NAT1
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Summary
NAT1 (N-acetyltransferase 1, HGNC:7645) is a protein-coding gene on chromosome 8p22, encoding Arylamine N-acetyltransferase 1 (P18440). Participates in the detoxification of a plethora of hydrazine and arylamine drugs.
This gene is one of two arylamine N-acetyltransferase (NAT) genes in the human genome, and is orthologous to the mouse and rat Nat2 genes. The enzyme encoded by this gene catalyzes the transfer of an acetyl group from acetyl-CoA to various arylamine and hydrazine substrates. This enzyme helps metabolize drugs and other xenobiotics, and functions in folate catabolism. Multiple transcript variants encoding different isoforms have been found for this gene.
Source: NCBI Gene 9 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 58 total
- GTEx eGene: eQTL in 10 tissues, sQTL in 3 (q < 0.05)
- Constraint (gnomAD): pLI 0.15 (intermediate), LOEUF 1.91 (unconstrained)
- MANE Select transcript:
NM_000662 - Notable: 58 clinical variants but no curated precision-oncology (CIViC) evidence yet
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7645 |
| Approved symbol | NAT1 |
| Name | N-acetyltransferase 1 |
| Location | 8p22 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000171428 |
| Ensembl biotype | protein_coding |
| OMIM | 108345 |
| Entrez | 9 |
Gene structure
Transcript identifiers
Ensembl transcripts: 22 — 19 protein_coding, 3 protein_coding_CDS_not_defined
MANE Select: ENST00000307719
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 3, TSL 2: 2, TSL 3: 1, TSL 5: 1
ENST00000307719, ENST00000517441, ENST00000517492, ENST00000517574, ENST00000518029, ENST00000519006, ENST00000520546, ENST00000545197, ENST00000903000, ENST00000903001, ENST00000903002, ENST00000903003, ENST00000903004, ENST00000903005, ENST00000903006, ENST00000903007, ENST00000903008, ENST00000903009, ENST00000938747, ENST00000938748, ENST00000938749, ENST00001136598
RefSeq mRNA: 10 — MANE Select: NM_000662
NM_000662, NM_001160170, NM_001160171, NM_001160172, NM_001160173, NM_001160174, NM_001160175, NM_001160176, NM_001160179, NM_001291962
CCDS: CCDS55205, CCDS6007
Canonical transcript exons
ENST00000307719 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001308408 | 18222042 | 18223689 |
| ENSE00002276990 | 18210109 | 18210180 |
| ENSE00003642832 | 18219411 | 18219489 |
Expression profiles
Bgee: expression breadth ubiquitous, 242 present calls, max score 98.26.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 1.8699 / max 51.3915, expressed in 971 samples.
Highest expression (Bgee): bronchial epithelial cell, epithelium of bronchus, bronchus, ileal mucosa, colonic mucosa.
Genetic regulation across tissues (GTEx eQTL / sQTL)
NAT1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 10 tissues and its splicing (sQTL) in 3 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
13 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Liver | sqtl | 2.1e-10 | -0.92 | 8:18195466:A:AAT |
| Brain Cerebellum | eqtl | 5.9e-09 | +0.60 | 8:18492419:G:A |
| Brain Cerebellar Hemisphere | eqtl | 8.4e-09 | +0.58 | 8:18499009:G:C |
| Colon Transverse | eqtl | 1.1e-03 | +0.10 | 8:18323560:A:G |
| Lung | eqtl | 6.8e-03 | +0.09 | 8:18305456:G:A |
| Esophagus Mucosa | eqtl | 8.1e-03 | +0.42 | 8:17598459:G:C |
| Testis | sqtl | 1.7e-02 | +0.43 | 8:18217303:G:GTTAAT |
| Brain Hypothalamus | eqtl | 1.8e-02 | -2.00 | 8:17277423:G:A |
| Thyroid | eqtl | 2.1e-02 | +0.59 | 8:18216492:T:C |
| Skin Not Sun Exposed Suprapubic | eqtl | 2.4e-02 | +0.16 | 8:18344309:A:G |
| Cells Cultured fibroblasts | eqtl | 2.4e-02 | -0.32 | 8:18197801:A:G |
| Whole Blood | sqtl | 2.4e-02 | +0.58 | 8:18009909:T:C |
| Brain Frontal Cortex BA9 | eqtl | 3.9e-02 | +0.62 | 8:17341739:A:C |
FANTOM5 promoters
4 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 87568 | 2.3685 | 1282 |
| 87569 | 1.8070 | 960 |
| 87566 | 0.0524 | 17 |
| 87567 | 0.0104 | 6 |
Top tissues by expression
showing 100 of 291 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| bronchial epithelial cell | CL:0002328 | 98.26 | gold quality |
| epithelium of bronchus | UBERON:0002031 | 96.66 | gold quality |
| bronchus | UBERON:0002185 | 95.60 | gold quality |
| ileal mucosa | UBERON:0000331 | 94.44 | gold quality |
| colonic mucosa | UBERON:0000317 | 94.16 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 93.72 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 93.17 | gold quality |
| nasopharynx | UBERON:0001728 | 93.15 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 91.63 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 91.40 | gold quality |
| jejunal mucosa | UBERON:0000399 | 90.81 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 89.77 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 89.67 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 88.90 | gold quality |
| nasal cavity mucosa | UBERON:0001826 | 88.28 | gold quality |
| corpus epididymis | UBERON:0004359 | 88.02 | gold quality |
| endometrium epithelium | UBERON:0004811 | 87.38 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 87.07 | gold quality |
| rectum | UBERON:0001052 | 86.05 | gold quality |
| pancreatic ductal cell | CL:0002079 | 85.12 | gold quality |
| nephron tubule | UBERON:0001231 | 84.43 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 84.17 | gold quality |
| duodenum | UBERON:0002114 | 84.04 | gold quality |
| right lobe of liver | UBERON:0001114 | 82.70 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 82.46 | gold quality |
| amniotic fluid | UBERON:0000173 | 82.26 | gold quality |
| liver | UBERON:0002107 | 81.15 | gold quality |
