Development of JAK inhibitors for the treatment of immune-mediated diseases: kinase-targeted inhibitors and pseudokinase-targeted inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Archives of pharmacal research"
DOI: 10.1007/s12272-020-01282-7
Abstract: JAKs are a family of intracellular tyrosine kinases consisting of four members, JAK1, JAK2, JAK3, and TYK2. They are key components of the JAK-STAT pathway that transmit signals of many cytokines involved in the pathogenesis… read more here.
Keywords: jak; mediated diseases; immune mediated; pseudokinase ... See more keywords
Glutamylation of Bacterial Ubiquitin Ligases by a Legionella Pseudokinase.
Sign Up to like & getrecommendations! Published in 2019 at "Trends in microbiology"
DOI: 10.1016/j.tim.2019.09.001
Abstract: Legionella pneumophila encodes a family of phosphoribosyl ubiquitination ligases (SidE) essential for the bacterium to establish successful infection. Four independent studies now show that the SidE family of ubiquitin ligases are regulated by a novel… read more here.
Keywords: ligases legionella; bacterial ubiquitin; ubiquitin ligases; glutamylation bacterial ... See more keywords
Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00845
Abstract: CASK (Ca2+/calmodulin-dependent Ser/Thr kinase) is a member of the MAGUK (membrane-associated guanylate kinase) family that functions as neurexin kinases with roles implicated in neuronal synapses and trafficking. The lack of a canonical DFG motif, which… read more here.
Keywords: ca2 calmodulin; calmodulin dependent; kinase; pseudokinase ... See more keywords
PK1 from Drosophila obscurin is an inactive pseudokinase with scaffolding properties
Sign Up to like & getrecommendations! Published in 2023 at "Open Biology"
DOI: 10.1098/rsob.220350
Abstract: Obscurins are large filamentous proteins with crucial roles in the assembly, stability and regulation of muscle. Characteristic of these proteins is a tandem of two C-terminal kinase domains, PK1 and PK2, that are separated by… read more here.
Keywords: obscurin inactive; drosophila obscurin; pk1 drosophila; pseudokinase scaffolding ... See more keywords
Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells
Sign Up to like & getrecommendations! Published in 2018 at "Science Signaling"
DOI: 10.1126/scisignal.aat7951
Abstract: Covalent EGFR family inhibitors bind to and induce the degradation of the pseudokinase TRIB2 to kill cancer cells. Targeting pseudokinases with kinase inhibitors Pseudokinases are structurally similar to kinases but lack catalytic activity; instead, pseudokinases… read more here.
Keywords: degradation; family; cancer cells; cancer ... See more keywords
Distinct PEAK3 interactors and outputs expand the signaling potential of the PEAK pseudokinase family
Sign Up to like & getrecommendations! Published in 2022 at "Science Signaling"
DOI: 10.1126/scisignal.abj3554
Abstract: The pseudokinase scaffolds PEAK1 and PEAK2 are implicated in cancer cell migration and metastasis. We characterized the regulation and role of the third family member PEAK3 in cell signaling. Similar to PEAK1 and PEAK2, PEAK3… read more here.
Keywords: peak3; pseudokinase; peak1 peak2; cell ... See more keywords
Back From the Dead: The Atypical Kinase Activity of a Pseudokinase Regulator of Cation Fluxes During Inducible Immunity
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Plant Science"
DOI: 10.3389/fpls.2022.931324
Abstract: While most pseudokinases lack phosphotransfer activity due to altered catalytic residues within their kinase domain, a subset of pseudokinases maintain kinase activity through atypical mechanisms. The Arabidopsis ILK1 is a pseudokinase from the Raf-like MAP3K… read more here.
Keywords: kinase activity; activity; pseudokinase; ilk1 ... See more keywords
Oncogenic Signalling of PEAK2 Pseudokinase in Colon Cancer
Sign Up to like & getrecommendations! Published in 2022 at "Cancers"
DOI: 10.3390/cancers14122981
Abstract: Simple Summary Catalytically inactive kinases, also named pseudokinases, play important roles in the regulation of cell growth and adhesion. While frequently deregulated in human cancer, their role in tumour development is partially elucidated. Here, we… read more here.
Keywords: cell growth; crc; colorectal cancer; pseudokinase ... See more keywords
JAK1 Pseudokinase V666G Mutant Dominantly Impairs JAK3 Phosphorylation and IL-2 Signaling
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24076805
Abstract: Overactive Janus kinases (JAKs) are known to drive leukemia, making them well-suited targets for treatment. We sought to identify new JAK-activating mutations and instead found a JAK1-inactivating pseudokinase mutation, V666G. In contrast to other pseudokinase… read more here.
Keywords: jak kinases; jak1 pseudokinase; v666g; pseudokinase ... See more keywords