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. 2023 Jul 12;24(14):11380. doi: 10.3390/ijms241411380

Figure 3.

Figure 3

(a) Activation of the adaptive immune system via various receptors, different interleukins and its receptors, and the Janus kinases (JAK) STAT pathway. JAK1, Janus kinase 1; JAK2, Janus kinase 2; JAK3, Janus kinase 3; TYK2, Tyrosine kinase 2; STAT1, Signal transducer and activator of transcription 1; STAT3, Signal transducer and activator of transcription 3; STAT4, Signal transducer and activator of transcription 4; STAT5, Signal transducer and activator of transcription 5; STAT6, Signal transducer and activator of transcription 6; SYK, Spleen tyrosine kinase; BTK, Bruton’s tyrosine kinase; AHR, Aryl-hydrocarbon receptor; TRPA1, Transient receptor cation ankyrin 1; CB1R, Cannabinoid type 1 receptor; CB2R, Cannabinoid type 2 receptor; LXR, Liver X receptor; STAT, Signal transducer and activator of transcription; PDE4, Phosphodiesterase-4; PAR2, Protease-activated receptor 2; H4R, Histamine 4 receptor; S1PR, Sphingosine-1-phosphate receptor. This figure was created with Biorender at www.biorender.com. (b) Mechanism of action of different drugs acting on the adaptive immune system via various receptors, different interleukins and its receptors, and the Janus kinases (JAK) STAT pathway. Dupilumab is a fully humanized monoclonal antibody targeting IL4Rα receptor. CBP201 is a human IgG4 monoclonal antibody that binds to IL-4Rα receptor. AK120 is an antibody against IL4Rα receptor. Tralokinumab and cendakimab, a fully humanized IgG4λ, bind to IL-13 at an epitope that overlaps with the binding site of receptors IL13Rαl subunit and IL13Rα2 subunit. Tezepelumab is an anti-TSLP antibody. Lebrikizumab, a humanized monoclonal IgG4 antibody that selectively blocks IL13 and prevents heterodimerization of type II IL4R receptor composed of IL4Rα and IL13Rαl subunit. Eblasakimab is a fully humanized monoclonal antibody that targets the IL-13Rα1 subunit, therefore inhibiting the signals by IL4 and IL-13. Mepolizumab, a humanized immunoglobulin G monoclonal antibody, binds to interleukin-5, inhibiting its activity. Benralizumab directly binds to the IL-5Rα chain to inhibit the signaling pathway. Nemolizumab, a humanized monoclonal antibody that antagonizes IL-31RA receptor. Vixarelimab, a first-in-class fully human monoclonal antibody that targets oncostatin M receptor. Fezakinumab is an anti-IL-22 monoclonal antibody. Ruxolitinib, baricitinib, and ivarmacitinib inhibit JAK1 and JAK2. Tofacitinib is an inhibitor of JAK1, JAK2, and JAK3. Delgocitinib and jaktinib are pan-jak inhibitors inhibiting JAK1, JAK2, JAK3, and TYK2. Brepocitinib is a selective JAK-1 and TYK-2 inhibitor. Ifidacitinib selectively targets JAK1 and JAK3. Upadacitinib, abrocotinib, and ivarmacitinib are JAK inhibitors with a higher potency for JAK-1. Gusacitinib is a dual JAK-SYK inhibitor. PRN473 is a covalent BTK inhibitor. Branebrutinib is a highly selective BTK inhibitor that covalently binds to the cysteine residue of BTK. Tapinarof is an AHR agonist. HC-030031 and GRC17536 are both TRPA1 antagonists. S-777469 is a CB2R agonist. VTP-38543 and ALX-101 are LXR-β agonists. Crisaborole, PF-07038124, Hemay-808, difamilast, and roflumilast are PDE4 inhibitors in topical forms, while apremilast and orismilast are PDE4 inhibitors in oral form. Methylbenzyl methylbenzimidazole piperidinyl methanone (MMP) is a selective PAR-2 inhibitor in topical form. JNJ 39758979, adriforant, and LEO 152020 are H4R antagonists. KRO-105714 is a dual antagonist of sphingosylphosphorylcholine and sphingosine-1-phosphate receptor 1 in topical form. JTE-013 is an S1PR2 antagonist in topical form. Etrasimod, LC51-0255, and udifitimod are oral S1PR modulators. SCD-044 is an S1PR1 agonist. JAK1, Janus kinase 1; JAK2, Janus kinase 2; JAK3, Janus kinase 3; TYK2, Tyrosine kinase 2; STAT1, Signal transducer and activator of transcription 1; STAT3, Signal transducer and activator of transcription 3; STAT4, Signal transducer and activator of transcription 4; STAT5, Signal transducer and activator of transcription 5; STAT6, Signal transducer and activator of transcription 6; SYK, Spleen tyrosine kinase; BTK, Bruton’s tyrosine kinase; AHR, Aryl-hydrocarbon receptor; TRPA1, Transient receptor cation ankyrin 1; CB1R, Cannabinoid type 1 receptor; CB2R, Cannabinoid type 2 receptor; LXR, Liver X receptor; STAT, Signal transducer and activator of transcription; PDE4, Phosphodiesterase-4; PAR2, Protease-activated receptor 2; H4R, Histamine 4 receptor; S1PR, Sphingosine-1-phosphate receptor. This figure was created with Biorender at www.biorender.com.