CS
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Summary
CS (citrate synthase, HGNC:2422) is a protein-coding gene on chromosome 12q13.3, encoding Citrate synthase, mitochondrial (O75390). Key enzyme of the Krebs tricarboxylic acid cycle which catalyzes the synthesis of citrate from acetyl coenzyme A and oxaloacetate. It is a selective cancer dependency (DepMap: 36.6% of cell lines).
The protein encoded by this gene is a Krebs tricarboxylic acid cycle enzyme that catalyzes the synthesis of citrate from oxaloacetate and acetyl coenzyme A. The enzyme is found in nearly all cells capable of oxidative metablism. This protein is nuclear encoded and transported into the mitochondrial matrix, where the mature form is found.
Source: NCBI Gene 1431 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 44 total
- GTEx eGene: eQTL in 9 tissues, sQTL in 13 (q < 0.05)
- Cancer dependency (DepMap): dependent in 36.6% of screened cell lines
- Constraint (gnomAD): pLI 1.00 (loss-of-function intolerant), LOEUF 0.36 (moderately constrained)
- MANE Select transcript:
NM_004077 - Interaction hub: 3,695 STRING partners (top 1% of genes corpus-wide)
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2422 |
| Approved symbol | CS |
| Name | citrate synthase |
| Location | 12q13.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000062485 |
| Ensembl biotype | protein_coding |
| OMIM | 118950 |
| Entrez | 1431 |
Gene structure
Transcript identifiers
Ensembl transcripts: 53 — 32 protein_coding, 11 retained_intron, 10 nonsense_mediated_decay
MANE Select: ENST00000351328
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 10, TSL 3: 9, TSL 4: 9, TSL 5: 3
ENST00000351328, ENST00000542324, ENST00000546585, ENST00000546621, ENST00000546891, ENST00000546930, ENST00000547283, ENST00000547298, ENST00000547449, ENST00000547912, ENST00000548041, ENST00000548567, ENST00000548746, ENST00000548849, ENST00000549143, ENST00000549221, ENST00000550044, ENST00000550159, ENST00000550655, ENST00000550700, ENST00000550734, ENST00000550996, ENST00000551137, ENST00000551155, ENST00000551253, ENST00000551430, ENST00000551441, ENST00000551473, ENST00000551936, ENST00000551968, ENST00000552222, ENST00000552331, ENST00000552688, ENST00000904224, ENST00000904225, ENST00000921535, ENST00000921536, ENST00000947272, ENST00000947273, ENST00000991491, ENST00000991492, ENST00001056701, ENST00001056702, ENST00001056704, ENST00001056706, ENST00001091666, ENST00001091667, ENST00001091668, ENST00001091669, ENST00001091670, ENST00001124711, ENST00001129837, ENST00001138979
RefSeq mRNA: 1 — MANE Select: NM_004077
NM_004077
CCDS: CCDS8913
Canonical transcript exons
ENST00000351328 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003462969 | 56275002 | 56275131 |
| ENSE00003480306 | 56275996 | 56276195 |
| ENSE00003501837 | 56285916 | 56286023 |
| ENSE00003501898 | 56273587 | 56273796 |
| ENSE00003513078 | 56282420 | 56282608 |
| ENSE00003533644 | 56283792 | 56283857 |
| ENSE00003541640 | 56274777 | 56274878 |
| ENSE00003562168 | 56300160 | 56300330 |
| ENSE00003629831 | 56286595 | 56286645 |
| ENSE00003656673 | 56282860 | 56282991 |
| ENSE00003841381 | 56271699 | 56273254 |
Expression profiles
Bgee: expression breadth ubiquitous, 293 present calls, max score 99.45.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 132.1132 / max 1009.6120, expressed in 1828 samples.
Highest expression (Bgee): ventricle myocardium, cardiac muscle of right atrium, heart right ventricle, gastrocnemius, vastus lateralis.
Genetic regulation across tissues (GTEx eQTL / sQTL)
CS is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 9 tissues and its splicing (sQTL) in 13 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 22 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Muscle Skeletal | sqtl | 3.2e-20 | +0.49 | 12:56298926:C:T |
| Cells Cultured fibroblasts | sqtl | 2.6e-12 | +0.45 | 12:56298926:C:T |
| Skin Sun Exposed Lower leg | sqtl | 4.0e-06 | -0.68 | 12:56360038:C:A |
| Heart Atrial Appendage | sqtl | 4.1e-05 | -0.83 | 12:56233835:A:G |
| Artery Tibial | eqtl | 5.6e-05 | -0.30 | 12:56300123:A:C |
| Esophagus Muscularis | sqtl | 7.3e-05 | +0.74 | 12:56251102:A:G |
| Esophagus Muscularis | eqtl | 1.4e-04 | -0.31 | 12:56300123:A:C |
| Heart Atrial Appendage | eqtl | 3.1e-04 | +0.27 | 12:55301436:T:G |
| Nerve Tibial | sqtl | 9.2e-04 | +0.30 | 12:56298926:C:T |
| Breast Mammary Tissue | sqtl | 9.6e-04 | -0.67 | 12:56116134:G:C |
| Skin Sun Exposed Lower leg | eqtl | 1.1e-03 | +0.15 | 12:56166056:G:A |
| Cells EBV-transformed lymphocytes | sqtl | 2.4e-03 | -0.87 | 12:56240855:G:C |
| Adrenal Gland | sqtl | 2.6e-03 | -0.33 | 12:56297816:T:C |
| Esophagus Gastroesophageal Junction | sqtl | 6.1e-03 | -0.78 | 12:56233835:A:G |
