International Union of Basic and Clinical Pharmacology. LXXXIV: Leukotriene Receptor Nomenclature, Distribution, and Pathophysiological Functions

Identification of GPR99 Protein as a Potential Third Cysteinyl Leukotriene Receptor with a Preference for Leukotriene E4 Ligand

“…Furthermore, in limited studies, LTE 4 was comparable with LTC 4 or LTD 4 in eliciting a vascular leak in skin in guinea pigs (11) or humans (12), and inhalation of LTE 4 , but not LTD 4 , by patients with asthma elicited an accumulation of eosinophils and basophils into the bronchial mucosa (13,14). These observations strongly supported an agonist function for LTE 4 , likely mediated by a receptor separate from those that are activated by its short-lived precursors (15).…”

Leukotriene C4 induces migration of human monocyte–derived dendritic cells without loss of immunostimulatory function

“…This is conceivable, given that CysLTR 1 is the primary receptor for LTD 4 with a 50-times lower binding affinity for LTC 4 (dissociation constant 0.4nM versus 21nM), whereas LTC 4 and LTD 4 bind with similar affinity to CysLTR 2 (ϳ 10nM), as determined in recombinant systems. 40 In addition, in a recent study, LTC 4 was shown to exert antagonistic effects on immature and mature murine bone marrow-derived DCs. Although LTC 4 activated immature DCs, it demonstrated a CysLTR 1 -dependent inhibition of induction of Th-1 responses when added to LPS-matured DCs, which had up regulated Cys-LTR 1 , further highlighting the immunoinhibitory function of Cys-LTR 1 on DCs.…”

“…This result is conceivable given that BLT 1 is expressed on human monocyte-derived DCs. BLT 1 is the high-affinity receptor for LTB 4 40 and signaling through BLT 1 results in the induction of strong Th2 responses. 41 In contrast, LTC 4 and LTD 4 mediate their biologic effects through both CysLTR 1 and CysLTR 2 , but only maturation in the presence of LTD 4 resulted in a greatly diminished induction of CTL responses by DCs.…”

Role of leukotriene antagonists and antihistamines in treatment of allergic rhinitis and asthma comorbidity

“…[16] Antileukotrienes are classified in two groups; cysteinyl leukotriene receptor antagonists (LTRAs) -zafirlukast, pranlukast, and montelukast -block the leukotriene receptor and thus block the end organ response of leukotriene. [16] Zafirlukast is a leukotriene (LT) D4 receptor antagonist and is efficient in LTD4 induced bronchoconstriction, early and late responses, exercise challenge, cold induced asthma, and chronic asthma. Leukotriene synthesis inhibitors -zileuton -block the biosynthesis of cysteinyl leukotrienes.…”