| caput epididymis | UBERON:0004358 | 81.03 | gold quality |
| renal glomerulus | UBERON:0000074 | 80.49 | gold quality |
| kidney epithelium | UBERON:0004819 | 79.87 | gold quality |
| oral cavity | UBERON:0000167 | 79.77 | gold quality |
| gingival epithelium | UBERON:0001949 | 79.52 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 79.51 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 79.33 | gold quality |
| transverse colon | UBERON:0001157 | 79.22 | gold quality |
| monocyte | CL:0000576 | 78.93 | gold quality |
| visceral pleura | UBERON:0002401 | 78.85 | gold quality |
| pleura | UBERON:0000977 | 78.81 | gold quality |
| leukocyte | CL:0000738 | 78.76 | gold quality |
| mononuclear cell | CL:0000842 | 78.70 | gold quality |
| parietal pleura | UBERON:0002400 | 78.63 | gold quality |
| gingiva | UBERON:0001828 | 78.51 | gold quality |
| islet of Langerhans | UBERON:0000006 | 77.91 | gold quality |
| vermiform appendix | UBERON:0001154 | 77.64 | gold quality |
| squamous epithelium | UBERON:0006914 | 76.90 | gold quality |
| bone marrow | UBERON:0002371 | 76.79 | gold quality |
| large intestine | UBERON:0000059 | 76.22 | gold quality |
| intestine | UBERON:0000160 | 75.97 | gold quality |
| cortex of kidney | UBERON:0001225 | 75.87 | gold quality |
| metanephros | UBERON:0000081 | 75.72 | gold quality |
| granulocyte | CL:0000094 | 75.60 | gold quality |
| colon | UBERON:0001155 | 75.60 | gold quality |
| endometrium | UBERON:0001295 | 75.19 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 75.18 | gold quality |
| small intestine | UBERON:0002108 | 75.01 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 74.93 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 74.75 | gold quality |
| mammary duct | UBERON:0001765 | 74.73 | gold quality |
| mammary gland | UBERON:0001911 | 74.67 | gold quality |
| epithelium of mammary gland | UBERON:0003244 | 74.67 | gold quality |
| gall bladder | UBERON:0002110 | 74.61 | gold quality |
| stromal cell of endometrium | CL:0002255 | 74.56 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 74.38 | gold quality |
| caecum | UBERON:0001153 | 74.35 | gold quality |
| kidney | UBERON:0002113 | 74.32 | gold quality |
| sperm | CL:0000019 | 73.44 | gold quality |
| skin of hip | UBERON:0001554 | 73.36 | gold quality |
| prostate gland | UBERON:0002367 | 73.24 | gold quality |
| heart right ventricle | UBERON:0002080 | 73.22 | silver quality |
| adult mammalian kidney | UBERON:0000082 | 73.06 | gold quality |
| bone marrow cell | CL:0002092 | 72.93 | gold quality |
| upper leg skin | UBERON:0004262 | 72.58 | gold quality |
| metanephros cortex | UBERON:0010533 | 72.46 | gold quality |
| placenta | UBERON:0001987 | 72.45 | gold quality |
| lower lobe of lung | UBERON:0008949 | 72.45 | gold quality |
| lymph node | UBERON:0000029 | 72.44 | gold quality |
| blood | UBERON:0000178 | 72.29 | gold quality |
| tibia | UBERON:0000979 | 71.98 | gold quality |
| decidua | UBERON:0002450 | 71.75 | gold quality |
| right lung | UBERON:0002167 | 71.67 | gold quality |
| tonsil | UBERON:0002372 | 71.63 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 71.59 | gold quality |
| male germ cell | CL:0000015 | 71.56 | gold quality |
| pancreas | UBERON:0001264 | 71.41 | gold quality |
| spleen | UBERON:0002106 | 71.16 | gold quality |
| esophagus mucosa | UBERON:0002469 | 71.00 | gold quality |
| body of stomach | UBERON:0001161 | 70.86 | gold quality |
| lung | UBERON:0002048 | 70.59 | gold quality |
| jejunum | UBERON:0002115 | 70.35 | gold quality |
| fallopian tube | UBERON:0003889 | 69.59 | gold quality |
| right uterine tube | UBERON:0001302 | 69.32 | gold quality |
| uterus | UBERON:0000995 | 69.16 | gold quality |
| sigmoid colon | UBERON:0001159 | 69.06 | gold quality |
| urinary bladder | UBERON:0001255 | 69.00 | gold quality |
| stomach | UBERON:0000945 | 68.93 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 68.92 | gold quality |
| upper lobe of lung | UBERON:0008948 | 68.67 | gold quality |
| left coronary artery | UBERON:0001626 | 68.49 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 68.48 | gold quality |
| omental fat pad | UBERON:0010414 | 68.48 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 4.82 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 237 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Locus coeruleus | tissue | 192.6 | |
| Salivary gland | tissue | 87.8 | low |
| Colon | tissue | 86.5 | low |
| Rectum | tissue | 82.9 | low |
| Choroid plexus | tissue | 78.9 | |
| Superior colliculi | tissue | 76.8 | |
| Stomach 1 | tissue | 73.5 | medium |
| Small intestine | tissue | 70.4 | not detected |
| Esophagus | tissue | 64.3 | low |
| Placenta | tissue | 61.8 | medium |
| Vagina | tissue | 57.3 | not detected |
| Urinary bladder | tissue | 56.8 | not detected |
| Spinal cord | tissue | 53.7 | |
| Epididymis | tissue | 53.1 | low |
| Duodenum | tissue | 52.9 | not detected |
| Breast | tissue | 49.4 | not detected |
| Kidney | tissue | 46.1 | low |
| Adipose tissue | tissue | 45.8 | not detected |
| Fallopian tube | tissue | 43.5 | medium |
| Liver | tissue | 42.2 | not detected |
| Cervix | tissue | 41.1 | not detected |
| Endometrium 1 | tissue | 39.1 | not detected |
| Prostate | tissue | 38.8 | not detected |
| Bone marrow | tissue | 38.2 | not detected |
| Medulla oblongata | tissue | 37.4 | |
| Substantia nigra | tissue | 36.8 | |
| Pancreas | tissue | 35.8 | not detected |
| Locus coeruleus | tissue | 34.7 | |
| Smooth muscle | tissue | 34.5 | high |
| Gallbladder | tissue | 33.7 | low |
| Ovary | tissue | 31.5 | medium |
| Tonsil | tissue | 30.9 | not detected |
