Target type: molecularfunction
Combining with a lipopolysaccharide and transmitting the signal across the cell membrane to initiate an innate immune response. Lipopolysaccharides (LPS) are major components of the outer membrane of Gram-negative bacteria, making them prime targets for recognition by the immune system. [PMID:14609719, PMID:15379975]
Lipopolysaccharide (LPS) immune receptor activity is a crucial component of the innate immune response, primarily mediated by Toll-like receptor 4 (TLR4). LPS, a major component of the outer membrane of Gram-negative bacteria, triggers a cascade of signaling events upon binding to TLR4. This interaction leads to the activation of downstream signaling pathways, such as the NF-κB pathway, ultimately resulting in the production of pro-inflammatory cytokines and the initiation of immune responses.
The molecular function of LPS immune receptor activity encompasses several key steps:
1. **LPS recognition:** TLR4, in conjunction with its co-receptors MD-2 and CD14, specifically recognizes and binds to LPS. The interaction between TLR4 and LPS is facilitated by the formation of a complex involving LPS, MD-2, and TLR4, enabling signal transduction.
2. **Signal transduction:** Upon LPS binding, TLR4 undergoes a conformational change, leading to the recruitment of adaptor proteins, such as MyD88 and TRIF, to the intracellular domain of TLR4. These adaptor proteins initiate distinct signaling cascades.
3. **Activation of downstream signaling pathways:** MyD88 activates the NF-κB pathway, while TRIF activates both the NF-κB pathway and the interferon regulatory factor 3 (IRF3) pathway. These pathways regulate the expression of various genes involved in immune responses.
4. **Cytokine production:** Activated NF-κB and IRF3 pathways stimulate the transcription and translation of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α), interleukin-1 (IL-1), and interleukin-6 (IL-6). These cytokines mediate various immune responses, including inflammation, fever, and leukocyte recruitment.
5. **Immune response activation:** The production of pro-inflammatory cytokines and the activation of immune cells, such as macrophages and neutrophils, contribute to the initiation and amplification of the innate immune response against bacterial infections.
The intricate molecular function of LPS immune receptor activity highlights the critical role of TLR4 in sensing microbial threats and initiating appropriate immune responses. This activity is essential for host defense against Gram-negative bacterial infections and plays a significant role in the development and regulation of both innate and adaptive immune responses.'
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Protein | Definition | Taxonomy |
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Lymphocyte antigen 96 | A lymphocyte antigen 96 that is encoded in the genome of human. [TLR:AMM, UniProtKB:Q9Y6Y9] | Homo sapiens (human) |
Scavenger receptor class B member 1 | A scavenger receptor class B member 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8WTV0] | Homo sapiens (human) |
Platelet-activating factor receptor | A mammalian-type platelet-activating factor receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25105] | Homo sapiens (human) |
Toll-like receptor 2 | A Toll-like receptor 2 that is encoded in the genome of human. [PRO:CNA] | Homo sapiens (human) |
Toll-like receptor 4 | A Toll-like receptor 4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:O00206] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
palmitic acid | hexadecanoic acid : A straight-chain, sixteen-carbon, saturated long-chain fatty acid. Palmitic Acid: A common saturated fatty acid found in fats and waxes including olive oil, palm oil, and body lipids. | long-chain fatty acid; straight-chain saturated fatty acid | algal metabolite; Daphnia magna metabolite; EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor; plant metabolite |
brotizolam | brotizolam: structure | organic molecular entity | |
carvedilol | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent | |
cilostamide | cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure | quinolines | |
clotrimazole | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic | |
dephostatin | dephostatin: from Streptomyces sp. MJ742-NF5; structure given in first source | ||
juglone | juglone : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogen at position 5 has been replaced by a hydroxy group. A plant-derived 1,4-naphthoquinone with confirmed antibacterial and antitumor activities. juglone: structure | hydroxy-1,4-naphthoquinone | geroprotector; herbicide; reactive oxygen species generator |
loratadine | loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness. | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
mesalamine | mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position. Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed) | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
etoposide phosphate | |||
nifedipine | Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
1,2,5,8-tetrahydroxy anthraquinone | 1,2,5,8-tetrahydroxy anthraquinone: structure in first source quinalizarin : A tetrahydroxyanthraquinone having the four hydroxy groups at the 1-, 2-, 5- and 8-positions. | tetrahydroxyanthraquinone | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor |
purpurin | purpurin : A trihydroxyanthraquinone derived from anthracene by substitution with oxo groups at C-9 and C-10 and with hydroxy groups at C-1, C-2 and C-4. purpurin: from Rubiaceae plants; structure in first source | trihydroxyanthraquinone | biological pigment; histological dye; plant metabolite |
