ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas
Summary Interleukin (IL)-2-inducible T cell kinase (ITK) is essential for T cell receptor (TCR)
signaling and plays an integral role in T cell proliferation and differentiation. Unlike the ITK …
signaling and plays an integral role in T cell proliferation and differentiation. Unlike the ITK …
Discovery of 7H-pyrrolo [2, 3-d] pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk)
G Tang, L Liu, X Wang, Z Pan - European Journal of Medicinal Chemistry, 2019 - Elsevier
Abstract Interleukin-2-inducible T-cell kinase (Itk) plays an important role in multiple signal
transduction pathways in T and mast cells, and is a potential drug target for treating …
transduction pathways in T and mast cells, and is a potential drug target for treating …
Design, synthesis and structure–activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK)
X Wang, G Xue, Z Pan - European Journal of Medicinal Chemistry, 2020 - Elsevier
Interleukin-2 inducible T-cell kinase (ITK), a member of the Tec family of tyrosine kinases,
plays an important role in T cell signaling downstream of the T-cell receptor (TCR). Herein …
plays an important role in T cell signaling downstream of the T-cell receptor (TCR). Herein …
Kinome profiling analysis identified Src pathway as a novel therapeutic target in combination with histone deacetylase inhibitors for cutaneous T-cell lymphoma
N Jimura, K Fujii, Z Qiao, R Tsuchiya… - Journal of …, 2021 - Elsevier
Abstract Background Histone deacetylase inhibitors (HDACi) are used to treat patients with
cutaneous T-cell lymphoma (CTCL), but they show limited efficacy. Hence, combination …
cutaneous T-cell lymphoma (CTCL), but they show limited efficacy. Hence, combination …
Degrading the signal amplifier: ITK as a target for targeted protein degradation
A August - Cell Chemical Biology, 2023 - Elsevier
In this issue of Cell Chemical Biology, Jiang and colleagues show for the first time that the
Tec kinase ITK can be targeted using PROTAC approaches. This new modality has …
Tec kinase ITK can be targeted using PROTAC approaches. This new modality has …
The retinoid derivant ECPIRM selectively exhibited anti-proliferation effects in cutaneous T-Cell lymphoma via ITK-mediated signaling pathway
H Li, C Wang, P Ma, M Zhang, H Yang, S Yuan… - Journal of …, 2020 - Elsevier
Abstract Background The treatment of Cutaneous T-cell lymphoma (CTCL) met huge
challenges because of the heterogeneity and the scarcity of targeted drugs. ECPIRM …
challenges because of the heterogeneity and the scarcity of targeted drugs. ECPIRM …
キノーム解析によるHDAC 阻害剤併用療法の新規標的候補分子プロゲステロン受容体の同定
藤井一恭， 野口玲， 吉松有紀， 近藤格， 金蔵拓郎 - 電気泳動, 2023 - jstage.jst.go.jp
抄録 ヒストン脱アセチル化酵素 (HDAC) 阻害剤は皮膚 T 細胞リンパ腫の有効な治療法であるが,
単剤では獲得耐性が必発であり, 適切な併用療法の開発が求められている. 我々は皮膚 T …
単剤では獲得耐性が必発であり, 適切な併用療法の開発が求められている. 我々は皮膚 T …