T3D0127 - Chlorpyrifos
| Record Information | |
|---|---|
| Version | 1.0 |
| Creation Date | 2009-03-06 18:58:07 UTC |
| Update Date | 2013-04-25 08:32:57 UTC |
| Accession Number | T3D0127 |
| Identification | |
| Common Name | Chlorpyrifos |
| Description | Chlorpyrifos is an organophosphate insecticide. In the home, it is used to control cockroaches, fleas, and termites; it is also used in some pet flea and tick collars. On the farm, it is used to control ticks on cattle and as a spray to control crop pests. (R488) |
| Compound Type |
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| Chemical Structure |
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| Synonyms |
|
| Chemical Formula | C9H11Cl3NO3PS |
| Average Molecular Weight | 350.586 |
| Monoisotopic Molecular Weight | 348.926283546 |
| Chemical IUPAC Name | chlorpyrifos |
| CAS Registry Number | 2921-88-2 |
| SMILES | CCOP(=S)(OCC)OC1=NC(Cl)=C(Cl)C=C1Cl |
| InChI Identifier | InChI=1S/C9H11Cl3NO3PS/c1-3-14-17(18,15-4-2)16-9-7(11)5-6(10)8(12)13-9/h5H,3-4H2,1-2H3 |
| InChI Key | InChIKey=SBPBAQFWLVIOKP-UHFFFAOYSA-N |
| Chemical Taxonomy | |
| Kingdom | Organic Compounds |
| Super Class | Heterocyclic Compounds |
| Class | Pyridines and Derivatives |
| Sub Class | Hydropyridines |
| Direct Parent | Pyridinones |
| Alternative Parents |
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| Molecular Framework | Aromatic Heteromonocyclic Compounds |
| Substituents |
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| External Descriptors |
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| External Links | |
| DrugBank ID | Not Available |
| PubChem Compound ID | 2730 ![]() |
| KEGG ID | C14322 ![]() |
| UniProt ID | Not Available |
| OMIM ID | Not Available |
| ChEBI ID | 34631 ![]() |
| BioCyc ID | Not Available |
| CTD ID | D004390 ![]() |
| Stitch ID | Chlorpyrifos ![]() |
| PDB ID | Not Available |
| ACToR ID | 465 |
| Wikipedia Link | http://en.wikipedia.org/wiki/Chlorpyrifos ![]() |
| Physical Properties | |
| Appearance | White crystals. |
| Melting Point | 42 C |
| Solubility | 0.00112 mg/mL at 24 °C [YALKOWSKY,SH & DANNENFELSER,RM (1992)] |
| Predicted LogP | 4.784318596666666 |
| Toxicity Profile | |
| Route of Exposure | Oral (R488) ; inhalation (R488) ; dermal (R488) |
| Mechanism of Action | Chlorpyrifos and its bioactivation product, chlorpyrifos oxon, inhibit neural acetylcholinesterase by forming a stable covalent bond at the active site. The result of this acetylcholinesterase inhibition is cholinergic overstimulation of the central nervous system. Chlorpyrifos oxon also binds to muscarinic receptors, altering the signal transduction, which affects cellular signalling and disrupts neurological function. It also inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. Chlorpyrifos alters cytochrome P-450 levels, controlling the metabolism of itself and other xenobiotics, and inhibits neuropathy target esterase, producing ataxia. (R488, R495, R497, R499, R973)) |
| Metabolism | Chlorpyrifos is absorbed mainly via ingestion and inhalation, but may also be absorbed to a lesser extent through the skin. Chlorpyrifos rapidly distributes to all the major organs and is bioactivated to chlorpyrifos oxon in the liver via cytochrome P-450-dependent desulfuration. The oxon is hydrolyzed by A-esterase to diethylphosphate and 3,5,6-trichloro-2-pyridinol (TCP), the major metabolite. Chlorpyrifos is primarily excreted in the urine in the form of TCP conjugates. (R488) |
| Toxicity Values | LD50: 102 mg/kg (Oral, Rat) (R490) LD50: 1233 mg/kg (Dermal, Rabbit) (R490) LD50: 192 mg/kg (Intraperitoneal, Mouse) (R263) LC50: 560 mg/m3 over 4 hours (Inhalation, Rat) (R490) |
| Lethal Dose | 300 mg/kg for an adult human. (R293) |
| Carcinogenicity (IARC Classification) | Not Available |
| Uses/Sources | Chlorpyrifos is used as a pesticide. In the home, it is used to control cockroaches, fleas, and termites; it is also used in some pet flea and tick collars. On the farm, it is used to control ticks on cattle and as a spray to control crop pests. (R488) |
| Minimum Risk Level | Acute Oral: 0.003 mg/kg/day (R260) Intermediate Oral: 0.003 mg/kg/day (R260) Chronic Oral: 0.001 mg/kg/day (R260) |
| Health Effects | Chlorpyrifos damages the nervous system. High levels may result in severe sweating, loss of bowel control, severe muscle tremors, seizures, loss of consciousness, coma, or death. (R488) |
| Symptoms | Chlorpyrifos exposure may produce a variety of effects on the nervous system including headaches, blurred vision, lacrimation, excessive salivation, runny nose, dizziness, confusion, muscle weakness or tremors, nausea, diarrhea, and sudden changes in heart rate. High levels may result in severe sweating, loss of bowel control, severe muscle tremors, seizures, loss of consciousness, coma, or death. (R488) |
| Treatment | The effects of chlorpyrifos can be reversed by administration of the cholinergic blocking agent, atropine. (R488) |
| References | |
| General References |
|
Targets
1. Acetylcholinesterase
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Chlorpyrifos and its bioactivation product, chlorpyrifos oxon, and inhibit neural acetylcholinesterase by forming a stable covalent bond at the active site. The result of this acetylcholinesterase inhibition is cholinergic overstimulation of the central nervous system. (R488)UniProt ID: P22303

