The application of PROTACs in immune-inflammation diseases
C Zhang, X Sun, P Song, Y Rao - Bioorganic & Medicinal Chemistry, 2024 - Elsevier
Immune-inflammatory diseases are a class of conditions with high prevalence that severely
impact the quality of life. Current treatment strategies include immunosuppressants …
impact the quality of life. Current treatment strategies include immunosuppressants …
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: A critical review
S Nagula, MS Galla, N Sharma, P Mishra - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
In account to the mounting evidences in the literature, pro-inflammatory mediators/targets
activate multiple signalling pathways to trigger the illness ultimately responsible for acute …
activate multiple signalling pathways to trigger the illness ultimately responsible for acute …
Comprehensive analysis of single cell and bulk RNA sequencing reveals the heterogeneity of melanoma tumor microenvironment and predicts the response of …
Y Zhang, C Zhang, J He, G Lai, W Li, H Zeng… - Inflammation …, 2024 - Springer
Background Tumor microenvironment (TME) heterogeneity is an important factor affecting
the treatment response of immune checkpoint inhibitors (ICI). However, the TME …
the treatment response of immune checkpoint inhibitors (ICI). However, the TME …
Discovery of a potent Gilteritinib-based FLT3-PROTAC degrader for the treatment of Acute myeloid leukemia
L Ye, Z Cui, Y Sun, H Zhou, Q Rong, D Wang, J Jin… - Bioorganic …, 2024 - Elsevier
Fms-like tyrosine receptor kinase 3 (FLT3) proteolysis targeting chimeras (PROTACs)
emerge as a promising approach to overcome the limitations of FLT3 inhibitors, while the …
emerge as a promising approach to overcome the limitations of FLT3 inhibitors, while the …
Selective inhibition of interleukin-2 inducible T cell kinase (ITK) enhances anti-tumor immunity in association with Th1-skewing, cytotoxic T cell activation, and reduced …
LY Hsu, JT Rosenbaum, E Verner, WB Jones, CM Hill… - bioRxiv, 2023 - biorxiv.org
ABSTRACT ITK is a tyrosine kinase expressed predominantly by T lymphocytes. In mice,
selective knock-out of the ITK gene produces Th1 skewing of T helper cell differentiation. We …
selective knock-out of the ITK gene produces Th1 skewing of T helper cell differentiation. We …
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 …
Covalent Targeting of Splicing in T Cells
Despite significant interest in therapeutic targeting of splicing, few chemical probes are
available for the proteins involved in splicing. Here, we show that elaborated stereoisomeric …
available for the proteins involved in splicing. Here, we show that elaborated stereoisomeric …
Discovery of a Potent and Orally Bioavailable Flt3-Protac Degrader for the Treatment of Acute Myeloid Leukemia
L Ye, Z Cui, Y Sun, H Zhou, Q Rong, D Wang… - Available at SSRN … - papers.ssrn.com
Fms-like tyrosine receptor kinase 3 (FLT3) proteolysis targeting chimeras (PROTACs)
emerge as a promising approach to overcome the limitations of FLT3 inhibitors, while the …
emerge as a promising approach to overcome the limitations of FLT3 inhibitors, while the …