| Adipose Visceral Omentum | sqtl | 7.1e-03 | +0.67 | 12:56241296:G:C |
| Brain Cortex | eqtl | 9.0e-03 | +1.04 | 12:57182156:G:A |
| Esophagus Mucosa | sqtl | 1.0e-02 | +0.26 | 12:56298926:C:T |
| Adipose Visceral Omentum | eqtl | 1.1e-02 | -0.20 | 12:55679762:T:A |
| Skin Not Sun Exposed Suprapubic | eqtl | 2.0e-02 | -0.30 | 12:55944654:TG:T |
| Cells EBV-transformed lymphocytes | eqtl | 2.9e-02 | +0.29 | 12:56300123:A:C |
FANTOM5 promoters
3 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 131504 | 106.7404 | 1827 |
| 131505 | 23.4241 | 1815 |
| 131503 | 1.9487 | 1043 |
Top tissues by expression
showing 100 of 295 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| left ventricle myocardium | UBERON:0006566 | 99.45 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 99.17 | gold quality |
| heart right ventricle | UBERON:0002080 | 99.06 | gold quality |
| gastrocnemius | UBERON:0001388 | 99.03 | gold quality |
| vastus lateralis | UBERON:0001379 | 99.02 | gold quality |
| myocardium | UBERON:0002349 | 98.99 | gold quality |
| body of tongue | UBERON:0011876 | 98.95 | gold quality |
| diaphragm | UBERON:0001103 | 98.94 | gold quality |
| cardiac ventricle | UBERON:0002082 | 98.92 | gold quality |
| heart left ventricle | UBERON:0002084 | 98.92 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 98.86 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 98.83 | gold quality |
| triceps brachii | UBERON:0001509 | 98.83 | gold quality |
| biceps brachii | UBERON:0001507 | 98.81 | gold quality |
| cardiac atrium | UBERON:0002081 | 98.80 | gold quality |
| gluteal muscle | UBERON:0002000 | 98.79 | gold quality |
| quadriceps femoris | UBERON:0001377 | 98.77 | gold quality |
| apex of heart | UBERON:0002098 | 98.77 | gold quality |
| muscle tissue | UBERON:0002385 | 98.77 | gold quality |
| right atrium auricular region | UBERON:0006631 | 98.76 | gold quality |
| deltoid | UBERON:0001476 | 98.72 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 98.72 | gold quality |
| muscle organ | UBERON:0001630 | 98.67 | gold quality |
| muscle of leg | UBERON:0001383 | 98.62 | gold quality |
| heart | UBERON:0000948 | 98.60 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 98.58 | gold quality |
| tibialis anterior | UBERON:0001385 | 98.43 | gold quality |
| right adrenal gland | UBERON:0001233 | 98.36 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 98.36 | gold quality |
| rectum | UBERON:0001052 | 98.35 | gold quality |
| tongue | UBERON:0001723 | 98.29 | gold quality |
| left adrenal gland | UBERON:0001234 | 98.26 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 98.18 | gold quality |
| mammalian vulva | UBERON:0000997 | 98.17 | gold quality |
| cortical plate | UBERON:0005343 | 98.17 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 98.15 | gold quality |
| upper leg skin | UBERON:0004262 | 98.15 | gold quality |
| adrenal cortex | UBERON:0001235 | 98.13 | gold quality |
| adrenal gland | UBERON:0002369 | 98.13 | gold quality |
| upper arm skin | UBERON:0004263 | 98.12 | gold quality |
| colonic epithelium | UBERON:0000397 | 98.08 | gold quality |
| transverse colon | UBERON:0001157 | 98.01 | gold quality |
| vena cava | UBERON:0004087 | 97.97 | gold quality |
| ganglionic eminence | UBERON:0004023 | 97.93 | gold quality |
| adrenal tissue | UBERON:0018303 | 97.85 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 97.78 | gold quality |
| olfactory bulb | UBERON:0002264 | 97.74 | silver quality |
| cerebellar hemisphere | UBERON:0002245 | 97.73 | gold quality |
| esophagus mucosa | UBERON:0002469 | 97.73 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 97.73 | gold quality |
| skin of leg | UBERON:0001511 | 97.70 | gold quality |
| cerebellar cortex | UBERON:0002129 | 97.69 | gold quality |
| superior surface of tongue | UBERON:0007371 | 97.69 | gold quality |
| skin of abdomen | UBERON:0001416 | 97.66 | gold quality |
| skin of hip | UBERON:0001554 | 97.64 | gold quality |
| cerebellum | UBERON:0002037 | 97.60 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 97.59 | gold quality |
| esophagus | UBERON:0001043 | 97.58 | gold quality |
| colon | UBERON:0001155 | 97.56 | gold quality |
| large intestine | UBERON:0000059 | 97.55 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 97.55 | gold quality |
| islet of Langerhans | UBERON:0000006 | 97.51 | gold quality |
| bone marrow cell | CL:0002092 | 97.49 | gold quality |
| zone of skin | UBERON:0000014 | 97.46 | gold quality |
| metanephros cortex | UBERON:0010533 | 97.46 | gold quality |
| intestine | UBERON:0000160 | 97.42 | gold quality |
| colonic mucosa | UBERON:0000317 | 97.41 | gold quality |
| paraflocculus | UBERON:0005351 | 97.39 | gold quality |
| body of stomach | UBERON:0001161 | 97.38 | gold quality |
