Target type: molecularfunction
Combining with leukotriene B4, LTB4, to initiate a change in cell activity. Leukotriene B4 is also known as (6Z, 8E, 10E, 14Z)-(5S, 12R)-5,12-dihydroxyicosa-6,8,10,14-tetraen-1-oate. [GOC:ai, ISBN:0198506732]
Leukotriene B4 (LTB4) receptor activity refers to the ability of a receptor protein to bind and respond to the signaling molecule LTB4. LTB4 is a potent lipid mediator produced by various cell types, primarily neutrophils and macrophages, in response to inflammation and immune stimuli. It plays a crucial role in the inflammatory response by initiating a cascade of events leading to leukocyte recruitment, adhesion, chemotaxis, and activation.
LTB4 receptor activity is mediated by the G protein-coupled receptor BLT1 (also known as LTB4R1), which is expressed on a variety of cells, including leukocytes, endothelial cells, and smooth muscle cells. Upon LTB4 binding to BLT1, the receptor undergoes conformational changes that activate associated G proteins, primarily of the Gαi and Gαq subtypes.
Activation of Gαi proteins leads to inhibition of adenylyl cyclase, resulting in decreased production of cAMP and suppression of cAMP-dependent signaling pathways. Conversely, activation of Gαq proteins triggers the phospholipase C (PLC) pathway, leading to the generation of inositol trisphosphate (IP3) and diacylglycerol (DAG). IP3 mobilizes intracellular calcium stores, while DAG activates protein kinase C (PKC).
The downstream signaling events mediated by LTB4 receptor activity culminate in a variety of cellular responses, including:
- **Leukocyte chemotaxis:** LTB4 receptor activation promotes directed migration of leukocytes towards the site of inflammation.
- **Leukocyte adhesion:** LTB4 receptor signaling enhances leukocyte adhesion to endothelial cells, facilitating their extravasation into inflamed tissues.
- **Leukocyte activation:** LTB4 receptor stimulation triggers the release of inflammatory mediators, such as reactive oxygen species (ROS) and cytokines, further amplifying the inflammatory response.
- **Smooth muscle contraction:** In certain tissues, LTB4 receptor activation can induce smooth muscle contraction, contributing to bronchoconstriction and vasoconstriction.
The precise cellular responses elicited by LTB4 receptor activity vary depending on the cell type and the specific downstream signaling pathways activated.
Overall, LTB4 receptor activity represents a critical component of the inflammatory response, playing a central role in leukocyte recruitment and activation. Dysregulation of LTB4 receptor signaling has been implicated in various inflammatory diseases, including asthma, rheumatoid arthritis, and inflammatory bowel disease. Therefore, targeting LTB4 receptor activity holds potential as a therapeutic strategy for the treatment of these conditions.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Leukotriene B4 receptor 1 | A leukotriene B4 receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15722] | Homo sapiens (human) |
| Leukotriene B4 receptor 2 | A leukotriene B4 receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9NPC1] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| candesartan | candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. candesartan: a nonpeptide angiotensin II receptor antagonist | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| avapro | irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease. | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| 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 |
| masoprocol | nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata) | catechols; lignan; tetrol | antioxidant; ferroptosis inhibitor; geroprotector; plant metabolite |
| gentian violet | crystal violet : An organic chloride salt that is the monochloride salt of crystal violet cation. It has been used in creams for the topical treatment of bacterial and fungal infections, being effective against some Gram-positive bacteria (notably Staphylococcus species) and some pathogenic fungi (including Candida species) but use declined following reports of animal carcinogenicity. It has also been used for dying wood, silk, and paper, as well as a histological stain. Gentian Violet: A dye that is a mixture of violet rosanilinis with antibacterial, antifungal, and anthelmintic properties. | organic chloride salt | anthelminthic drug; antibacterial agent; antifungal agent; antiseptic drug; histological dye |
