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Last update 08 May 2025

LTB4R2

Last update 08 May 2025

Basic Info

Synonyms

BLT2, BLT2R, BLTR2

+ [9]

Introduction

Low-affinity receptor for leukotrienes including leukotriene B4. Mediates chemotaxis of granulocytes and macrophages. The response is mediated via G-proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTB4 > 12-epi-LTB4 > LTB5 > LTB3.

Drugs associated with LTB4R2

T-10430

Target

LTB4R2

Mechanism

LTB4R2 agonists

Active Org.

Johann Wolfgang Goethe-Universität Frankfurt am Main

Originator Org.

Johann Wolfgang Goethe-Universität Frankfurt am Main

Active Indication

Psoriasis

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

PA-501

Target

LTB4R2

Mechanism

LTB4R2 inhibitors

Active Org.

Pharvis Korea Pharm Co., Ltd.

Originator Org.

Pharvis Korea Pharm Co., Ltd.

Active Indication

Severe asthma

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with LTB4R2

100 Translational Medicine associated with LTB4R2

0 Patents (Medical) associated with LTB4R2

222

Literatures (Medical) associated with LTB4R2

23 Jan 2025·Journal of Medicinal Chemistry

Identification of a Chemical Probe for BLT2 Activation by Scaffold Hopping

Article

Author: Kaps, Alexander ; Elewa, Mohammed A. F. ; Schmidtko, Achim ; Proschak, Ewgenij ; Elson, Lewis ; Ildefeld, Niklas ; Marinescu, Beatrice ; Müller, Susanne ; Schubert-Zsilavecz, Manfred ; Kaiser, Astrid ; Macinkovic, Igor ; Steinhilber, Dieter ; Weigert, Andreas ; Ehrler, Johanna H. M. ; Kallenborn-Gerhardt, Wiebke ; Heering, Jan ; Hernandez-Olmos, Victor ; Rajkumar, Rinusha ; Alnouri, Mohamad Wessam ; Offermanns, Stefan

The leukotriene B4 receptor 2 (BLT2) is a G-protein coupled receptor, which is endogenously activated by 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT). BLT2 is gaining attention as a potential therapeutic target involved in various pathologies including diabetic wound healing, ophthalmic diseases, and colitis. However, validation of BLT2 as drug target requires chemical probes and pharmacological tools which will allow for application in vivo. In this work, we present the discovery of a novel chemical probe T-10430 for BLT2 agonism following a scaffold-hopping approach. T-10430 exhibits high potency, good selectivity profile, promising physicochemical and PK properties and can potentially serve as orally applicable pharmacological tool for validation of BLT2 as drug target. Using T-10430, we demonstrate the beneficial effect of BLT2 activation in mouse model of psoriasis.

01 Jan 2025·Journal of Pediatric Surgery

Impact of Epithelial Claudin-4 and Leukotriene B4 Receptor 2 in Normoganglionic Hirschsprung Disease Colon on Post Pull-through Enterocolitis

Article

Author: Goto, Hiroki ; Ochi, Takanori ; Abe, Kumpei ; Fujimoto, Takashi ; Arii, Rumi ; Shibuya, Soichi ; Fujiwara, Kentaro ; Iida, Hisae ; Okazaki, Tadaharu ; Yamada, Shunsuke ; Lane, Geoffrey J ; Ishiyama, Asuka ; Yazaki, Yuta ; Lane, Geoffrey J. ; Ueda-Abe, Eri ; Takeda, Masahiro ; Shimizu, Masahiro ; Suda, Kazuto ; Koga, Hiroyuki ; Urao, Masahiko ; Yamataka, Atsuyuki ; Miyano, Go