| lower esophagus | UBERON:0013473 | 97.38 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 97.38 | gold quality |
| ventricular zone | UBERON:0003053 | 97.37 | gold quality |
| type B pancreatic cell | CL:0000169 | 97.36 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 97.36 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 97.35 | gold quality |
| sigmoid colon | UBERON:0001159 | 97.34 | gold quality |
| embryo | UBERON:0000922 | 97.33 | gold quality |
| postcentral gyrus | UBERON:0002581 | 97.33 | gold quality |
| minor salivary gland | UBERON:0001830 | 97.32 | gold quality |
| body of pancreas | UBERON:0001150 | 97.31 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 97.31 | gold quality |
| adipose tissue | UBERON:0001013 | 97.30 | gold quality |
| peritoneum | UBERON:0002358 | 97.30 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 97.30 | gold quality |
| omental fat pad | UBERON:0010414 | 97.30 | gold quality |
| vagina | UBERON:0000996 | 97.28 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 97.26 | gold quality |
| nipple | UBERON:0002030 | 97.25 | gold quality |
| pons | UBERON:0000988 | 97.24 | gold quality |
| stromal cell of endometrium | CL:0002255 | 97.19 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 97.18 | gold quality |
| stomach | UBERON:0000945 | 97.17 | gold quality |
| small intestine | UBERON:0002108 | 97.16 | gold quality |
| parietal lobe | UBERON:0001872 | 97.15 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 97.15 | gold quality |
| caecum | UBERON:0001153 | 97.13 | gold quality |
| renal medulla | UBERON:0000362 | 97.06 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 97.04 | gold quality |
| mucosa of stomach | UBERON:0001199 | 97.03 | gold quality |
| connective tissue | UBERON:0002384 | 97.01 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 15.89 |
| E-MTAB-9801 | no | 2.84 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 80 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Tongue | tissue | 561.0 | |
| Skeletal muscle | tissue | 515.2 | medium |
| Heart muscle | tissue | 298.9 | high |
| Frontal cortex | tissue | 221.3 | |
| Caudate putamen | tissue | 201.7 | |
| Superior colliculi | tissue | 157.7 | |
| Thalamus | tissue | 153.1 | |
| Spinal cord | tissue | 150.7 | |
| Cerebral cortex | tissue | 145.3 | high |
| Somatosensory cortex | tissue | 145.3 | |
| Adipose tissue | tissue | 144.7 | high |
| Medulla oblongata | tissue | 140.8 | |
| Pons | tissue | 139.4 | |
| Midbrain | tissue | 134.2 | |
| Postcentral gyrus | tissue | 130.9 | |
| Occipital cortex | tissue | 130.5 | |
| Motor cortex | tissue | 120.5 | |
| Parathyroid gland | tissue | 119.8 | high |
| Retina | tissue | 119.5 | |
| Rectum | tissue | 116.6 | high |
| Choroid plexus | tissue | 115.4 | |
| Hippocampal formation | tissue | 112.0 | |
| Substantia nigra | tissue | 111.6 | |
| Temporal cortex | tissue | 107.0 | |
| Prefrontal cortex | tissue | 105.8 | |
| Bone marrow | tissue | 104.8 | high |
| Retrosplenial and cingulate cortex | tissue | 103.4 | |
| Colon | tissue | 103.2 | high |
| Putamen | tissue | 103.1 | |
| Entorhinal cortex | tissue | 102.7 | |
| Cerebellum | tissue | 101.6 | high |
| Retrosplenial cortex | tissue | 99.5 | |
| Tonsil | tissue | 99.4 | high |
| Ventral forebrain | tissue | 97.0 | |
| Hypothalamus | tissue | 94.0 | |
| Periaqueductal gray | tissue | 93.2 | |
| Duodenum | tissue | 92.0 | high |
| Locus coeruleus | tissue | 92.0 | |
| Septum | tissue | 90.3 | |
| Insular cortex | tissue | 90.2 | |
| Basal ganglia | tissue | 90.1 | high |
| Esophagus | tissue | 89.9 | high |
| Olfactory bulb | tissue | 87.2 | |
| Kidney | tissue | 80.8 | high |
| Adrenal gland | tissue | 80.1 | high |
| Amygdala | tissue | 78.7 | |
| Nucleus accumbens | tissue | 78.4 | |
| Small intestine | tissue | 76.5 | high |
| Corpus callosum | tissue | 73.5 | |
| Smooth muscle | tissue | 72.4 | medium |
| Hippocampus | tissue | 70.8 | high |
| Salivary gland | tissue | 69.5 | high |
| Vagina | tissue | 65.6 | high |
| Urinary bladder | tissue | 65.6 | high |
| Thymus | tissue | 64.7 | |
| Skin 1 | tissue | 63.5 | high |
| Lymph node | tissue | 62.7 | high |
| Stomach 1 | tissue | 62.7 | high |
| Appendix | tissue | 58.2 | high |
| Pancreas | tissue | 58.0 | high |
Brain sub-regions (HPA Brain Atlas): detected in 192; highest nTPM — Ventral spinal cord (150.7), Dorsal spinal cord (116.5), Pulvinar (115.5), Lateral geniculate body (113.9), Precentral gyrus, middle (112.9).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): FEZF2, MAF, MYB, POU1F1, RORA, SP1, TBR1, TEAD1
miRNA regulators (miRDB)
Targeting CS by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
showing 30 of 108 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-3689D | 100.00 | 66.14 | 1181 |
