Leukotriene receptor

Protein family

The leukotriene (LT) receptors are G protein-coupled receptors that bind and are activated by the leukotrienes. They include the following proteins:

Leukotriene B4 receptors (BLTRs) – bind to and are activated by LTB4:
- BLT₁ (Leukotriene B₄ receptor 1) – LTB4R
- BLT₂ (Leukotriene B₄ receptor 2) – LTB4R2
Cysteinyl leukotriene receptors (CysLTRs) – bind to and are activated by LTC4, LTD4, and LTE4:
- CysLT₁ (Cysteinyl leukotriene receptor 1) – CYSLTR1
- CysLT₂ (Cysteinyl leukotriene receptor 2) – CYSLTR2

The recently elucidated CysLT_E, represented by GPR99/OXGR1, may constitute a third CysLTR.^[1]

References

^ Kanaoka Y, Maekawa A, Austen KF (2013). "Identification of GPR99 protein as a potential third cysteinyl leukotriene receptor with a preference for leukotriene E4 ligand". J. Biol. Chem. 288 (16): 10967–72. doi:10.1074/jbc.C113.453704. PMC 3630866. PMID 23504326.

External links

IUPHAR GPCR Database – Leukotriene receptors
Leukotriene+Receptors at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

Membrane proteins, receptors: cell surface receptors

G protein–coupled receptor

Class A	Eicosanoid receptor (Prostaglandin receptor) Protease-activated receptor Neurotransmitter receptor Purinergic receptor Biogenic amine receptor Olfactory receptor
Class B	Secretin receptor
Class C	Metabotropic glutamate receptor
Class D	Pheromone receptor
Class E	cAMP receptor
Class F	Frizzled/smoothened

Ligand-gated ion channel

Purinergic receptor

Enzyme-linked receptor

Other/ungrouped

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2), EP (1 2 3 4), FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin & Zeta, but not Sigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	Calcium-sensing receptor GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled & Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

Leukotriene signaling modulators

Receptor
(ligands)

BLTTooltip Leukotriene B4 receptor

BLT₁Tooltip Leukotriene B4 receptor 1	Agonists: 12-HETE 20-Hydroxy-LTB₄ Leukotriene B₄ LY-255283 Antagonists: 20-Carboxy-LTB₄ Amelubant CGS-23131 (LY-223982) CGS-25019C CP-105696 CP-195543 Etalocib LY-293111 Moxilubant ONO-4057 RG-14893 RP-69698 SB-209247 SC-53228 Ticolubant U-75302 ZK-158252
BLT₂Tooltip Leukotriene B4 receptor 2	Agonists: 12-HETE 12-HHT 12-HpETE 15-HETE 15-HpETE 20-Hydroxy-LTB₄ Leukotriene B₄ Antagonists: CP-195543 LY-255283 ZK-158252

CysLTTooltip Cysteinyl leukotriene receptor

CysLT₁Tooltip Cysteinyl leukotriene receptor 1	Agonists: Leukotriene C₄ Leukotriene D₄ Leukotriene E₄ Antagonists: Ablukast BAYu9773 BAYu9916 BAYx7195 Cinalukast FPL-55712 ICI-198615 Iralukast LY-170680 Masilukast MK-571 Montelukast ONO-1078 Pobilukast Pranlukast Ritolukast SKF-104353 SR-2640 Sulukast Tipelukast Tomelukast Verlukast Zafirlukast ZD-3523
CysLT₂Tooltip Cysteinyl leukotriene receptor 2	Agonists: Leukotriene C₄ Leukotriene D₄ Leukotriene E₄ Antagonists: BAYu9773 BAYu9916
CysLT_ETooltip Cysteinyl leukotriene receptor E	Agonists: Leukotriene E₄

Enzyme
(inhibitors)

5-LOXTooltip Arachidonate 5-lipoxygenase	2-TEDC Baicalein BW-A4C BW-B70C Caffeic acid CDC CJ-13610 Curcumin Fenleuton Hyperforin Hypericum perforatum (St. John's Wort) Meclofenamic acid (meclofenamate) Minocycline N-Stearoyldopamine Timegadine Zileuton FLAPTooltip Arachidonate 5-lipoxygenase-activating protein inhibitors: AM-103 AM-679 BAYx1005 MK-591 MK-886
12-LOXTooltip Arachidonate 12-lipoxygenase	2-TEDC 3-Methoxytropolone Baicalein CDC
15-LOXTooltip Arachidonate 15-lipoxygenase	2-TEDC CDC Luteolin PD-146176
LTA₄HTooltip Leukotriene A4 hydrolase	Acebilustat Captopril DG-051 Fosinoprilat JNJ-26993135 SA-6541 SC-57461A Ubenimex (bestatin)
LTB₄HTooltip Leukotriene B4 ω-hydroxylase	17-Octadecynoic acid
LTC₄STooltip Leukotriene C4 synthase	Azelastine MK-886
LTC₄HTooltip Leukotriene C4 hydrolase	Acivicin Serine-borate complex
LTD₄Tooltip Leukotriene D4 hydrolase	Cilastatin Ubenimex (bestatin)