| Thalamus | tissue | 30.2 | |
| Medulla oblongata | tissue | 29.6 | |
| Thymus | tissue | 28.4 | |
| Skin 1 | tissue | 28.3 | not detected |
| Hippocampus | tissue | 27.6 | medium |
| Midbrain | tissue | 26.5 | |
| Tongue | tissue | 26.1 | |
| Nucleus accumbens | tissue | 26.1 | |
| Lymph node | tissue | 24.9 | not detected |
| Pons | tissue | 24.8 | |
| Thyroid gland | tissue | 24.5 | not detected |
| Corpus callosum | tissue | 23.9 | |
| Frontal cortex | tissue | 23.2 | |
| Postcentral gyrus | tissue | 23.2 | |
| Seminal vesicle | tissue | 22.9 | not detected |
| Spinal cord | tissue | 22.5 | |
| Hippocampal formation | tissue | 22.4 | |
| Appendix | tissue | 22.1 | not detected |
| Entorhinal cortex | tissue | 21.6 | |
| Lung | tissue | 21.0 | not detected |
| Putamen | tissue | 18.4 | |
| Septum | tissue | 18.4 | |
| Hypothalamus | tissue | 18.1 | |
| Pons | tissue | 17.9 | |
| Cerebral cortex | tissue | 17.8 | medium |
| Motor cortex | tissue | 17.8 | |
| Retrosplenial and cingulate cortex | tissue | 17.5 | |
| Ventral forebrain | tissue | 17.4 |
Brain sub-regions (HPA Brain Atlas): detected in 830; highest nTPM — Dorsal spinal cord (386.8), Median raphe nucleus (361.8), Dorsal hippocampus (327.4), Dorsal raphe nucleus (298.3), Lateral hypothalamic area (284.5).
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
Targeting NAT1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
showing 30 of 73 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-19A-3P | 99.98 | 75.33 | 2762 |
| HSA-MIR-19B-3P | 99.98 | 75.44 | 2754 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-4487 | 99.96 | 64.58 | 1252 |
| HSA-MIR-548AB | 99.95 | 71.31 | 3488 |
| HSA-MIR-559 | 99.95 | 72.28 | 3609 |
| 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 |
| HSA-MIR-548AU-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AY-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548B-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548BB-5P | 99.94 | 71.27 | 3509 |
| HSA-MIR-548C-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548D-5P | 99.94 | 71.23 | 3502 |
Functional genomics
gnomAD constraint: pLI 0.147, LOEUF 1.91, missense Z -0.828 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000307719 — one region, missense o/e 1.18.
Literature-anchored findings (GeneRIF, showing 40)
- Heart tube patterning in Drosophila requires integration of axial and segmental information provided by the Bithorax Complex genes and hedgehog signaling. (PMID:12223408)
- The analysis of these mutations has allowed us to define a new infraabdominal-8 regulatory region, located 5’ to the Abdominal-B transcription unit, and has helped to characterize better the complex regulation of the Abdominal-B gene. (PMID:12399311)
- The promoter targeting sequence (PTS) from the Abdominal-B locus of the bithorax complex facilitates the activity of a distantly located enhancer in transgenic embryos and it restricts the enhancer to a single promoter. (PMID:12490558)
- Data report the mapping of binding sites for ultrabithorax, Abd-A and Abd-B on polytene chromosomes in the Drospohila fat body. (PMID:12835385)
- the Fab-7 boundary contains separable regions that function at different stages of development (PMID:15329342)
- Abd-B acts at multiple levels to regulate gonad development and is a conserved factor in establishing gonad sexual dimorphism in diverse species. (PMID:15454263)
- certain mutations in Abd-B can be rescued in trans by the other copy of the gene in the genetic phenomenon known as transvection (PMID:15572134)
- The relationship between Abd-B and abd-A in the female genital disc is opposite to that of the embryonic epidermis, and contravenes the rule that posteriorly expressed Hox genes downregulate more anterior ones. (PMID:16319117)
- Abdominal-B Hox protein directly activates expression of the yellow pigmentation gene in posterior segments (PMID:16814723)
- Regulatory regons seems to control specifically the level of Abd-B expression in only one parasegment of the bithorax. (PMID:16818450)
- Abdominal-B induces the expression of four intermediate signaling molecules and transcription factors; this expression results in the mosaic activation of several realizator genes during the organogenesis of the external respiratory organ of the larva. (PMID:17113384)
- Enhancer interference limits the interaction of the Abdominal-B promoter to the enhancer(s) from only one regulatory domain in a specific abdominal segment. (PMID:17307884)
- the enhancer blocking capability of the Fab-8 insulator in stably transfected Drosophila S2 cells and show this activity depends on the Fab-8 CTCF binding sites (PMID:17825318)
- Fab-7 and Fab-8 boundaries effectively interact with the upstream region of the Abd-B promoter (PMID:18426914)
- development of the dorsal histoblast nests that will give rise to the adult epithelium is impaired in the posterior segments which identity is specified by Abdominal-B (PMID:18667003)
- Using gene conversion, we exchanged the Fab-7 and Fab-8 boundaries within the BX-C. (PMID:18987027)
- Studies indicate that interaction of Abdominal-B (ABD-B) with dorso ventral and intrasegmental positional information leads to the local activation of ABD-B primary targets in the dorsal region of the eighth abdominal segment (A8). (PMID:19247941)
- The promoter targeting sequences (PTS) from Abd-B locus overcome the enhancer blocking effect of insulators and facilitate long-range enhancer-promoter interactions in transgenic flies (PMID:20045684)
- Results suggest that the expression of cas is segment-specifically regulated negatively by Ubx and abdA genes, but positively by the AbdB gene. (PMID:20563987)