| HSA-MIR-6851-5P | 100.00 | 65.63 | 1294 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-4283 | 100.00 | 66.42 | 2097 |
| HSA-MIR-4514 | 99.99 | 67.10 | 1870 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-19A-3P | 99.98 | 75.33 | 2762 |
| HSA-MIR-19B-3P | 99.98 | 75.44 | 2754 |
| HSA-LET-7F-2-3P | 99.98 | 70.98 | 2588 |
| HSA-MIR-1185-1-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-1185-2-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-3688-3P | 99.97 | 72.02 | 2834 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-548AJ-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548X-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-559 | 99.95 | 72.28 | 3609 |
| HSA-MIR-548AB | 99.95 | 71.31 | 3488 |
| HSA-MIR-548J-3P | 99.94 | 72.61 | 4881 |
| HSA-MIR-548A-5P | 99.94 | 71.27 | 3482 |
| HSA-MIR-548AD-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AE-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AK | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AM-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AP-5P | 99.94 | 71.14 | 3489 |
| HSA-MIR-548AQ-5P | 99.94 | 71.34 | 3426 |
| HSA-MIR-548AR-5P | 99.94 | 71.28 | 3515 |
| HSA-MIR-548AS-5P | 99.94 | 71.22 | 3482 |
Functional genomics
gnomAD constraint: pLI 1, LOEUF 0.356, missense Z 4.36 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD)
ENST00000351328 splits into 2 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD
| Region (GRCh38) | Missense obs / exp | o/e | Constrained |
|---|---|---|---|
| 12:56,273,087–56,285,946 | 223 / 503.5 | 0.44 | no |
| 12:56,285,947–56,300,201 | 55 / 69.9 | 0.79 | no |
| DepMap (CRISPR cell-line fitness): dependent in 36.6% of screened cell lines. |
Most-dependent cell lines (DepMap gene-effect, lower = stronger; ≤ −0.5 shown): OCI-AML3 (-1.841), OCI-AML2 (-1.154), LS1034 (-1.13), Ki-JK (-1.119), TUHR10TKB (-1.113), SK-N-BE(2) (-1.095), SU-DHL-10 (-1.092), MEL-HO (-1.054), HEC-59 (-1.041), MCF-7 (-1.013), KPL-1 (-1.009), NCI-H23 (-1.007), SNU-398 (-0.996), TALL-1 (-0.979), HCC2998 (-0.974).
Literature-anchored findings (GeneRIF, showing 19)
- Responses of skeletal and cardiac muscles in CS activity and gene expression at 1 and 48 h after endurance training. Acute effect of exercise on training-induced elevation in CS activity in rat soleus but not ventricle muscles. (PMID:12531911)
- possible role of CS-specific autoantibodies in the pathomechanism of allograft vasculopathy (PMID:15711981)
- It is likely that enhanced citrate synthase activity contributes to the conversion of glucose to lipids in pancreatic cancer providing substrate for membrane lipids synthesis. (PMID:15714131)
- These results provide an important basis for the study of mitochondrial dysfunction due to aberrant CSa trafficking. (PMID:19479947)
- Citrate synthase (CS) is a direct RORalpha target gene and one mechanism by which RORalpha regulates lipid metabolism is via regulation of CS expression. (PMID:22485150)
- The citrate synthase knockdown cells exhibited severe defects in respiratory activity and marked decreases in ATP production, but great increases in glycolytic metabolism. (PMID:23139858)
- Paretic muscle in hemiparetic stroke survivors had lower CS concentration. (PMID:26361074)
- Citrate synthase activity was lower in patients with heart failure with preserved ejection fraction compared to controls. (PMID:27179829)
- citrate synthase and ACSS1 have tumorigenic functions in hepatocellular carcinoma (PMID:27363021)
- mir-122 and its targets G6PC3, ALDOA and CS play roles in the hypoxia responses that regulate glucose and energy metabolism and can serve as hypoxia biomarkers. (PMID:27793029)
- Hence, we conclude that SIRT3 exhibits neuroprotection via deacetylating and increasing mitochondrial enzyme activities. (PMID:28161643)
- Data suggest that downregulation of citrate synthase (CS) expression in 293T cells leads to low level of ATP production, excessive superoxide formation and cell apoptosis, which implies a possible mechanism for hearing loss in A/J mice. (PMID:28216161)
- Data suggest that METTL12, localized in mitochondrial matrix, modifies/methylates Lys368 of citrate synthase in external surface region close to its catalytic site; addition/removal of methylation has no effect on citrate synthase activity; Lys368 occurs in highly conserved sequence of amino acid residues of citrate synthase. (METTL12 = methyltransferase-like protein 12) (PMID:28391595)
- METTL12 methylates CS on Lys-395, which is localized in the CS active site. Interestingly, the METTL12-mediated methylation inhibited CS activity and was blocked by the CS substrate oxaloacetate. (PMID:28887308)
