4R3, B4RVY8, B7HB48, B7HNU0, B7IXG8, B7JM28, B7JVJ6, B7KAF7, B8D2I3, B8E247, B8FQ45, B8HWL8, B9E104, B9L1L6, B9MEU8, C0ZC10, C1L2S1, C3LJV1

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
AKT1	“up-regulates activity”	TKT	phosphorylation
AKT	“up-regulates activity”	TKT	phosphorylation
TKT	“down-regulates quantity”	“D-xylulose 5-phosphate(2-)”	“chemical modification”
TKT	“down-regulates quantity”	“D-ribofuranose 5-phosphate(2-)”	“chemical modification”
TKT	“up-regulates quantity”	“sedoheptulose 7-phosphate”	“chemical modification”
TKT	“up-regulates quantity”	“D-glyceraldehyde 3-phosphate(2-)”	“chemical modification”
NFE2L2	“up-regulates quantity by expression”	TKT	“transcriptional regulation”
VRK2	“up-regulates activity”	TKT	phosphorylation
FBXL6	“up-regulates activity”	TKT	ubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 136 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Apoptotic execution phase	5	25.9×	2e-04
Selective autophagy	5	15.1×	2e-03
Aggrephagy	5	13.5×	2e-03
Apoptosis	7	12.8×	2e-04
Programmed Cell Death	7	11.1×	4e-04
Macroautophagy	6	7.5×	6e-03
Signaling by Interleukins	10	7.0×	2e-04
Platelet activation, signaling and aggregation	6	6.9×	1e-02

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of innate immune response	5	21.8×	4e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	2
Uncertain significance	70
Likely benign	21
Benign	13

Top pathogenic / likely-pathogenic (4)

Variant ID	HGVS	Classification
223089	NM_001064.4(TKT):c.633G>A (p.Trp211Ter)	Pathogenic
223091	NM_001064.4(TKT):c.952C>T (p.Arg318Cys)	Pathogenic
3235058	NM_001064.4(TKT):c.181C>T (p.Gln61Ter)	Likely pathogenic
4277802	NM_001064.4(TKT):c.1697-1G>A	Likely pathogenic

SpliceAI

2446 predictions. Top by Δscore:

Variant	Effect	Δscore
3:53225758:AGG:A	donor_gain	1.0000
3:53225782:CAG:C	donor_gain	1.0000
3:53225800:C:A	donor_gain	1.0000
3:53225927:GCCAC:G	acceptor_gain	1.0000
3:53225928:CCAC:C	acceptor_gain	1.0000
3:53225928:CCACC:C	acceptor_gain	1.0000
3:53225929:CAC:C	acceptor_gain	1.0000
3:53225929:CACC:C	acceptor_gain	1.0000
3:53225930:ACC:A	acceptor_loss	1.0000
3:53225931:CCTAG:C	acceptor_loss	1.0000
3:53225932:C:CC	acceptor_gain	1.0000
3:53225933:T:A	acceptor_loss	1.0000
3:53225938:A:AC	acceptor_gain	1.0000
3:53225938:A:C	acceptor_gain	1.0000
3:53226752:TTACC:T	donor_loss	1.0000
3:53226753:TACCT:T	donor_loss	1.0000
3:53226754:A:AC	donor_gain	1.0000
3:53226754:AC:A	donor_gain	1.0000
3:53226754:ACCTT:A	donor_gain	1.0000
3:53226755:C:CA	donor_loss	1.0000
3:53226755:C:CC	donor_gain	1.0000
3:53226755:CC:C	donor_gain	1.0000
3:53226755:CCT:C	donor_gain	1.0000
3:53226755:CCTT:C	donor_gain	1.0000
3:53226755:CCTTC:C	donor_gain	1.0000
3:53226874:CTTTT:C	acceptor_gain	1.0000
3:53226875:TTTT:T	acceptor_gain	1.0000
3:53226876:TTT:T	acceptor_gain	1.0000
3:53226877:TT:T	acceptor_gain	1.0000
3:53226878:TCT:T	acceptor_loss	1.0000