- Data show that the bithorax complex is an approximately 330kb genomic region that is responsible for directing the transcription of three homeotic (Hox) genes Ultrabithorax (Ubx), abdominal-A (abd-A) and Abdominal-B (Abd-B) during embryonic development. (PMID:21821017)
- By functionally dissecting the Abd-B protein, new features of Abd-B dependent target gene regulation were detected. (PMID:22005458)
- Dsx is a transcriptional target of Abdominal-B, and its regulation sculpts sex-specific abdomen morphology. (PMID:22488883)
- We also found that Abd-B expression in the secondary cells contributes to glycosylation of at least three accessory gland proteins: ovulin (Acp26Aa), CG1656, and CG1652 (PMID:23555301)
- Abdominal-B and caudal inhibit the formation of specific neuroblasts in the Drosophila tail region. (PMID:23903193)
- ABD-B binds more strongly to oligonucleotides containing two 5’-TTAT-3’ canonical core motifs than the probe containing the 5’-TTAC-3’ motif. (PMID:24219869)
- Abd-B provides cues for integrin localization, critical for stem cell positioning. (PMID:24480643)
- Abd-B is required in neurons during development for females to become highly receptive to male courtship. Abd-B neurons control pausing, a key aspect of female sexual receptivity, in response to male courtship. (PMID:24998527)
- We also observed that these functions of abd-A are required in its exclusive as well as the coexpression domain with that of Abd-B (PMID:25340649)
- analysis of blocking and bypass activities of the Fab-8 boundary in the Drosophila bithorax complex (PMID:27428541)
- Data report that the repression of Abd-B, in cyst stem cells (CySCs) is essential for the homeostasis and cell identity maintenance in the adult Drosophila testis. Derepression of Abd-B in CySCs disrupts the proper self-renewal of both germline stem cells (GSCs) and CySCs, and leads to an excessive expansion of early stage somatic cells, which originate from both lineages. (PMID:28698559)
- iab-7 polycomb response element (PRE) functions as a component of the Fab-7 boundary. The boundary activity of the iab-7 PRE sequence depends upon a complex called the LBC, LBC is a multiprotein complex that contains at least three distinct DNA binding proteins, the GAGA factor (GAF), Clamp, and Mod(mdg4). (PMID:30110328)
- complete reconstitution of bypass and blocking functions (PMID:31209019)
- The capacity of Abdominal-B to use the sex-specific isoform of Dsx as a cofactor underlines the possibility that these two classes of protein are capable of cooperating in selection and regulation of target genes in a tissue- and sex-specific manner (PMID:31371379)
- Redundant enhancers in the iab-5 domain cooperatively activate Abd-B in the A5 and A6 abdominal segments of Drosophila. (PMID:34473267)
- The Drosophila Fab-7 boundary modulates Abd-B gene activity by guiding an inversion of collinear chromatin organization and alternate promoter use. (PMID:36640345)
- Boundary bypass activity in the abdominal-B region of the Drosophila bithorax complex is position dependent and regulated. (PMID:37582404)
- the formation of the buried hydrophobic stacks is critical for the correct folding of the parallel beta-helix, triple-stranded beta-helix, and beta-prism domains in the tailspike protein. (PMID:15322277)
- These results underscore the importance of the TSP C-terminus in the assembly of the mature trimer and demonstrate its potential utility as a model to study the folding and assembly of the TSP C-terminus in isolation. (PMID:19196242)
- TSP morphology controls viral DNA release. (PMID:22364412)
- Crystal structure of the tailspike protein and its interdomain linker (PMID:24816102)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | zgc:101040 | ENSDARG00000005176 |
| danio_rerio | si:dkey-78a14.4 | ENSDARG00000036066 |
| mus_musculus | Nat1 | ENSMUSG00000025588 |
| mus_musculus | Nat2 | ENSMUSG00000051147 |
| mus_musculus | Nat3 | ENSMUSG00000056426 |
| rattus_norvegicus | Nat2 | ENSRNOG00000029977 |
| rattus_norvegicus | Nat1 | ENSRNOG00000049498 |
| rattus_norvegicus | Nat3 | ENSRNOG00000074135 |
Paralogs (1): NAT2 (ENSG00000156006)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:97279) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 2 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| reduced fertility | 1 |
| decreased liver enzyme/coenzyme activity | 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 |
|---|---|---|---|
| Oryctolagus cuniculus | P11246 | 95.2% | Diamond |
| Mesocricetus auratus | P50293 | 93.1% | Diamond |
| Macaca mulatta | Q7YRG5 | 89.0% | Diamond |
| Felis catus | O62696 | 83.3% | Diamond |
| Bos taurus | Q1JPA6 | 82.8% | Diamond |
| Salmonella enterica subsp. enterica serovar Typhimurium str. LT2 | Q00267 | 74.4% | Diamond |
| Gallus gallus | P13913 | 65.4% | Diamond |
| Mycolicibacterium smegmatis | O86309 | 60.9% | 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 |
|---|---|---|
| ASAH1-AS1 | ncRNA | 101929066 |
| ASAH1 | protein-coding | 427 |
| PCM1 | protein-coding | 5108 |
| NAT2 | protein-coding | 10 |
Protein
Protein identifiers
Arylamine N-acetyltransferase 1 — P18440 (reviewed: P18440)
Alternative names: Arylamide acetylase 1, Monomorphic arylamine N-acetyltransferase, N-acetyltransferase type 1
All UniProt accessions (2): P18440, F5H5R8
UniProt curated annotations — full annotation on UniProt →
Function. Participates in the detoxification of a plethora of hydrazine and arylamine drugs. Catalyzes the N- or O-acetylation of various arylamine and heterocyclic amine substrates and is able to bioactivate several known carcinogens.