Gene: ACHE

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R488 — ATSDR - Agency for Toxic Substances and Disease Registry (1997). Toxicological profile for chlorpyrifos. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
2. Muscarinic acetylcholine receptor M1
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (R495)UniProt ID: P11229

Gene: CHRM1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R495 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.
[7513360
]
3. Muscarinic acetylcholine receptor M2
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition.
Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (R495)UniProt ID: P08172

Gene: CHRM2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R495 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.
[7513360
]
4. Muscarinic acetylcholine receptor M3
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (R495)UniProt ID: P20309

Gene: CHRM3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R495 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.
[7513360
]
5. Muscarinic acetylcholine receptor M4
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (R495)UniProt ID: P08173

Gene: CHRM4

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R495 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.
[7513360
]
6. Muscarinic acetylcholine receptor M5
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (R495)UniProt ID: P08912

Gene: CHRM5

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R495 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.
[7513360
]
7. Serum albumin
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Chlorpyrifos oxon binds albumin and may generate an antibody response. (R496)UniProt ID: P02768

Gene: ALB

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R496 — Li B, Schopfer LM, Hinrichs SH, Masson P, Lockridge O: Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry assay for organophosphorus toxicants bound to human albumin at Tyr411. Anal Biochem. 2007 Feb 15;361(2):263-72. Epub 2006 Dec 4.
[17188226
]
8. Cytochrome P450 3A4
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide.
Chlorpyrifos is an irreversible non-competitive inhibitor of cytochrome P-450 3A4. (R498)UniProt ID: P08684

Gene: CYP3A4

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R498 — Usmani KA, Hodgson E, Rose RL: In vitro metabolism of carbofuran by human, mouse, and rat cytochrome P450 and interactions with chlorpyrifos, testosterone, and estradiol. Chem Biol Interact. 2004 Dec 7;150(3):221-32.
[15560889
]
9. Neuropathy target esterase
Phospholipase B that deacylates intracellular phosphatidylcholine (PtdCho), generating glycerophosphocholine (GroPtdCho). This deacylation occurs at both sn-2 and sn-1 positions of PtdCho. Its specific chemical modification by certain organophosphorus (OP) compounds leads to distal axonopathy.
Chlorpyrifos inhibits neuropathy target esterase, producing ataxia. (R499)UniProt ID: Q8IY17