AlphaMissense

4120 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:53229368:G:C	F392L	1.000
3:53229368:G:T	F392L	1.000
3:53229370:A:G	F392L	1.000
3:53229377:A:C	F389L	1.000
3:53229377:A:T	F389L	1.000
3:53229379:A:G	F389L	1.000
3:53229128:C:T	G425E	0.999
3:53229129:C:A	G425W	0.999
3:53229130:G:C	D424E	0.999
3:53229130:G:T	D424E	0.999
3:53229131:T:A	D424V	0.999
3:53229131:T:G	D424A	0.999
3:53229132:C:G	D424H	0.999
3:53229296:G:C	H416Q	0.999
3:53229296:G:T	H416Q	0.999
3:53233172:C:A	K244N	0.999
3:53233172:C:G	K244N	0.999
3:53241141:G:C	H110Q	0.999
3:53241141:G:T	H110Q	0.999
3:53241143:G:C	H110D	0.999
3:53241169:C:A	R101M	0.999
3:53226771:C:G	D561H	0.998
3:53229131:T:C	D424G	0.998
3:53229137:C:T	G422E	0.998
3:53229298:G:C	H416D	0.998
3:53229303:C:T	G414D	0.998
3:53229342:C:G	R401P	0.998
3:53229378:A:C	F389C	0.998
3:53229379:A:T	F389I	0.998
3:53229383:G:C	S387R	0.998

dbSNP variants (sampled 300 via entrez): RS1000110061 (3:53229502 C>T), RS1000248427 (3:53234554 C>G,T), RS1000253863 (3:53251050 C>A,T), RS1000284952 (3:53250838 G>C), RS1000308005 (3:53239647 G>T), RS1000603653 (3:53225066 G>A), RS1000768774 (3:53256778 C>T), RS1000842454 (3:53235568 T>G), RS1001213367 (3:53238955 C>A,G), RS1001282943 (3:53235357 C>T), RS1001377038 (3:53234045 G>A,T), RS1001628956 (3:53256122 G>A,T), RS1001642869 (3:53244393 G>T), RS1001673844 (3:53244263 C>A,G,T), RS1001726604 (3:53238740 C>T)

Disease associations

OMIM: gene MIM:606781 | disease phenotypes: MIM:617044

GenCC curated gene-disease

Disease	Classification	Inheritance
transketolase deficiency	Strong	Autosomal recessive

Mondo (1): transketolase deficiency (MONDO:0014881)

Orphanet (1): Transketolase deficiency (Orphanet:488618)

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4983 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1232461	MOLIBRESIB	2	1,538

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

ChEMBL bioactivities

94 potent at pChembl≥5 of 102 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.52	Kd	3	nM	CHEMBL255138
8.33	EC50	4.7	nM	CHEMBL403691
8.15	Kd	7	nM	CHEMBL255603
8.10	EC50	8	nM	CHEMBL252843
8.10	EC50	8	nM	CHEMBL402594
8.08	EC50	8.3	nM	CHEMBL271044
8.06	EC50	8.7	nM	CHEMBL256627
8.05	EC50	9	nM	CHEMBL401948
8.05	EC50	9	nM	CHEMBL270613
8.00	Kd	10	nM	CHEMBL256627
7.92	EC50	12	nM	CHEMBL440237
7.92	Kd	12	nM	3-DEAZATHIAMINE
7.89	EC50	13	nM	CHEMBL253045
7.82	EC50	15	nM	CHEMBL252845
7.80	Kd	16	nM	CHEMBL403021
7.75	EC50	18	nM	CHEMBL252086
7.68	EC50	21	nM	CHEMBL403212
7.66	Kd	22	nM	CHEMBL401817
7.64	Kd	23	nM	CHEMBL256831
7.60	Kd	25	nM	CHEMBL402329
7.60	Kd	25	nM	CHEMBL402566
7.58	EC50	26	nM	CHEMBL252086
7.57	Kd	27	nM	CHEMBL255340
7.55	EC50	28	nM	CHEMBL252844
7.55	EC50	28	nM	CHEMBL252441
7.55	Kd	28	nM	CHEMBL258077
7.54	Kd	29	nM	CHEMBL256454
7.52	EC50	30	nM	CHEMBL255339
7.50	EC50	32	nM	CHEMBL251888
7.48	Kd	33	nM	CHEMBL252086
7.47	Kd	34	nM	CHEMBL271044
7.44	Kd	36	nM	CHEMBL270632
7.44	Kd	36	nM	CHEMBL403365
7.40	Kd	40	nM	CHEMBL255541
7.34	Kd	46	nM	CHEMBL270613
7.30	EC50	50	nM	CHEMBL258077
7.28	EC50	52	nM	CHEMBL401965
7.28	Kd	53	nM	CHEMBL255542
7.25	EC50	56	nM	CHEMBL402329
7.24	Kd	57	nM	CHEMBL429246
7.22	Kd	60	nM	CHEMBL256177
7.20	Kd	63	nM	CHEMBL401572
7.19	Kd	64	nM	CHEMBL255550
7.19	Kd	64	nM	CHEMBL271521
7.12	Kd	75	nM	CHEMBL403212
6.98	Kd	104	nM	CHEMBL270168
6.96	EC50	110	nM	CHEMBL252637
6.96	Kd	109	nM	CHEMBL270384
6.96	EC50	110	nM	CHEMBL403365
6.94	EC50	116	nM	CHEMBL253044

