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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Book ChapterDOI
Cellular thermal shift assay (CETSA) for determining the drug binding affinity using Ba/F3 clones stably expressing receptor pseudokinases.
TL;DR: In this article , the authors describe the establishment of Ba/F3 clones stably expressing receptor pseudokinases, such as receptor tyrosine kinase-like orphan receptors (ROR1, ROR2), and the use thereof to evaluate binding of small molecule inhibitors to their intracellular (pseudo)kinase domain by CETSA.
Posted ContentDOI
Nanobodies identify an activated state of the TRIB2 pseudokinase
Sam A. Jamieson,Michael Pudjihartono,Christopher R Horne,Robert C. Day,James M. Murphy,Peter D. Mace +5 more
TL;DR: In combination, this study identifies features of TRIB2 that could be exploited for the development of inhibitors, and nanobody tools for future investigation ofTRIB1–3 function.
Journal ArticleDOI
Nanobodies identify an activated state of the TRIB2 pseudokinase
TL;DR: In this paper , the TRIB2-Nb4.103 complex was identified as a nanobody that can stabilize TRIB 2 pseudokinase domain dimer in a face-to-face manner.
Journal ArticleDOI
Pseudokinase NRP1 facilitates endocytosis of transferrin in the African trypanosome
TL;DR: In this article , the pseudokinase NRP1 (Tb427tmp.160.4770) was identified as a regulator of trypanosoma brucei endocytosis.
Posted ContentDOI
SHED-dependent oncogenic signalling of the PEAK3 pseudo-kinase
youcef Ounoughene,Elise fourgous,Yvan Boublik,Estelle Saland,Nathan Guiraud,Christian Recher,Serge Urbach,Philippe Fort,Jean-Emmanuel Sarry,Didier Fesquet,Serge Roche +10 more
TL;DR: In this article, the authors identified PEAK3 as a member of this family based on structural homology; however, its signalling mechanism remains unclear, and they found that although it can self-associate, PEAK-3 shows higher evolutionary divergence than PEAK1/2.
References
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Journal ArticleDOI
The Protein Kinase Complement of the Human Genome
TL;DR: The protein kinase complement of the human genome is catalogued using public and proprietary genomic, complementary DNA, and expressed sequence tag sequences to provide a starting point for comprehensive analysis of protein phosphorylation in normal and disease states and a detailed view of the current state of human genome analysis through a focus on one large gene family.
Journal ArticleDOI
The protein kinase family: conserved features and deduced phylogeny of the catalytic domains.
TL;DR: Phylogenetic mapping of the conserved protein kinase catalytic domains can serve as a useful first step in the functional characterization of these newly identified family members.
Journal ArticleDOI
A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera
Chloé James,Valérie Ugo,Jean-Pierre Le Couedic,Judith Staerk,François Delhommeau,Catherine Lacout,Loïc Garçon,Hana Raslova,Roland Berger,Annelise Bennaceur-Griscelli,Jean-Luc Villeval,Stefan N. Constantinescu,Nicole Casadevall,William Vainchenker +13 more
TL;DR: A clonal and recurrent mutation in the JH2 pseudo-kinase domain of the Janus kinase 2 (JAK2) gene in most (> 80%) polycythaemia vera patients leads to constitutive tyrosine phosphorylation activity that promotes cytokine hypersensitivity and induces erythrocytosis in a mouse model.
Journal ArticleDOI
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
Georgia Hatzivassiliou,Kyung Song,Ivana Yen,Barbara J. Brandhuber,Daniel Anderson,Ryan Alvarado,Mary J. C. Ludlam,David Stokoe,Susan L. Gloor,Guy Vigers,Tony Morales,Ignacio Aliagas,Bonnie Liu,Steve Sideris,Klaus P. Hoeflich,Bijay S. Jaiswal,Somasekar Seshagiri,Hartmut Koeppen,Marcia Belvin,Lori Friedman,Shiva Malek +20 more
TL;DR: It is demonstrated that ATP-competitive kinase inhibitors can have opposing functions as inhibitors or activators of signalling pathways, depending on the cellular context, which provides new insights into the therapeutic use of ATP- competitive RAF inhibitors.
Journal ArticleDOI
The Pseudokinase MLKL Mediates Necroptosis via a Molecular Switch Mechanism
James M. Murphy,Peter E. Czabotar,Peter E. Czabotar,Joanne M Hildebrand,Joanne M Hildebrand,Isabelle S Lucet,Jian-Guo Zhang,Jian-Guo Zhang,Silvia Alvarez-Diaz,Silvia Alvarez-Diaz,Rowena S. Lewis,Rowena S. Lewis,Najoua Lalaoui,Najoua Lalaoui,Donald Metcalf,Donald Metcalf,Andrew I. Webb,Andrew I. Webb,Samuel N. Young,Samuel N. Young,Leila N. Varghese,Leila N. Varghese,Gillian M. Tannahill,Gillian M. Tannahill,Esme C. Hatchell,Esme C. Hatchell,Ian J. Majewski,Ian J. Majewski,Toru Okamoto,Toru Okamoto,Renwick C. J. Dobson,Renwick C. J. Dobson,Douglas J. Hilton,Douglas J. Hilton,Jeffrey J. Babon,Jeffrey J. Babon,Nicos A. Nicola,Nicos A. Nicola,Andreas Strasser,Andreas Strasser,John Silke,John Silke,Warren S. Alexander,Warren S. Alexander +43 more
TL;DR: Structural-guided mutation of the MLKL pseudoactive site resulted in constitutive, RIPK3-independent necroptosis, demonstrating that modification ofMLKL is essential for propagation of the ne croptosis pathway downstream of RIPK 3.
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