Gene: PNPLA6

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R499 — Richardson RJ, Moore TB, Kayyali US, Fowke JH, Randall JC: Inhibition of hen brain acetylcholinesterase and neurotoxic esterase by chlorpyrifos in vivo and kinetics of inhibition by chlorpyrifos oxon in vitro: application to assessment of neuropathic risk. Fundam Appl Toxicol. 1993 Apr;20(3):273-9.
[7684990
]
10. Cannabinoid receptor 1
Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.
Chlorpyrifos oxon inhibits cannabinoid receptor 1. (R500)UniProt ID: P21554

Gene: CNR1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R500 — Quistad GB, Nomura DK, Sparks SE, Segall Y, Casida JE: Cannabinoid CB1 receptor as a target for chlorpyrifos oxon and other organophosphorus pesticides. Toxicol Lett. 2002 Sep 5;135(1-2):89-93.
[12243867
]
11. Fatty-acid amide hydrolase 1
Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules. Hydrolyzes polyunsaturated substrate anandamide preferentially as compared to monounsaturated substrates.
Chlorpyrifos inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. (R973)UniProt ID: O00519

Gene: FAAH

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R973 — Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55.
[11350214
]
12. Fatty-acid amide hydrolase 2
Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules. Hydrolyzes monounsaturated substrate anandamide preferentially as compared to polyunsaturated substrates.
Chlorpyrifos inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. (R973)UniProt ID: Q6GMR7

Gene: FAAH2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R973 — Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55.
[11350214
]
13. Calcium-transporting ATPase type 2C member 1
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P98194

Gene: ATP2C1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
14. Calcium-transporting ATPase type 2C member 2
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium (By similarity).
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: O75185

Gene: ATP2C2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
15. Gamma-aminobutyric acid receptor subunit alpha-1
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P14867

Gene: GABRA1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
16. Gamma-aminobutyric acid receptor subunit alpha-2
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P47869

Gene: GABRA2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
17. Gamma-aminobutyric acid receptor subunit alpha-3
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P34903

Gene: GABRA3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
18. Gamma-aminobutyric acid receptor subunit alpha-4
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P48169

Gene: GABRA4

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
19. Gamma-aminobutyric acid receptor subunit alpha-5
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P31644

Gene: GABRA5

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
20. Gamma-aminobutyric acid receptor subunit alpha-6
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: Q16445

Gene: GABRA6

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
21. Gamma-aminobutyric acid receptor subunit beta-1
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P18505

Gene: GABRB1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
22. Gamma-aminobutyric acid receptor subunit beta-2
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P47870

Gene: GABRB2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
23. Gamma-aminobutyric acid receptor subunit beta-3
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P28472

Gene: GABRB3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
24. Gamma-aminobutyric acid receptor subunit delta
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: O14764

Gene: GABRD

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
25. Gamma-aminobutyric acid receptor subunit epsilon
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P78334

Gene: GABRE

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
26. Gamma-aminobutyric acid receptor subunit gamma-1
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: Q8N1C3

Gene: GABRG1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
27. Gamma-aminobutyric acid receptor subunit gamma-2
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P18507

Gene: GABRG2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
28. Gamma-aminobutyric acid receptor subunit gamma-3
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: Q99928

Gene: GABRG3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
29. Gamma-aminobutyric acid receptor subunit pi
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: O00591

Gene: GABRP

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
30. Gamma-aminobutyric acid receptor subunit rho-1
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA receptor could play a role in retinal neurotransmission.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P24046