- The active sites of the citrate synthase is almost identical, the differences in reactions catalyzed by citrate synthase are caused by residues that are in the vicinity of the active site and influence conformational changes of the citrate synthase. (PMID:31141475)
- Rethinking the Citric Acid Cycle: Connecting Pyruvate Carboxylase and Citrate Synthase to the Flow of Energy and Material. (PMID:33435350)
- The left-lateralisation of citrate synthase activity in the anterior cingulate cortex of male violent suicide victims. (PMID:36350374)
- The Novel Role of Mitochondrial Citrate Synthase and Citrate in the Pathophysiology of Alzheimer’s Disease. (PMID:37393492)
- Citrate synthase lysine K215 hypoacetylation contributes to microglial citrate accumulation and pro-inflammatory functions after traumatic brain injury. (PMID:38421106)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cs | ENSDARG00000103364 |
| mus_musculus | Cs | ENSMUSG00000005683 |
| mus_musculus | Csl | ENSMUSG00000046934 |
| rattus_norvegicus | Cs | ENSRNOG00000023520 |
| drosophila_melanogaster | kdn | FBGN0261955 |
| caenorhabditis_elegans | WBGENE00000833 |
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:88529) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 9 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| increased or absent threshold for auditory brainstem response | 2 |
| abnormal digit morphology | 1 |
| abnormal auditory brainstem response | 1 |
| increased susceptibility to age-related hearing loss | 1 |
| impaired glucose tolerance | 1 |
| impaired hearing | 1 |
| decreased prepulse inhibition | 1 |
| abnormal retina blood vessel morphology | 1 |
| preweaning lethality, complete penetrance | 1 |
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Aspergillus fumigatus A1163 | B0YD89 | 100.0% | Diamond |
| Aspergillus fumigatus | Q50I20 | 100.0% | Diamond |
| Thunnus obesus | Q6S9V8 | 100.0% | Diamond |
| Thunnus albacares | Q6S9V9 | 100.0% | Diamond |
| Iguana iguana | Q0GNE0 | 99.8% | Diamond |
| Amblyrhynchus cristatus | Q0GNE1 | 99.8% | Diamond |
| Aedes aegypti | Q16P20 | 99.8% | Diamond |
| Katsuwonus pelamis | Q6S9V7 | 99.4% | Diamond |
| Kajikia audax | Q6S9V5 | 99.1% | Diamond |
| Xiphias gladius | Q6S9V6 | 99.1% | Diamond |
| Macaca fascicularis | P0C1Z2 | 98.9% | Diamond |
| Mesocricetus auratus | Q0QEL7 | 98.1% | Diamond |
| Sus scrofa | P00889 | 97.2% | Diamond |
| Bos taurus | Q29RK1 | 97.2% | Diamond |
| Caenorhabditis briggsae | Q61JF9 | 97.0% | Diamond |
| Fusarium solani | C7C435 | 96.2% | Diamond |
| Fusarium verticillioides | C7C436 | 96.2% | Diamond |
| Xenopus tropicalis | Q28DK1 | 95.7% | Diamond |
| Xenopus laevis | Q7ZWZ5 | 95.7% | Diamond |
| Tetraodon nigroviridis | Q4S5X1 | 95.5% | Diamond |
| Leishmania infantum | A4HXU4 | 95.1% | Diamond |
| Leishmania major | Q4QDX3 | 95.1% | Diamond |
| Aspergillus nidulans FGSC A4 | O00098 | 92.1% | Diamond |
| Aspergillus niger | P51044 | 92.1% | Diamond |
| Gallus gallus | P23007 | 91.9% | Diamond |
| Glossina morsitans morsitans | Q0QHL3 | 90.6% | Diamond |
| Leishmania braziliensis | A4H9H8 | 86.7% | Diamond |
| Arabidopsis thaliana | P20115 | 85.8% | Diamond |
| Citrus maxima | P49298 | 83.7% | Diamond |
| Daucus carota | O80433 | 83.5% | Diamond |
| Neurospora crassa OR74A | P34085 | 81.9% | Diamond |
| Saccharomyces cerevisiae S288C | P08679 | 81.6% | Diamond |
| Candida tropicalis | P79024 | 80.8% | Diamond |
| Solanum tuberosum | Q43175 | 80.8% | Diamond |
| Fragaria x ananassa | P83372 | 78.4% | Diamond |
| Yarrowia lipolytica CLIB122 | Q6C793 | 76.0% | Diamond |
| Dictyostelium discoideum | Q553V1 | 73.6% | Diamond |
| Schizosaccharomyces pombe 972h- | Q10306 | 71.0% | Diamond |
| Thermosulfidibacter takaii ABI70S6 | A0A0S3QTD0 | 64.2% | Diamond |
| Tetrahymena thermophila | P24118 | 61.0% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| CNPY2-AS1 | ncRNA | 112268098 |
| IL23A | protein-coding | 51561 |
| COQ10A | protein-coding | 93058 |
| PAN2 | protein-coding | 9924 |
| CNPY2 | protein-coding | 10330 |
| ANKRD52 | protein-coding | 283373 |
| SLC39A5 | protein-coding | 283375 |
| NABP2 | protein-coding | 79035 |
| STAT2 | protein-coding | 6773 |
| RNF41 | protein-coding | 10193 |
Protein
Protein identifiers
Citrate synthase, mitochondrial — O75390 (reviewed: O75390)
Alternative names: Citrate (Si)-synthase
All UniProt accessions (21): A0A0C4DGI3, B4DJV2, O75390, F8VPA1, F8VPF9, F8VR34, F8VRI6, F8VRP1, F8VTT8, F8VU34, F8VVY4, F8VWQ5, F8VX07, F8VX68, F8VZK9, F8W0J2, F8W1S4, F8W4S1, F8W642, H0YH82, H0YIC4
UniProt curated annotations — full annotation on UniProt →
Function. Key enzyme of the Krebs tricarboxylic acid cycle which catalyzes the synthesis of citrate from acetyl coenzyme A and oxaloacetate.
Subunit / interactions. Homodimer.
Subcellular location. Mitochondrion matrix.