Subcellular location. Cytoplasm.
Polymorphism. N-acetylation polymorphism is determined by a low or high NAT activity in liver and has been implicated in the action and toxicity of amine-containing drugs. Slow acetylation genotypes have been associated with significant lung cancer risk. Candidate risk factor for susceptibility to neural tube defects. The NAT1*10 allele has been associated with increased risk of colon and urinary bladder cancers and with higher levels of N-acetyltransferase activity and DNA adducts in aromatic amine tumor target organs such as colon and urinary bladder.
Miscellaneous. NAT1 was historically considered to be monomorphic in nature but reports of allelic variations at the NAT1 locus suggest that it is a polymorphically expressed enzyme.
Similarity. Belongs to the arylamine N-acetyltransferase family.
RefSeq proteins (10): NP_000653, NP_001153642, NP_001153643, NP_001153644, NP_001153645, NP_001153646, NP_001153647, NP_001153648, NP_001153651, NP_001278891 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001447 | Arylamine_N-AcTrfase | Family |
| IPR038765 | Papain-like_cys_pep_sf | Homologous_superfamily |
| IPR053710 | Arylamine_NAT_domain_sf | Homologous_superfamily |
Pfam: PF00797
Enzyme classification (BRENDA)
- EC 2.3.1.5 — arylamine N-acetyltransferase (BRENDA: 76 organisms, 504 substrates, 242 inhibitors, 322 Km, 150 kcat entries)
- EC 3.1.2.1 — acetyl-CoA hydrolase (BRENDA: 33 organisms, 27 substrates, 33 inhibitors, 16 Km, 2 kcat entries)
Substrate kinetics (BRENDA)
94 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| 2-AMINOFLUORENE | 0.0002–5.8 | 50 |
| ACETYL-COA | 0.0084–560 | 23 |
| 5-AMINOSALICYLIC ACID | 0.0067–1.7 | 16 |
| ISONIAZID | 0.18–102 | 14 |
| ACETYL-COA | 0.0001–15 | 14 |
| P-AMINOBENZOIC ACID | 0.0028–152 | 13 |
| SULFAMETHAZINE | 0.02–5.39 | 11 |
| 4-NITROPHENYL ACETATE | 0.164–10 | 9 |
| HYDRALAZINE | 0.0134–1.327 | 9 |
| 4-AMINOSALICYLATE | 0.0941–3.827 | 8 |
| 4-AMINOSALICYLIC ACID | 0.258–2.2 | 8 |
| 4-AMINOBENZOIC ACID | 0.049–166 | 7 |
| 5-AMINOSALICYLATE | 0.2–0.662 | 7 |
| 4-AMINOBIPHENYL | 0.0058–1.57 | 5 |
| P-AMINOSALICYLIC ACID | 0.059–5.39 | 5 |
Catalyzed reactions (Rhea)
- an arylamine + acetyl-CoA = an N-acetylarylamine + CoA (RHEA:16613)
- an N-hydroxyarylamine + acetyl-CoA = an N-acetoxyarylamine + CoA (RHEA:20277)
UniProt features (48 total): strand 13, helix 12, sequence variant 11, binding site 5, active site 3, chain 1, mutagenesis site 1, turn 1, modified residue 1
Structure
Experimental structures (PDB)
2 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 2IJA | Human N-acetyltransferase 1 F125S mutant | X-RAY DIFFRACTION | 1.7 |
| 2PQT | Human N-acetyltransferase 1 | X-RAY DIFFRACTION | 1.78 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P18440-F1 | 98.20 | 0.99 |
Human Protein Atlas
Protein class: Metabolic proteins, Transporters, Electrochemical Potential-driven transporters, Predicted membrane proteins, Plasma proteins, Disease related genes, FDA approved drug targets, Small molecule drugs, Human disease related genes
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cytosol; mitochondria
Antibody reliability (HPA): IH enhanced · IF approved
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 |
|---|---|
| 68 | acyl-thioester intermediate |
| 107 | |
| 122 |
Ligand- & substrate-binding residues (5)
| Position | Role |
|---|---|
| 103 | CoA |
| 104 | CoA |
| 106–107 | substrate |
| 208 | CoA |
| 214 | CoA |
Post-translational modifications (1)
| Type | Positions |
|---|---|
| N-acetylmethionine | 1 |
Mutagenesis-validated functional residues (1)
| Position | Phenotype |
|---|---|
| 64 | reduced enzymatic activity. |
Function
Pathways and Gene Ontology
Reactome pathways
2 curated (TAS) of 6; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
6 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-156582 | Acetylation | curated |
| R-HSA-9753281 | Paracetamol ADME | curated |
| R-HSA-211859 | Biological oxidations | — |
| R-HSA-9748784 | Drug ADME | — |
| R-HSA-1430728 | Metabolism | — |
| R-HSA-156580 | Phase II - Conjugation of compounds | — |
MSigDB gene sets: 168 (showing top):
WALLACE_PROSTATE_CANCER_RACE_UP, REACTOME_BIOLOGICAL_OXIDATIONS, GOZGIT_ESR1_TARGETS_DN, GAUSSMANN_MLL_AF4_FUSION_TARGETS_A_DN, DACOSTA_UV_RESPONSE_VIA_ERCC3_UP, SMID_BREAST_CANCER_RELAPSE_IN_LUNG_DN, BROWNE_HCMV_INFECTION_16HR_UP, PUJANA_CHEK2_PCC_NETWORK, RUTELLA_RESPONSE_TO_CSF2RB_AND_IL4_UP, SMID_BREAST_CANCER_LUMINAL_B_UP, DACOSTA_UV_RESPONSE_VIA_ERCC3_COMMON_UP, HELLER_HDAC_TARGETS_SILENCED_BY_METHYLATION_UP, RIGGINS_TAMOXIFEN_RESISTANCE_DN, SPIELMAN_LYMPHOBLAST_EUROPEAN_VS_ASIAN_DN, XU_GH1_AUTOCRINE_TARGETS_DN
GO Biological Process (1): xenobiotic metabolic process (GO:0006805)
