There's more to death than life: Noncatalytic functions in kinase and pseudokinase signaling.
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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
Citations
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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
Inhibitor-induced HER2-HER3 heterodimerisation promotes proliferation through a novel dimer interface
Jeroen Claus,Gargi Patel,Gargi Patel,Flavia Autore,Audrey Colomba,Gregory Weitsman,Tanya N. Soliman,Selene K. Roberts,Laura C. Zanetti-Domingues,Michael Hirsch,Francesca Collu,Roger George,Elena Ortiz-Zapater,Paul R. Barber,Paul R. Barber,Boris Vojnovic,Boris Vojnovic,Yosef Yarden,Marisa L. Martin-Fernandez,Angus J.M. Cameron,Angus J.M. Cameron,Franca Fraternali,Tony Ng,Tony Ng,Peter J. Parker,Peter J. Parker +25 more
TL;DR: It is shown that lapatinib, an ATP-competitive inhibitor of HER2, is able to induce proliferation cooperatively with the HER3 ligand neuregulin, and this provides mechanistic insights into the liabilities involved in targeting kinases with ATP- competitive inhibitors.
Journal ArticleDOI
Molecular Basis for poly(A) RNP Architecture and Recognition by the Pan2-Pan3 Deadenylase.
Ingmar B. Schäfer,Masami Yamashita,Jan M. Schuller,Steffen Schüssler,Peter Reichelt,Mike Strauss,Elena Conti +6 more
TL;DR: The structure reveals the basis for the periodic repeating architecture at the 3′ end of cytoplasmic mRNAs and illustrates mechanistically how RNA-bound Pab1 oligomers act as rulers for poly(A) tail length over the m RNAs’ lifetime.
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The structure of the Pan2–Pan3 core complex reveals cross-talk between deadenylase and pseudokinase
TL;DR: It is shown that recombinant Saccharomyces cerevisiae Pan2–Pan3 can deadenylate RNAs in vitro without needing the poly(A)-binding protein Pab1.
Journal ArticleDOI
Non-catalytic signaling by pseudokinase ILK for regulating cell adhesion
Julia Vaynberg,Koichi Fukuda,Fan Lu,Fan Lu,Katarzyna Bialkowska,Yinghua Chen,Edward F. Plow,Jun Qin,Jun Qin +8 more
TL;DR: It is shown that by recruiting FA adaptors PINCH and Parvin into a heterotrimeric complex (IPP), ILK triggers F-actin filament bundling – a process known to generate force/mechanical signal to promote cytoskeleton reassembly and dynamic cell adhesion.
Journal ArticleDOI
Structural Insights into Pseudokinase Domains of Receptor Tyrosine Kinases
Joshua B. Sheetz,Sebastian Mathea,Hanna Karvonen,Ketan Malhotra,Deep Chatterjee,Wilhelmiina Niininen,Robert Perttilä,Franziska Preuss,Franziska Preuss,Krishna Suresh,Steven Stayrook,Yuko Tsutsui,Ravi Radhakrishnan,Daniela Ungureanu,Stefan Knapp,Stefan Knapp,Mark A. Lemmon +16 more
TL;DR: Structures of all pseudokinase domains from the Wnt-binding receptor tyrosine kinases found that they share a conserved inactive conformation in their activation loop that resembles the autoinhibited insulin receptor kinase (IRK).
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