Post-translational modifications. Methylated. Trimethylation at Lys-395 by CSKMT decreases citrate synthase activity. In response to mitochondrial stress, the precursor protein is ubiquitinated by the SIFI complex in the cytoplasm before mitochondrial import, leading to its degradation. Within the SIFI complex, UBR4 initiates ubiquitin chain that are further elongated or branched by KCMF1.
Pathway. Carbohydrate metabolism; tricarboxylic acid cycle; isocitrate from oxaloacetate: step 1/2.
Miscellaneous. Citrate synthase is found in nearly all cells capable of oxidative metabolism.
Similarity. Belongs to the citrate synthase family.
RefSeq proteins (1): NP_004068* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR002020 | Citrate_synthase | Family |
| IPR010109 | Citrate_synthase_euk | Family |
| IPR016142 | Citrate_synth-like_lrg_a-sub | Homologous_superfamily |
| IPR016143 | Citrate_synth-like_sm_a-sub | Homologous_superfamily |
| IPR019810 | Citrate_synthase_AS | Active_site |
| IPR036969 | Citrate_synthase_sf | Homologous_superfamily |
Pfam: PF00285
Enzyme classification (BRENDA)
- EC 2.3.3.1 — citrate (Si)-synthase (BRENDA: 15 organisms, 9 substrates, 48 inhibitors, 28 Km, 18 kcat entries)
- EC 2.3.3.16 — citrate synthase (unknown stereospecificity) (BRENDA: 100 organisms, 82 substrates, 183 inhibitors, 214 Km, 98 kcat entries)
Substrate kinetics (BRENDA)
6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ACETYL-COA | 0.0007–125 | 101 |
| OXALOACETATE | 0.0011–90.3 | 93 |
| ACETYL-COA | 0.005–10 | 14 |
| OXALOACETATE | 0.0036–5 | 14 |
| PROPIONYL-COA | 0.0017–0.016 | 5 |
| CITRATE | 0.0005–0.001 | 4 |
Catalyzed reactions (Rhea)
- oxaloacetate + acetyl-CoA + H2O = citrate + CoA + H(+) (RHEA:16845)
UniProt features (77 total): helix 28, modified residue 18, sequence conflict 8, strand 8, turn 4, active site 3, binding site 3, mutagenesis site 2, transit peptide 1, chain 1, short sequence motif 1
Structure
Experimental structures (PDB)
11 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 8ZVV | human citrate synthase complexed with citrate | X-RAY DIFFRACTION | 1.59 |
| 8ZVU | Human citrate synthase intermediate 4 | X-RAY DIFFRACTION | 1.78 |
| 8ZVR | Human citrate synthase intermediate 2 | X-RAY DIFFRACTION | 1.8 |
| 8ZVW | human citrate synthase complexed with oxaloacetate and coenzyme A | X-RAY DIFFRACTION | 1.82 |
| 8ZVL | human citrate synthases complexed with oxaloacetate | X-RAY DIFFRACTION | 2.05 |
| 8ZVT | Human citrate synthase intermediate 3 | X-RAY DIFFRACTION | 2.05 |
| 8ZW1 | citrate synthases complexed with oxaloacetate and acetyl-CoA | X-RAY DIFFRACTION | 2.1 |
| 5UZQ | Crystal structure of citrate synthase from homo sapiens | X-RAY DIFFRACTION | 2.16 |
| 8ZVM | Human citrate synthase intermediate 1 | X-RAY DIFFRACTION | 2.27 |
| 5UZP | Crystal structure of citrate synthase mutant A348G from homo sapiens | X-RAY DIFFRACTION | 2.29 |
| 5UZR | Crystal structure of citrate synthase from homo sapiens | X-RAY DIFFRACTION | 2.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O75390-F1 | 94.56 | 0.93 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Transferases, Metabolic proteins, Predicted membrane proteins, Predicted intracellular proteins, Plasma proteins, Citric acid cycle related proteins, Essential proteins
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): mitochondria
Antibody reliability (HPA): IH enhanced · IF enhanced
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)
| Position | Role |
|---|---|
| 301 | |
| 347 | |
| 402 |
Ligand- & substrate-binding residues (3)
| Position | Role |
|---|---|
| 356 | oxaloacetate |
| 428 | oxaloacetate |
| 448 | oxaloacetate |
Post-translational modifications (18)
| Type | Positions |
|---|---|
| N6-acetyllysine | 76, 321, 327, 375, 382, 393, 459 |
| N6-succinyllysine | 76, 103, 193, 321, 327, 375, 393, 450, 459, 57 |
| N6,n6,n6-trimethyllysine | 395 |
Mutagenesis-validated functional residues (2)
| Position | Phenotype |
|---|---|
| 393 | does not inhibit methylation. |
| 395 | inhibits methylation. |
Function
Pathways and Gene Ontology
Reactome pathways
3 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
8 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-71403 | Citric acid cycle (TCA cycle) | curated |
| R-HSA-9854311 | Maturation of TCA enzymes and regulation of TCA cycle | curated |
| R-HSA-9837999 | Mitochondrial protein degradation | curated |
| R-HSA-1428517 | Aerobic respiration and respiratory electron transport | — |
| R-HSA-1430728 | Metabolism | — |
| R-HSA-392499 | Metabolism of proteins | — |
| R-HSA-1268020 | Mitochondrial protein import | electronic |
| R-HSA-9609507 | Protein localization | — |
MSigDB gene sets: 304 (showing top):
MORF_MTA1, MORF_DNMT1, MORF_ESPL1, WWTAAGGC_UNKNOWN, GCM_GSPT1, MORF_UBE2I, MORF_RRM1, MORF_HDAC1, MORF_CDK2, TGACCTY_ERR1_Q2, MORF_HDAC2, HNF1_Q6, CHX10_01, GGGTGGRR_PAX4_03, GCM_BCL2L1