GO Molecular Function (6): arylamine N-acetyltransferase activity (GO:0004060), protein-cysteine S-acyltransferase activity (GO:0019707), protein binding (GO:0005515), acetyltransferase activity (GO:0016407), transferase activity (GO:0016740), acyltransferase activity (GO:0016746)
GO Cellular Component (2): cytosol (GO:0005829), cytoplasm (GO:0005737)
Reactome top-level categories
4 top-level categories:
| Category | Pathways |
|---|---|
| Phase II - Conjugation of compounds | 1 |
| Drug ADME | 1 |
| Biological oxidations | 1 |
| Metabolism | 1 |
GO top-level categories
11 GO namespaces:
| Category | Terms |
|---|---|
| acyltransferase activity, transferring groups other than amino-acyl groups | 2 |
| cellular anatomical structure | 2 |
| metabolic process | 1 |
| cellular response to xenobiotic stimulus | 1 |
| N-acetyltransferase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| catalytic activity | 1 |
| transferase activity | 1 |
| cytoplasm | 1 |
| intracellular anatomical structure | 1 |
Protein interactions and networks
STRING
showing 15 of 462 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| NAT1 | AADAC | P22760 | 840 |
| NAT1 | GATD3 | P0DPI2 | 760 |
| NAT1 | PNOC | Q13519 | 756 |
| NAT1 | MNAT1 | P51948 | 746 |
| NAT1 | ESCO1 | Q5FWF5 | 706 |
| NAT1 | ESCO2 | Q56NI9 | 705 |
| NAT1 | NAA15 | Q9BXJ9 | 692 |
| NAT1 | PSCA | O43653 | 668 |
| NAT1 | CYP2E1 | P05181 | 655 |
| NAT1 | CHRNA2 | Q15822 | 616 |
| NAT1 | AANAT | Q16613 | 555 |
| NAT1 | MUC6 | Q6W4X9 | 552 |
| NAT1 | ASMT | P46597 | 529 |
| NAT1 | PPP3CC | P48454 | 510 |
| NAT1 | MUTYH | Q9UIF7 | 508 |
IntAct
Human interaction partners of NAT1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
2 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| ICAM1 | physical association | 0.590 | 2 |
| MRRF | association | 0.350 | 1 |
BioGRID (10 interactions; top human partners by supporting records): ICAM1 (Affinity Capture-MS; 3 records), APEX1 (Affinity Capture-RNA), FTO (Affinity Capture-MS), KRAS (Synthetic Lethality), MRRF (Affinity Capture-MS), NR2C2 (Affinity Capture-MS), SBDS (Affinity Capture-MS), SNTA1 (Protein-peptide)
SIGNOR signaling
1 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| AR | “up-regulates quantity by expression” | NAT1 | “transcriptional regulation” |
Disease & clinical
Genetic variants
Variant evidence for NAT1: 58 ClinVar records (0 pathogenic / likely pathogenic).
ClinVar
58 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 37 |
| Likely benign | 10 |
| Benign | 2 |
HPA cancer prognostics
RNA cancer specificity: Cancer enhanced (Liver Hepatocellular Carcinoma)
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
10 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Colon Adenocarcinoma (TCGA) | favorable | 1.22e-06 |
| Kidney Renal Clear Cell Carcinoma (TCGA) | favorable | 2.9e-06 |
| Kidney Renal Clear Cell Carcinoma (TCGA) | favorable | 2.2e-05 |
| Liver Hepatocellular Carcinoma (TCGA) | unfavorable | 5.63e-05 |
| Glioblastoma Multiforme (validation) | favorable | 0.000228 |
| Liver Hepatocellular Carcinoma (TCGA) | unfavorable | 0.00024 |
| Pancreatic Adenocarcinoma (TCGA) | unfavorable | 0.000355 |
| Breast Invasive Carcinoma (validation) | favorable | 0.00048 |
| Lung Adenocarcinoma (validation) | unfavorable | 0.000799 |
| Ovary Serous Cystadenocarcinoma (validation) | unfavorable | 0.000951 |
Disease associations
OMIM: gene MIM:108345 | disease phenotypes:
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5101 (SINGLE PROTEIN)
PharmGKB: 1 entry (CPIC guideline: no)
Binding affinities (BindingDB)
37 measured of 44 human assays (48 total across all organisms); most potent 37 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| CHEMBL3262086 | IC50 | 120 nM |
| (Z)-5-(3’,5’-Diiodo-4’-hydroxybenzylidene)-2-thioxothiazolidine-4-one | IC50 | 138 nM |
| CHEMBL3262085 | IC50 | 540 nM |
| (Z)-5-(3’-Hydroxybenzylidene)-2-thioxothiazolidin-4-one | IC50 | 600 nM |
| CHEMBL3262049 | IC50 | 900 nM |
| (Z)-5-(2’-Hydroxybenzylidene)-2-thioxothiazolidin-4-one | IC50 | 1100 nM |
| (Z)-3-Amino-5-(4’-hydroxy-3’,5-diiodobenzylidene)-2-thioxo-thiazolidin-4-one | IC50 | 1100 nM |
| CHEMBL2047717 | IC50 | 1100 nM |
| CHEMBL1568345 | IC50 | 1700 nM |
| CHEMBL3262055 | IC50 | 1900 nM |
| CHEMBL3262084 | IC50 | 2600 nM |
| CHEMBL3262053 | IC50 | 2800 nM |
| (Z)-5-(3’,4’-Dichlorobenzylidene)-2-thioxothiazolidin-4-one | IC50 | 3400 nM |
| 2-Hydroxy-5-[1-(4-hydroxy-3,5-diiodo-phenyl)-meth-(Z)-ylidene]-thiazol-4-one | IC50 | 3600 nM |
| (Z)-5-(2’-Methylbenzylidene)-2-thioxothiazolidin-4-one | IC50 | 3900 nM |
| CHEMBL3262048 | IC50 | 4100 nM |
| CHEMBL3262082 | IC50 | 4200 nM |
| 5-(4-chlorobenzylidene)-2-thioxothiazolidin-4-one | IC50 | 4700 nM |
| CHEMBL3262087 | IC50 | 5800 nM |
| CHEMBL3262077 | IC50 | 6600 nM |
| (Z)-5-(4’-Hydroxy-3’,5’-diiodobenzylidene)-3-methyl-2-thioxothiazolidin-4-one | IC50 | 7600 nM |
| CHEMBL3262056 | IC50 | 8000 nM |
| (Z)-5-(4’-Biphenylmethylene)-2-thioxothiazolidin-4-one | IC50 | 8100 nM |
