bms-911543 and Dermatitis--Atopic

bms-911543 has been researched along with Dermatitis--Atopic* in 1 studies

Other Studies

1 other study(ies) available for bms-911543 and Dermatitis--Atopic

Article	Year
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling. Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12 Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor complex, JAK inhibition may offer an alternate small molecule approach to disrupting IL-13 signaling. Herein we demonstrate that JAK1 is likely the isoform most important to IL-13 signaling. Structure-based design was then used to improve the JAK1 potency of a series of previously reported JAK2 inhibitors. The ability to impede IL-13 signaling was thereby significantly improved, with the best compounds exhibiting single digit nM IC Topics: Dermatitis, Atopic; Humans; Interleukin-13; Janus Kinase 1; Janus Kinase 2; Signal Transduction	2019

Article

Year

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12

Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor complex, JAK inhibition may offer an alternate small molecule approach to disrupting IL-13 signaling. Herein we demonstrate that JAK1 is likely the isoform most important to IL-13 signaling. Structure-based design was then used to improve the JAK1 potency of a series of previously reported JAK2 inhibitors. The ability to impede IL-13 signaling was thereby significantly improved, with the best compounds exhibiting single digit nM IC

Topics: Dermatitis, Atopic; Humans; Interleukin-13; Janus Kinase 1; Janus Kinase 2; Signal Transduction

2019