GO Biological Process (3): carbohydrate metabolic process (GO:0005975), tricarboxylic acid cycle (GO:0006099), citrate metabolic process (GO:0006101)
GO Molecular Function (5): RNA binding (GO:0003723), citrate synthase activity (GO:0036440), identical protein binding (GO:0042802), transferase activity (GO:0016740), acyltransferase activity, acyl groups converted into alkyl on transfer (GO:0046912)
GO Cellular Component (4): nucleus (GO:0005634), mitochondrion (GO:0005739), mitochondrial matrix (GO:0005759), extracellular exosome (GO:0070062)
Reactome top-level categories
5 top-level categories:
| Category | Pathways |
|---|---|
| Protein localization | 1 |
| Aerobic respiration and respiratory electron transport | 1 |
| Metabolism of proteins | 1 |
| Citric acid cycle (TCA cycle) | 1 |
| Metabolism | 1 |
GO top-level categories
13 GO namespaces:
| Category | Terms |
|---|---|
| primary metabolic process | 2 |
| intracellular membrane-bounded organelle | 2 |
| aerobic respiration | 1 |
| tricarboxylic acid metabolic process | 1 |
| nucleic acid binding | 1 |
| acyltransferase activity, acyl groups converted into alkyl on transfer | 1 |
| protein binding | 1 |
| catalytic activity | 1 |
| acyltransferase activity | 1 |
| cytoplasm | 1 |
| mitochondrion | 1 |
| intracellular organelle lumen | 1 |
| extracellular vesicle | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 8 of 12 annotations. The rest are phylogenetic / computational / electronic (IEA).
8 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| carbohydrate metabolic process | BP | direct assay |
| extracellular exosome | CC | high-throughput assay |
| mitochondrial matrix | CC | direct assay |
| mitochondrion | CC | direct assay |
| nucleus | CC | high-throughput assay |
| RNA binding | MF | high-throughput assay |
| citrate synthase activity | MF | direct assay |
| identical protein binding | MF | physical interaction |
Protein interactions and networks
STRING
showing 15 of 3,695 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CS | IDH2 | P48735 | 914 |
| CS | IDH1 | O75874 | 892 |
| CS | ACO2 | Q99798 | 854 |
| CS | PKM | P14618 | 834 |
| CS | FH | P07954 | 830 |
| CS | ACO1 | P21399 | 822 |
| CS | SLC25A16 | P16260 | 809 |
| CS | MDH2 | P40926 | 800 |
| CS | PC | P11498 | 787 |
| CS | VDAC3 | Q9Y277 | 777 |
| CS | GAPDH | P00354 | 776 |
| CS | ACLY | P53396 | 773 |
| CS | OGDH | Q02218 | 763 |
| CS | PDIA6 | Q15084 | 763 |
| CS | LDHC | P07864 | 729 |
IntAct
Human interaction partners of CS in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
25 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| NEK10 | proximity | 0.420 | 1 |
| ATXN7L1 | physical association | 0.400 | 1 |
| HSPE1 | physical association | 0.400 | 1 |
| PLEC | physical association | 0.400 | 1 |
| NS | association | 0.350 | 1 |
| OPA3 | association | 0.350 | 1 |
| PAK2 | association | 0.350 | 1 |
| SLC25A32 | association | 0.350 | 1 |
| ANXA5 | physical association | 0.000 | 1 |
| ARF6 | physical association | 0.000 | 1 |
| EIF5B | physical association | 0.000 | 1 |
| EIF6 | physical association | 0.000 | 1 |
| GPI | physical association | 0.000 | 1 |
| HLA-B | physical association | 0.000 | 1 |
| LCOR | physical association | 0.000 | 1 |
| MCC | physical association | 0.000 | 1 |
| PA2G4 | physical association | 0.000 | 1 |
| SGK1 | physical association | 0.000 | 1 |
| SND1 | physical association | 0.000 | 1 |
| SNRPB2 | physical association | 0.000 | 1 |
| TAB2 | physical association | 0.000 | 1 |
| TRAF6 | physical association | 0.000 | 1 |
| TRAP1 | physical association | 0.000 | 1 |
| UBE2N | physical association | 0.000 | 1 |
| ZNF207 | physical association | 0.000 | 1 |
BioGRID (721 interactions; top human partners by supporting records in a sample of 600 records): ACAD9 (Proximity Label-MS; 3 records), CLPP (Proximity Label-MS; 3 records), DLAT (Co-fractionation; 3 records), ECHS1 (Co-fractionation; 3 records), GFM1 (Proximity Label-MS; 3 records), GRSF1 (Proximity Label-MS; 3 records), HINT2 (Proximity Label-MS; 3 records), HSD17B10 (Two-hybrid; 3 records), LRPPRC (Proximity Label-MS; 3 records), MDH2 (Proximity Label-MS; 3 records), MRPS26 (Proximity Label-MS; 3 records), MTERF3 (Proximity Label-MS; 3 records), MTIF2 (Proximity Label-MS; 3 records), OAT (Co-fractionation; 3 records), SDHA (Co-fractionation; 3 records)
SIGNOR signaling
showing 4 of 6 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| CS | “down-regulates quantity” | acetyl-CoA | “chemical modification” |
| CS | “down-regulates quantity” | oxaloacetate(2-) | “chemical modification” |
| CS | “up-regulates quantity” | citrate(3-) | “chemical modification” |
| CSKMT | “down-regulates activity” | CS | methylation |
Protein complexes (CORUM) (1)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
1 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| CS-MAP3K7IP1-MAP3K7IP2 complex | 3 | CS, TAB1, TAB2 |
Disease & clinical
Genetic variants
Variant evidence for CS: 44 ClinVar records (0 pathogenic / likely pathogenic); 5 GWAS associations.