PubChem BioAssay actives

92 with measured affinity, of 118 total; 50 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
N-[4-amino-5-[[5-(2-hydroxyethyl)-4-methylthiophen-3-yl]methyl]pyrimidin-2-yl]acetamide	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.0030	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethyl acetate	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0047	uM
2-[3-[(6-amino-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0070	uM
N-[(2-amino-6-chloro-3-pyridinyl)methyl]-N-[(Z)-3-[[(Z)-2-[(2-amino-6-chloro-3-pyridinyl)methyl-formylamino]-5-hydroxypent-2-en-3-yl]disulfanyl]-5-hydroxypent-2-en-2-yl]formamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0080	uM
[(Z)-3-acetylsulfanyl-4-[(2-amino-6-methyl-3-pyridinyl)methyl-formylamino]pent-3-enyl] acetate	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0080	uM
2-[3-[(2-amino-4,6-dimethyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0083	uM
2-[3-[(2-amino-6-ethyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0087	uM
2-[3-[(2-amino-6-chloro-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol chloride	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0090	uM
2-[3-[(2-amino-6-chloro-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0090	uM
2-[4-[(4-amino-2-methylpyrimidin-5-yl)methyl]-3-methylthiophen-2-yl]ethanol	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.0120	uM
N-[(2-amino-6-methyl-3-pyridinyl)methyl]-N-[(Z)-3-[[(Z)-2-[(2-amino-6-methyl-3-pyridinyl)methyl-formylamino]-5-hydroxypent-2-en-3-yl]disulfanyl]-5-hydroxypent-2-en-2-yl]formamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0120	uM
N-[(2-amino-6-methyl-3-pyridinyl)methyl]-N-[(Z)-5-hydroxy-3-(2-hydroxyethyldisulfanyl)pent-2-en-2-yl]formamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0130	uM
N-[(2-amino-6-methyl-3-pyridinyl)methyl]-N-[(1Z)-1-(2-oxo-1,3-oxathian-4-ylidene)ethyl]formamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0150	uM
2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-2-oxo-1,3-thiazol-5-yl]ethyl phosphono hydrogen phosphate	320588: Inhibition of apo-transketolase	kd	0.0160	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol chloride	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0180	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-2-ethyl-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0210	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethyl phosphono hydrogen phosphate	320377: Binding affinity to apo-transketolase	kd	0.0220	uM
N-[6-amino-5-[[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium-3-yl]methyl]-2-pyridinyl]acetamide	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0230	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-2,4-dimethyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0250	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-(hydroxymethyl)-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0250	uM
(1S)-1-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethane-1,2-diol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0270	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-2,4-dimethyl-1,3-thiazol-3-ium-5-yl]ethanol chloride	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0280	uM
[(Z)-4-[(2-amino-6-methyl-3-pyridinyl)methyl-formylamino]-3-benzoylsulfanylpent-3-enyl] benzoate	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0280	uM
(1R)-1-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethane-1,2-diol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0280	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0290	uM
1-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium-2-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.0300	uM
N-[(Z)-3-[[(Z)-2-[acetyl-[(2-amino-6-methyl-3-pyridinyl)methyl]amino]-5-hydroxypent-2-en-3-yl]disulfanyl]-5-hydroxypent-2-en-2-yl]-N-[(2-amino-6-methyl-3-pyridinyl)methyl]acetamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0320	uM
2-[3-[(2-amino-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0360	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-2-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0360	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-ethyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0400	uM
3-[[(Z)-2-[(2-amino-6-methyl-3-pyridinyl)methyl-formylamino]-5-hydroxypent-2-en-3-yl]disulfanyl]propanoic acid	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.0520	uM
1-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethane-1,2-diol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0530	uM
6-amino-5-[[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium-3-yl]methyl]pyridine-2-carbonitrile	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0570	uM
2-[4-[(4-amino-2-cyclopropylpyrimidin-5-yl)methyl]-3-methylthiophen-2-yl]ethanol	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.0600	uM
2-[4-[[4-amino-2-(trifluoromethyl)pyrimidin-5-yl]methyl]-3-methylthiophen-2-yl]ethanol	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.0630	uM
2-[3-[(4-amino-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.0640	uM
2-[4-[(4-amino-2-propan-2-ylpyrimidin-5-yl)methyl]-3-methylthiophen-2-yl]ethanol	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.0640	uM
2-[3-[[2-amino-6-(trifluoromethyl)-3-pyridinyl]methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.1040	uM
2-[3-[(2-amino-5-iodo-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.1090	uM
2-[3-[(2-amino-3-pyridinyl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol chloride	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.1100	uM
[(Z)-2-[(2-amino-6-methyl-3-pyridinyl)methyl-formylamino]-5-hydroxypent-2-en-3-yl]sulfanylmethyl 2,2-dimethylpropanoate	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.1160	uM
2-[5-[[5-(2-hydroxyethyl)-4-methyl-1,3-thiazol-3-ium-3-yl]methyl]pyridine-2-carbonyl]benzoic acid	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.1400	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149594: Binding affinity to human TKT incubated for 45 mins by Kinobead based pull down assay	kd	0.1513	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149594: Binding affinity to human TKT incubated for 45 mins by Kinobead based pull down assay	kd	0.1669	uM
[2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethoxy-methylphosphoryl] dihydrogen phosphate	320588: Inhibition of apo-transketolase	kd	0.1700	uM
2-[4-methyl-3-[(5-methyl-3-pyridinyl)methyl]-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.2200	uM
2-[4-[(4-amino-2-phenylpyrimidin-5-yl)methyl]-3-methylthiophen-2-yl]ethanol	320591: Inhibition of apo-transketolase by coupled TPPK/Apo-TK enzymatic assay	kd	0.2300	uM
2-[4-methyl-3-[[6-(trifluoromethyl)-3-pyridinyl]methyl]-1,3-thiazol-3-ium-5-yl]ethanol	320378: Inhibition of transketolase by TPPK/apo-TK coupled assay	kd	0.3100	uM
N-[(2-amino-3-pyridinyl)methyl]-N-[(Z)-3-[[(Z)-2-[(2-amino-3-pyridinyl)methyl-formylamino]-5-hydroxypent-2-en-3-yl]disulfanyl]-5-hydroxypent-2-en-2-yl]formamide	313901: Inhibition of transketolase in human HCT116 cells	ec50	0.4790	uM
2-[3-[(2-amino-6-methyl-3-pyridinyl)methyl]-4-methyl-2-(pyridin-3-ylmethyl)-1,3-thiazol-3-ium-5-yl]ethanol	320379: Inhibition of human transketolase in HCT116 cells	ec50	0.8400	uM