suramin sodium | suramin sodium : An organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness. | organic sodium salt | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
lithocholic acid | lithocholate : A bile acid anion that is the conjugate base of lithocholic acid. lithocholic acid : A monohydroxy-5beta-cholanic acid with a alpha-hydroxy substituent at position 3. It is a bile acid obtained from chenodeoxycholic acid by bacterial action. Lithocholic Acid: A bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic. | bile acid; C24-steroid; monohydroxy-5beta-cholanic acid | geroprotector; human metabolite; mouse metabolite |
chrysophanic acid | chrysophanic acid: RN given refers to parent cpd; structure in Merck, 9th ed, #2260 chrysophanol : A trihydroxyanthraquinone that is chrysazin with a methyl substituent at C-3. It has been isolated from Aloe vera and exhibits antiviral and anti-inflammatory activity. | dihydroxyanthraquinone | anti-inflammatory agent; antiviral agent; plant metabolite |
myristic acid | Myristic Acid: A saturated 14-carbon fatty acid occurring in most animal and vegetable fats, particularly butterfat and coconut, palm, and nutmeg oils. It is used to synthesize flavor and as an ingredient in soaps and cosmetics. (From Dorland, 28th ed) tetradecanoate : A long-chain fatty acid anion that is the conjugate base of myristic acid; major species at pH 7.3. tetradecanoic acid : A straight-chain, fourteen-carbon, long-chain saturated fatty acid mostly found in milk fat. | long-chain fatty acid; straight-chain saturated fatty acid | algal metabolite; Daphnia magna metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; human metabolite |
ethidium bromide | organic bromide salt | geroprotector; intercalator; trypanocidal drug | |
daunorubicin | anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine. daunorubicin : A natural product found in Actinomadura roseola. Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS. | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
rimcazole | rimcazole: RN given refers to (cis)-isomer; structure given in first source | carbazoles | |
sch 37370 | N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine | ||
ro 24-4736 | Ro 24-4736: structure given in first source; platelet activating factor antagonist | ||
daunorubicin hydrochloride | anthracycline | ||
web 2086 | WEB 2086: structure given in first source; PAF antagonist | organonitrogen heterocyclic compound; organosulfur heterocyclic compound | |
pacein | orcein : A variable mixture of several compounds isolated from lichens, the eight most abundant being alpha-aminoorcein, alpha-hydroxyorcein, beta-aminoorcein, gamma-aminoorcein, beta-hydroxyorcein, gamma-hydroxyorcein, beta-aminoorceimine and beta-aminoorceimine (all are phenoxazine-based). It is used for the demonstration of elastic fibres as well as to stain the rough endoplasmic reticulum of hepatitis B infected liver cells. pacein : A member of the class of benzofurans that is dibenzo[b,d]furan-3,7-dione bearing two methyl substituents at positions 1 and 9 as well as two 2,4-dihydroxy-6-methylanilino substituents at positions 2 and 8. PAcein: structure | ||
cv 3988 | CV 3988: platelet activating factor antagonist; structure given in first source | ||
1-hexadecyl-2-acetyl-glycero-3-phosphocholine | 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis. Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION. | 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine | antihypertensive agent; beta-adrenergic antagonist; bronchoconstrictor agent; hematologic agent; vasodilator agent |
methotrexate | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent | |
mk 287 | MK 287: RN given refers to the trans-(-)-isomer L-680573; L-680574 is an optical enantiomer; L-668750 is the racemic mixture; structure given in first source | ||
rupatadine | rupatadine: structure given in first source; RN given refers to trihydrochloride | benzocycloheptapyridine | |
sdz 64-412 | SDZ 64-412: structure given in first source; PAF antagonist | ||
doxorubicin hydrochloride | anthracycline | ||
xanthohumol | xanthohumol : A member of the class of chalcones that is trans-chalcone substituted by hydroxy groups at positions 4, 2' and 4', a methoxy group at position 6' and a prenyl group at position 3'. Isolated from Humulus lupulus, it induces apoptosis in human malignant glioblastoma cells. xanthohumol: from hop plant, Humulus lupulus | aromatic ether; chalcones; polyphenol | anti-HIV-1 agent; antineoplastic agent; antiviral agent; apoptosis inducer; EC 2.3.1.20 (diacylglycerol O-acyltransferase) inhibitor; metabolite |
2-thiophenecarboxylic acid 2-(1,3-dioxo-2-isoindolyl)ethyl ester | phthalimides | ||
curcumin | curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa. Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes. | aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol | anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger |
suramin sodium | suramin(6-) : An organosulfate oxoanion that is the hexanion of suramin resulting from the deprotonation of the six sulfo groups; major species at pH 7.3. | organosulfate oxoanion | |
gw-5074 | |||
nf 449 | |||
ginkgolide b | |||
ro 24-0238 | Ro 24-0238: PAF antagonist | ||
l 652731 | |||
parthenolide | sesquiterpene lactone | drug allergen; inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug | |
lexipafant | lexipafant: an imidazolyl derivative which forms part of a fused heterocyclic system | ||
abt 299 | ABT 299: converted in vivo to A-85783.0; a platelet activating factor antagonist; structure in first source | ||
orvepitant | |||
resatorvid | |||
crx-526 | CRX-526: aminoalkyl-glucosaminide-phosphate; lipid A-mimetic with anti-inflammatory properties; structure in first source |