| CHEMBL3262059 | IC50 | 8400 nM |
| CHEMBL3262061 | IC50 | 9600 nM |
| CHEMBL3262062 | IC50 | 10000 nM |
| CHEMBL3262073 | IC50 | 10000 nM |
| CHEMBL3262060 | IC50 | 10300 nM |
| CHEMBL3262054 | IC50 | 12100 nM |
| CHEMBL3262058 | IC50 | 12100 nM |
| (Z)-5-(4’-Fluorobenzylidene)-2-thioxothiazolidin-4-one | IC50 | 12900 nM |
| CHEMBL3262057 | IC50 | 14500 nM |
| (Z)-5-(3’-Methylbenzylidene)-2-thioxothiazolidin-4-one | IC50 | 17000 nM |
| (Z)-5-(2’-Methoxybenzylidene)-2-thioxothiazolidin-4-one | IC50 | 17600 nM |
| CHEMBL3262074 | IC50 | 19000 nM |
| CHEMBL3262076 | IC50 | 19300 nM |
| CHEMBL3262075 | IC50 | 22100 nM |
ChEMBL bioactivities
28 potent at pChembl≥5 of 40 total, top 28 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 6.92 | IC50 | 120 | nM | CHEMBL3262086 |
| 6.86 | IC50 | 138 | nM | CHEMBL458614 |
| 6.48 | IC50 | 330 | nM | CHEMBL458614 |
| 6.27 | IC50 | 540 | nM | CHEMBL3262085 |
| 6.22 | IC50 | 600 | nM | CHEMBL457919 |
| 6.05 | IC50 | 900 | nM | CHEMBL3262049 |
| 5.96 | IC50 | 1100 | nM | CHEMBL2047717 |
| 5.96 | IC50 | 1100 | nM | CHEMBL431550 |
| 5.96 | IC50 | 1100 | nM | CHEMBL511165 |
| 5.77 | IC50 | 1700 | nM | CHEMBL1568345 |
| 5.72 | IC50 | 1900 | nM | CHEMBL3262055 |
| 5.58 | IC50 | 2600 | nM | CHEMBL3262084 |
| 5.55 | IC50 | 2800 | nM | CHEMBL3262053 |
| 5.47 | IC50 | 3400 | nM | CHEMBL506606 |
| 5.44 | IC50 | 3600 | nM | CHEMBL110470 |
| 5.41 | IC50 | 3900 | nM | CHEMBL458705 |
| 5.39 | IC50 | 4100 | nM | CHEMBL3262048 |
| 5.38 | IC50 | 4200 | nM | CHEMBL3262082 |
| 5.33 | IC50 | 4700 | nM | CHEMBL201467 |
| 5.24 | IC50 | 5800 | nM | CHEMBL3262087 |
| 5.18 | IC50 | 6600 | nM | CHEMBL3262077 |
| 5.12 | IC50 | 7600 | nM | CHEMBL456849 |
| 5.10 | IC50 | 8000 | nM | CHEMBL3262056 |
| 5.09 | IC50 | 8100 | nM | CHEMBL502693 |
| 5.08 | IC50 | 8400 | nM | CHEMBL3262059 |
| 5.02 | IC50 | 9600 | nM | CHEMBL3262061 |
| 5.00 | IC50 | 1e+04 | nM | CHEMBL3262062 |
| 5.00 | IC50 | 1e+04 | nM | CHEMBL3262073 |
PubChem BioAssay actives
27 with measured affinity, of 59 total; 26 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-(8-amino-3-anilino-1,4-dioxonaphthalen-2-yl)benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 0.1200 | uM |
| (5Z)-5-[(4-hydroxy-3,5-diiodophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346067: Inhibition of NAT1 in human ZR75 cell lysate assessed as acetylation of aryl amine using PABA as substrate | ic50 | 0.1380 | uM |
| N-[8-amino-3-(3,5-dimethylanilino)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 0.5400 | uM |
| (5Z)-5-[(3-hydroxyphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 0.6000 | uM |
| N-[3-(4-bromoanilino)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 0.9000 | uM |
| (5Z)-5-[(2-hydroxyphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 1.1000 | uM |
| (5Z)-3-amino-5-[(4-hydroxy-3,5-diiodophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 1.1000 | uM |
| N-(3-anilino-1,4-dioxonaphthalen-2-yl)benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 1.7000 | uM |
| N-[3-(4-bromophenoxy)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 1.9000 | uM |
| N-[7-amino-3-(3,5-dimethylanilino)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 2.6000 | uM |
| N-(1,4-dioxo-3-phenoxynaphthalen-2-yl)benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 2.8000 | uM |
| (5Z)-5-[(3,4-dichlorophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 3.4000 | uM |
| (5Z)-5-[(4-hydroxy-3,5-diiodophenyl)methylidene]-1,3-thiazolidine-2,4-dione | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 3.6000 | uM |
| (5Z)-5-[(2-methylphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 3.9000 | uM |
| N-[3-(3,5-dimethylanilino)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 4.1000 | uM |
| N-[5-amino-3-(3,5-dimethylanilino)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 4.2000 | uM |
| (5Z)-5-[(4-chlorophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 4.7000 | uM |
| N-[3-(3,5-dimethylanilino)-1,4-dioxonaphthalen-2-yl]-N-methylbenzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 5.8000 | uM |
| N-[3-(3,5-dimethylanilino)-5-nitro-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 6.6000 | uM |
| (5Z)-5-[(4-hydroxy-3,5-diiodophenyl)methylidene]-3-methyl-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 7.6000 | uM |
| N-[3-(2-chlorophenyl)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 8.0000 | uM |
| (5Z)-5-[(4-phenylphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 346066: Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman’s method | ic50 | 8.1000 | uM |
| N-[3-(3-formylphenyl)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 8.4000 | uM |
| N-[3-(furan-2-yl)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 9.6000 | uM |
| N-[3-(furan-3-yl)-1,4-dioxonaphthalen-2-yl]benzenesulfonamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 10.0000 | uM |