CTD chemical–gene interactions

83 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression, increases expression	4
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	4
Arsenic	increases abundance, affects cotreatment, increases expression	3
Tobacco Smoke Pollution	affects expression, decreases expression, increases expression	3
Tretinoin	affects cotreatment, increases expression	3
sodium arsenate	increases abundance, increases expression	2
cobaltous chloride	increases expression	2
mercuric bromide	increases expression, affects cotreatment	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression, increases expression	2
Arsenic Trioxide	affects binding, decreases reaction, affects cotreatment, increases expression	2
Acetaminophen	decreases expression, increases expression	2
Cadmium	increases abundance, increases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Valproic Acid	affects expression, increases expression	2
Cadmium Chloride	increases abundance, increases expression	2
p-Chloromercuribenzoic Acid	affects cotreatment, increases expression	2
Particulate Matter	increases abundance, increases expression, affects cotreatment	2
FR900359	increases phosphorylation	1
bisphenol F	increases expression	1
TAK-243	increases sumoylation	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
pirinixic acid	increases expression, affects binding, increases activity	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, affects localization, decreases expression	1
arsenite	affects binding, decreases reaction	1
manganese chloride	affects cotreatment, increases abundance, increases expression	1
benzo(e)pyrene	decreases methylation	1
lead chloride	increases expression	1
cupric chloride	increases expression	1
cupric oxide	increases expression	1

ChEMBL screening assays

18 unique, capped per target: 18 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4270851	Binding	Binding affinity to transketolase in human Hela cells lysates assessed as protein enrichment by measuring normalized heavy/light ratio at by nano-LC-ESIMS/MS analysis	Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics. — J Nat Prod

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1ZC	Abcam A-549 TKT KO	Cancer cell line	Male
CVCL_D2DD	Abcam HCT 116 TKT KO	Cancer cell line	Male

Clinical trials (associated diseases)

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