PURPOSETo investigate whether Leukotriene B4 receptor 2 (BLT-2), an upstream regulator of tight junction protein (TJP) Claudin-4, and TJPs could be etiologic factors in Hirschsprung-associated enterocolitis (HAEC) after pull-through (PT) for Hirschsprung disease (HD).METHODSNormoganglionic colon (HD-N) and aganglionic rectum (HD-A) specimens from rectal/rectosigmoid (R/RS) or descending/transverse (D/T) HD were assessed using quantitative polymerase chain reaction (qPCR) for Occludin, TJP-1, TJP-2, Junctional adhesion molecule (JAM)-1, JAM-2, Claudin-1, Claudin-3, Claudin-4, and BLT-2 and immunoblotting for Claudin-4 using fresh specimens obtained intraoperatively (2021-2024; n = 17; R/RS = 15 and D/T = 2). Claudin-4 immunohistochemistry was also evaluated quantitatively using preserved (n = 29; R/RS = 20 and D/T = 9; 2009-2021) and fresh HD specimens for comparison with anorectal malformation patients having colostomy closure as controls (n = 42) and between HD-A versus HD-N, R/RS versus D/T, and HAEC (+) versus HAEC (-). Technically inadequate or transitional zone PT were excluded.RESULTSSubjects were 123 PT cases. Mean ages at PT/colostomy closure (years) were R/RS: 2.7 ± 2.9, D/T: 1.6 ± 2.2, and controls: 1.4 ± 0.7. Postoperative HAEC occurred 18 times in 14 PT cases (grade I = 5, grade II = 13). Post-PT HAEC was significantly more frequent in D/T (50.0% versus 6.4%; p < 0.001); Claudin-4 was significantly lower in HD-N from post-PT HAEC cases, especially D/T (p < 0.05) on immunohistochemistry. Claudin-4 was significantly lower in HD-N/HD-A compared with controls on immunoblotting (p < 0.05) and immunohistochemistry (p < 0.001). qPCR showed TJP-1, TJP-2, JAM-1, JAM-2, Claudin-4, and BLT-2 were significantly lower in HD-N/HD-A compared with controls.CONCLUSIONSLower Claudin-4 and BLT2 in post-PT HAEC HD-N (especially D/T) suggests generalized epithelial barrier derangement with possible etiologic implications for HAEC.LEVEL OF EVIDENCEⅡ.

01 Jan 2025·Current Therapeutic Research

Alpha-Lipoic Acid-Mediated Inhibition of LTB4 Synthesis Suppresses Epithelial-Mesenchymal Transition, Modulating Functional and Tumorigenic Capacities in Non-Small Cell Lung Cancer A549 Cells

Article

Author: Contreras, Héctor R ; Valle, Alexandra ; Castellón, Enrique A ; López-Moncada, Fernanda ; Gv, Kevin Brockway ; Ríos, Juan Carlos ; Faúndez, Mario ; Indo, Sebastián ; Torres, María José

BackgroundLeukotriene B₄ (LTB₄) plays a crucial role in carcinogenesis by inducing epithelial-mesenchymal transition (EMT), a process associated with tumor progression. The synthesis of LTB₄ is mediated by leukotriene A₄ hydrolase (LTA₄H), and it binds to the receptors BLT₁ and BLT₂. Dysregulation in LTB₄ production is linked to the development of various pathologies. Therefore, the identification or design of inhibitors of LTB₄ synthesis or receptor antagonists represents an ongoing challenge. In this context, our laboratory previously demonstrated that alpha-lipoic acid (ALA) inhibits LTA₄H. The objective of this study was to evaluate the effect of ALA on the expression of canonical EMT markers and the functional and tumorigenic capacities induced by LTB₄ in A549 cells.MethodsThe expression of cPLA₂, 5LOX, FLAP, LTA₄H, BLT1, and LTB₄ production in human adenocarcinomic alveolar basal epithelial A549 cells was assessed using Western blot, RT-qPCR, and ELISA, respectively. Subsequently, the expression of canonical EMT markers was evaluated by Western blot. Functional assays were performed to assess cell viability, proliferation, invasion, migration, and clonogenicity using MTT, Western blot, Transwell assays, and colony formation assays, respectively. Results were expressed as median with interquartile range (n≥3) and analyzed using the Kruskal-Wallis or Tukey multiple comparisons tests.ResultsA549 cells express key proteins involved in LTB₄ synthesis and receptor binding, including LTA₄H and BLT₁, and ALA inhibits the production of LTB₄. Additionally, LTA₄H and BLT1 were detected in lung adenocarcinoma tissue samples. LTB₄ was found to induce EMT, whereas ALA treatment enhanced the expression of epithelial markers and reduced the expression of mesenchymal markers. Furthermore, ALA treatment resulted in a decrease in LTB₄ levels and attenuated the functional and tumorigenic capacities of A549 cells, including their viability, migration, invasion, and clonogenic potential.ConclusionsThese findings suggest that ALA may offer therapeutic potential in the context of lung cancer, as it could be integrated into conventional pharmacological therapies to enhance treatment efficacy and mitigate the adverse effects associated with chemotherapy. Further studies are warranted to confirm the clinical applicability of ALA as an adjunctive treatment in lung cancer.

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LTB4R2

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