Gene: GABRR1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
31. Gamma-aminobutyric acid receptor subunit rho-2
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA receptor could play a role in retinal neurotransmission.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: P28476

Gene: GABRR2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
32. Gamma-aminobutyric acid receptor subunit rho-3
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel (By similarity).
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: A8MPY1

Gene: GABRR3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
33. Gamma-aminobutyric acid receptor subunit theta
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (R029)UniProt ID: Q9UN88

Gene: GABRQ

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
34. Plasma membrane calcium-transporting ATPase 1
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P20020

Gene: ATP2B1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
35. Plasma membrane calcium-transporting ATPase 2
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: Q01814

Gene: ATP2B2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
36. Plasma membrane calcium-transporting ATPase 3
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: Q16720

Gene: ATP2B3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
37. Plasma membrane calcium-transporting ATPase 4
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P23634

Gene: ATP2B4

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
38. Sarcoplasmic/endoplasmic reticulum calcium ATPase 1
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the translocation of calcium from the cytosol to the sarcoplasmic reticulum lumen. Contributes to calcium sequestration involved in muscular excitation/contraction.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: O14983

Gene: ATP2A1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
39. Sarcoplasmic/endoplasmic reticulum calcium ATPase 2
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the translocation of calcium from the cytosol to the sarcoplasmic reticulum lumen. Isoform 2 is involved in the regulation of the contraction/relaxation cycle.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P16615

Gene: ATP2A2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
40. Sarcoplasmic/endoplasmic reticulum calcium ATPase 3
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium. Transports calcium ions from the cytosol into the sarcoplasmic/endoplasmic reticulum lumen. Contributes to calcium sequestration involved in muscular excitation/contraction.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: Q93084

Gene: ATP2A3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
41. Sodium/potassium-transporting ATPase subunit gamma
May be involved in forming the receptor site for cardiac glycoside binding or may modulate the transport function of the sodium ATPase.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P54710

Gene: FXYD2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
42. Sodium/potassium-transporting ATPase subunit alpha-1
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P05023

Gene: ATP1A1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
43. Sodium/potassium-transporting ATPase subunit alpha-2
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium, providing the energy for active transport of various nutrients.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P50993

Gene: ATP1A2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
44. Sodium/potassium-transporting ATPase subunit alpha-3
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P13637

Gene: ATP1A3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
45. Sodium/potassium-transporting ATPase subunit alpha-4
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients. Plays a role in sperm motility.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: Q13733

Gene: ATP1A4

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
46. Sodium/potassium-transporting ATPase subunit beta-1
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The beta subunit regulates, through assembly of alpha/beta heterodimers, the number of sodium pumps transported to the plasma membrane.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P05026

Gene: ATP1B1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
47. Sodium/potassium-transporting ATPase subunit beta-2
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of the beta-2 subunit is not known.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P14415

Gene: ATP1B2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
48. Sodium/potassium-transporting ATPase subunit beta-3
This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of the beta-3 subunit is not known.
This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (R029)UniProt ID: P54709

Gene: ATP1B3

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- R029 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.
49. Estrogen receptor
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.
Causes endocrine disruption in humans by binding to and inhibiting the estrogen receptor. (S301)UniProt ID: P03372

Gene: ESR1

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- S301 — Luft S, Milki E, Glustrom E, Ampiah-Bonney R, O'Hara P. Binding of Organochloride and Pyrethroid Pesticides To Estrogen Receptors ? and ?: A Fluorescence Polarization Assay. Biophysical Journal 2009;96(3):444a.
50. Estrogen receptor beta
Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
Causes endocrine disruption in humans by binding to and inhibiting the estrogen receptor. (S301)UniProt ID: Q92731

Gene: ESR2

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report

References:
- S301 — Luft S, Milki E, Glustrom E, Ampiah-Bonney R, O'Hara P. Binding of Organochloride and Pyrethroid Pesticides To Estrogen Receptors ? and ?: A Fluorescence Polarization Assay. Biophysical Journal 2009;96(3):444a.