| N-[3-(3-formylphenyl)-1,4-dioxonaphthalen-2-yl]benzamide | 1141283: Inhibition of human NAT1 assessed as rate of free thiol coenzyme A production using arylamine and AcCoA as substrate by Ellman’s method | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
119 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| 4-Aminobenzoic Acid | increases reaction, affects acetylation, increases metabolic processing, decreases reaction, increases acetylation | 7 |
| Tobacco Smoke Pollution | affects reaction, increases abundance, affects response to substance, affects expression, decreases expression (+1 more) | 7 |
| Valproic Acid | decreases methylation, affects cotreatment, increases expression, affects expression | 7 |
| 4-biphenylamine | increases response to substance, increases mutagenesis, increases acetylation, increases activity, affects response to substance | 5 |
| 2-aminofluorene | increases acetylation, increases metabolic processing | 5 |
| Estradiol | increases expression, decreases expression, affects cotreatment | 4 |
| sodium arsenite | increases expression, increases methylation | 3 |
| benzidine | affects acetylation, affects response to substance, affects expression, affects mutagenesis, increases activity (+1 more) | 3 |
| Air Pollutants | increases abundance, increases expression, affects expression, decreases expression, affects cotreatment | 3 |
| Benzo(a)pyrene | affects methylation, increases expression, affects response to substance | 3 |
| Hydrogen Peroxide | decreases activity, decreases reaction | 3 |
| Aflatoxin B1 | decreases methylation, increases expression, affects cotreatment, increases response to substance | 3 |
| methylmercuric chloride | decreases expression | 2 |
| 4-phenylenediamine | decreases activity, decreases expression, increases acetylation | 2 |
| 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine | increases expression, affects response to substance | 2 |
| 2-hydroxyamino-1-methyl-6-phenylimidazo(4,5-b)pyridine | affects acetylation, affects activity, increases metabolic processing | 2 |
| 3-nitrobenzanthrone | increases activity, affects cotreatment, increases reduction | 2 |
| Acetyl Coenzyme A | decreases activity, decreases reaction, affects cotreatment, increases activity, increases reduction (+1 more) | 2 |
| Aerosols | decreases expression, affects expression | 2 |
| Cotinine | affects response to substance, affects abundance, affects reaction, increases abundance | 2 |
| Folic Acid | decreases activity, increases acetylation | 2 |
| Ozone | affects cotreatment, increases expression, increases abundance, affects expression | 2 |
| Aminosalicylic Acid | increases acetylation | 2 |
| Pentachlorophenol | decreases reaction, increases acetylation, decreases activity | 2 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Tetrachlorodibenzodioxin | increases expression, affects cotreatment | 2 |
| Toluene 2,4-Diisocyanate | affects response to substance, increases response to substance | 2 |
| Cyclosporine | decreases expression | 2 |
| Paclitaxel | decreases activity, decreases expression | 2 |
| p-Chloromercuribenzoic Acid | affects cotreatment, increases expression | 2 |
ChEMBL screening assays
10 unique, capped per target: 7 binding, 3 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3077325 | Binding | Inhibition of Homo sapiens (human) arylamine N-acetyltransferase 1 | Design, synthesis, and biological evaluation of new 4-thiazolidinone derivatives substituted with benzimidazole ring as potential chemotherapeutic agents — *Med Chem Res* |
| CHEMBL3529019 | ADMET | Increase in NAT1 enzyme activity in human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control | Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. — *Drug Metab Dispos* |
Cellosaurus cell lines
21 cell lines: 12 spontaneously immortalized cell line, 9 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_8558 | YG10007 | Spontaneously immortalized cell line | Female |
| CVCL_A2GZ | V79MZh1A2/hNAT1 | Spontaneously immortalized cell line | Male |
| CVCL_A9BA | MDA-MB-231 NAT1 scrambled | Cancer cell line | Female |
| CVCL_A9BB | MDA-MB-231 NAT1 down | Cancer cell line | Female |
| CVCL_A9BC | MDA-MB-231 NAT1 up | Cancer cell line | Female |
| CVCL_A9BD | MDA-MB-231 NAT1+/- 2-12 | Cancer cell line | Female |
| CVCL_A9BE | MDA-MB-231 NAT1-/- 2-19 | Cancer cell line | Female |
| CVCL_A9BF | MDA-MB-231 NAT1-/- 5-50 | Cancer cell line | Female |
| CVCL_D1NY | Abcam K-562 NAT1 KO | Cancer cell line | Female |
| CVCL_D2KI | Abcam Raji NAT1 KO | Cancer cell line | Male |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for NAT1 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Pharmacogenomically associated drugs (drugs whose metabolism/response is associated with variants in this gene (PharmGKB) — not drugs that target it): Mesalamine, Thioguanine