| bw-755c | 4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine: A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia. | ||
| tepoxalin | tepoxalin : A hydroxamic acid obtained by formal condensation of the carboxy group of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]propanoic acid with the amino group of N-methylhydroxylamine. It is used in veterinary medicine for the control of pain and inflammation caused by musculoskeletal disorders such as hip dysplasia and arthritis in dogs. | aromatic ether; hydroxamic acid; monochlorobenzenes; pyrazoles | antipyretic; apoptosis inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; immunomodulator; lipoxygenase inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| zileuton | 1-benzothiophenes; ureas | anti-asthmatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor; leukotriene antagonist; non-steroidal anti-inflammatory drug | |
| valsartan | valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION. | biphenylyltetrazole; monocarboxylic acid; monocarboxylic acid amide | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| ubenimex | ubenimex: growth inhibitor | ||
| 1-(10h-phenothiazin-2-yl)ethanone | 1-(10H-phenothiazin-2-yl)ethanone: structure in first source | phenothiazines | |
| sc 41930 | SC 41930: leukotriene B4 receptor antagonist; structure in first source | ||
| ly 255283 | LY 255283: structure given in UD; leukotriene B4 antagonist | aromatic ketone | |
| rg 14893 | RG 14893: structure in first source; leukotriene B4 receptor antagonist | ||
| pyrrolidino-benzylphenoxyethanamine | |||
| ly 293111 | LY 293111: a leukotriene B4 receptor antagonist; structure given in first source | aromatic ether | |
| 7-(3-(2-(cyclopropylmethyl)-3-methoxy-4-((methylamino)carbonyl)phenoxy)propoxy)-3,4-dihydro-8-propyl-2h-1-benzopyran-2-propanoic acid | 7-(3-(2-(cyclopropylmethyl)-3-methoxy-4-((methylamino)carbonyl)phenoxy)propoxy)-3,4-dihydro-8-propyl-2H-1-benzopyran-2-propanoic acid: structure in first source; inhibits leukotriene B4 receptors | ||
| amastatin | amastatin : A tetrapeptide comprising (2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl, L-valyl, L-valyl and L-aspartic acid units joined in sequence amastatin: structure; inhibits aminopeptidase | tetrapeptide | EC 3.4.11.* (aminopeptidase) inhibitor; protease inhibitor |
| e 3040 | E 3040: a dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase; structure given in first source | benzothiazoles; organic hydroxy compound; pyridines; secondary amino compound | anti-inflammatory drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; uricosuric drug |
| cocaine | cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. | benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid | adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| spiro[1,3-dihydroperimidine-2,1'-cycloheptane] | naphthalenes | ||
| 5-(2-furanyl)-N-[1-[(2-methylphenyl)methyl]-3-pyrazolyl]-7-(trifluoromethyl)-3-pyrazolo[1,5-a]pyrimidinecarboxamide | pyrazolopyrimidine | ||
| 1-methyl-N-[4-(4-morpholinyl)phenyl]-2-quinolinimine | morpholines | ||
| gl-4 | |||
| leukotriene b4 | leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway. Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990) | dihydroxy monocarboxylic acid; hydroxy polyunsaturated fatty acid; leukotriene; long-chain fatty acid | human metabolite; mouse metabolite; plant metabolite; vasoconstrictor agent |
| sb 201993 | (E)-3-((((6-(2-carboxyethenyl)-5-((8-(4-methoxyphenyl)octyl)oxy)-2-pyridinyl)methyl)thio)methyl)benzoic acid: structure given in first source; a competitive LTB(4) receptor antagonist | ||
| ono 4057 | ONO-LB 457: LTB4 receptor antagonist; structure given in first source | ||
| ticolubant | Ticolubant: a leukotriene B4 antagonist | ||
| ly 223982 | LY 223982: RN & structure in first source; leukotriene B4 antagonist | ||
| cp 195543 | CP 195543: a potent & selective leukotriene B4 antagonist; structure in first source | ||
| cp 105696 | CP 105696: a leukotriene B4 receptor antagonist; structure in first source | ||
| leucettamine b | leucettamine B: a protein kinase inhibitor isolated from the marine sponge Leucetta microraphis; structure in first source | ||
| ubenimex | peptide | ||
| pf-04418948 | 1-(4-fluorobenzoyl)-3-(((6-methoxy-2-naphthyl)oxy)methyl)azetidine-3-carboxylic acid: structure in first source |