ClinVar
44 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 33 |
| Likely benign | 1 |
| Benign | 2 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 27 predictions of 852):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 12:56273585–56273586 | donor_loss | 1.0000 | 4 |
| 12:56273797–56273798 | acceptor_loss | 1.0000 | 5 |
| 12:56273799 | acceptor_gain | 1.0000 | |
| 12:56273806 | acceptor_gain | 1.0000 | |
| 12:56274775–56274776 | donor_loss | 1.0000 | 5 |
| 12:56274879–56274881 | acceptor_gain | 1.0000 | 2 |
| 12:56274879–56274880 | acceptor_loss | 1.0000 | 4 |
| 12:56274885 | acceptor_gain | 1.0000 | |
| 12:56274890–56274892 | acceptor_gain | 1.0000 | 3 |
| 12:56275158 | acceptor_gain | 1.0000 |
AlphaMissense
1,530 missense substitutions predicted likely pathogenic (of 3,028 scored), across 354 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| M165 | 9 | 0.894 | 0.983 |
| H347 | 8 | 0.999 | 1.000 |
| D354 | 8 | 0.999 | 0.999 |
| D402 | 8 | 0.999 | 1.000 |
| H265 | 8 | 0.997 | 0.999 |
| F424 | 8 | 0.997 | 1.000 |
| H301 | 8 | 0.996 | 0.999 |
| D264 | 8 | 0.993 | 0.998 |
| H262 | 8 | 0.986 | 0.999 |
| N400 | 8 | 0.982 | 1.000 |
| D235 | 8 | 0.981 | 0.991 |
| H273 | 8 | 0.977 | 0.997 |
| D201 | 8 | 0.976 | 0.995 |
| N269 | 8 | 0.969 | 0.999 |
| H163 | 8 | 0.956 | 0.995 |
| S405 | 8 | 0.956 | 0.999 |
| S271 | 8 | 0.946 | 0.999 |
| F93 | 8 | 0.944 | 0.997 |
| N396 | 8 | 0.942 | 0.998 |
| H404 | 8 | 0.928 | 0.990 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
2 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Kidney Renal Clear Cell Carcinoma (TCGA) | favorable | 2.13e-07 |
| Lung Adenocarcinoma (validation) | unfavorable | 0.000651 |
Disease associations
OMIM: gene MIM:118950 | disease phenotypes:
GWAS associations
5 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST008839_127 | Height | 1e-189 |
| GCST010002_69 | Refractive error | 6e-174 |
| GCST90090967_16 | Height | 2e-12 |
| GCST002740_7 | Inflammatory skin disease | 3e-12 |
| GCST001885_1 | Height | 3e-9 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4295678 (SINGLE PROTEIN)
PharmGKB: 1 entry (CPIC guideline: no)
Binding affinities (BindingDB)
1 measured of 1 human assays (2 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| CHEMBL5653589 | KD | 1440 nM |
CTD chemical–gene interactions
72 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Doxorubicin | decreases expression, decreases reaction | 3 |
| bisphenol A | affects expression, increases expression | 2 |
| bisphenol S | increases expression | 2 |
| Resveratrol | decreases expression, decreases reaction, increases activity | 2 |
| Dronabinol | decreases expression, increases expression | 2 |
| Zidovudine | affects expression, decreases expression | 2 |
| Particulate Matter | affects cotreatment, increases abundance, increases expression, decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| bisphenol F | increases expression | 1 |
| dicrotophos | increases expression | 1 |
| 2,4,6-tribromophenol | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| pyrogallol 1,3-dimethyl ether | affects cotreatment, affects localization, increases expression, decreases expression | 1 |
| 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid | decreases activity, decreases reaction | 1 |
| sodium arsenite | decreases expression | 1 |
| cobaltous chloride | decreases expression | 1 |
| perfluorooctanoic acid | increases expression | 1 |
| ochratoxin A | decreases expression | 1 |
| acipimox | increases expression | 1 |
| methacrylaldehyde | affects cotreatment, increases oxidation | 1 |
| ebselen | decreases activity, decreases reaction | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 2,3,5-(triglutathion-S-yl)hydroquinone | increases ADP-ribosylation | 1 |
| manganese(III)-tetrakis(4-benzoic acid)porphyrin | decreases reaction, decreases activity | 1 |
| nutlin 3 | affects cotreatment, increases secretion | 1 |
| 2,3-bis(4-hydroxyphenyl)-propionitrile | increases activity, decreases reaction | 1 |
| 4,4’,4’’-(4-propyl-((1)H)-pyrazole-1,3,5-triyl) tris-phenol | decreases reaction, increases activity | 1 |
| bisphenol B | increases expression | 1 |
| 2,2’,4,4’-tetrabromodiphenyl ether | decreases expression | 1 |
ChEMBL screening assays
4 unique, capped per target: 4 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4118555 | Binding | Binding affinity to CS in human NCI-H23 cells at 1 uM by mass spectrometry based pull down assay | Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. — *Bioorg Med Chem* |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for CS across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.