There's more to death than life: Noncatalytic functions in kinase and pseudokinase signaling.
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TLDR
A review of the non-catalytic functions of protein kinases can be found in this paper, where the authors consider pseudokinases, proteins that are devoid of enzymatic activity altogether and demonstrate that, beyond conventional notions of kinase function, catalytic activity can be dispensable for biological function.About:
This article is published in Journal of Biological Chemistry.The article was published on 2021-01-01 and is currently open access. It has received 40 citations till now. The article focuses on the topics: Kinase activity & Protein kinase A.read more
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Journal ArticleDOI
Targeting the Non-Catalytic Functions: a New Paradigm for Kinase Drug Discovery?
TL;DR: The characterized noncatalytic functions of kinases are summarized, and the recent progress on developing small-molecule modulators of the noncatalyst functions of Kinase catalytic functions are highlighted.
Journal ArticleDOI
Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.
TL;DR: In this paper , the authors summarize and analyze recent progress in blocking non-enzymatic functions of target proteins by PROTAC-mediated degradation, highlighting representative case studies and discussing the pharmacological features originating from inhibition of the non enzymatic function.
Journal ArticleDOI
Chemical Probes for Understudied Kinases: Challenges and Opportunities.
Ricardo A. M. Serafim,Jonathan M. Elkins,William J. Zuercher,Stefan Laufer,Matthias Gehringer +4 more
TL;DR: In this paper, the authors highlight recent case studies illustrating the development of high-quality chemical probes for less-studied kinases and their application in target validation and discuss the associated challenges and opportunities.
Journal ArticleDOI
Looking lively: emerging principles of pseudokinase signaling.
Joshua B. Sheetz,Mark A. Lemmon +1 more
TL;DR: In this paper , the authors discuss recent structural data on conformational transitions and nucleotide binding by pseudokinases and discuss how biasing this conformational toggle may provide opportunities to target pseudokinase pharmacologically in disease.
Journal ArticleDOI
Structure vs. Function of TRIB1—Myeloid Neoplasms and Beyond
TL;DR: The TRIB1 family of proteins as discussed by the authors plays important roles in differentiation, development, and oncogenesis, and is known to be accessible to small-molecule inhibitors in spite of its inability to bind ATP.
References
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Journal ArticleDOI
Structural and functional diversity of the microbial kinome.
TL;DR: This huge phylogenetic and functional space is explored to cast light on the ancient evolution of this superfamily of enzymes built on a common protein kinase–like (PKL) fold and serves as a model for further structural and functional analysis of enzyme evolution.
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A robust methodology to subclassify pseudokinases based on their nucleotide-binding properties.
James M. Murphy,James M. Murphy,Qingwei Zhang,Samuel N. Young,Michael L. Reese,Fiona P. Bailey,Patrick A. Eyers,Daniela Ungureanu,Henrik Hammaren,Olli Silvennoinen,Leila N. Varghese,Leila N. Varghese,Kelan Chen,Kelan Chen,Anne Tripaydonis,Natalia Jura,Koichi Fukuda,Jun Qin,Zachary L. Nimchuk,Mary Beth Mudgett,Sabine Elowe,Christine L. Gee,Ling Liu,Roger J. Daly,Gerard Manning,Jeffrey J. Babon,Jeffrey J. Babon,Isabelle S Lucet +27 more
TL;DR: The thermal-shift assay is proposed to be adopted as the standard technique for establishing the nucleotide-binding and catalytic potential of kinase-like domains.
Journal ArticleDOI
Allosteric Activation of Functionally Asymmetric RAF Kinase Dimers
Jiancheng Hu,Edward C. Stites,Haiyang Yu,Elizabeth Germino,Hiruy S. Meharena,Philip J.S. Stork,Alexandr P. Kornev,Susan S. Taylor,Andrey S. Shaw +8 more
TL;DR: It is shown that the dimer is functionally asymmetric with one kinase functioning as an activator to stimulate activity of the partner, receiver kinase.
Journal ArticleDOI
Tribbles homolog 2 inactivates C/EBPα and causes acute myelogenous leukemia
Karen Keeshan,Yiping He,Bas J. Wouters,Olga Shestova,Lanwei Xu,Hong Sai,Carlos G. Rodriguez,Ivan Maillard,John W. Tobias,Peter J. M. Valk,Martin Carroll,Jon C. Aster,Ruud Delwel,Warren S. Pear +13 more
TL;DR: The data identify Trib2 as an oncogene that induces AML through a mechanism involving inactivation of C/EBPalpha, and Trib2 expression was elevated in a subset of human AML patient samples.
Journal ArticleDOI
The molecular regulation of Janus kinase (JAK) activation.
Jeffrey J. Babon,Jeffrey J. Babon,Isabelle S Lucet,Isabelle S Lucet,James M. Murphy,James M. Murphy,Nicos A. Nicola,Nicos A. Nicola,Leila N. Varghese,Leila N. Varghese +9 more
TL;DR: The JAK (Janus kinase) family members serve essential roles as the intracellular signalling effectors of cytokine receptors, and the current knowledge of their physiological functions and the causative role of activating and inactivating JAK mutations in human diseases is reviewed.
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