Structure and Regulation of the Human Nek2 Centrosomal Kinase
P. Rellos,Frank J. Ivins,Joanne E. Baxter,Ashley C. W. Pike,Timothy J. Nott,Donna-Marie Parkinson,Sanjan Das,Steven Howell,Oleg Fedorov,Qi Yu Shen,Andrew M. Fry,Stefan Knapp,Stephen J. Smerdon +12 more
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TLDR
A role for dimerization-dependent allosteric regulation that combines with autophosphorylation and proteinosphatase 1c phosphatase activity to generate the precise spatial and temporal control required for Nek2 function in centrosomal maturation is suggested.About:
This article is published in Journal of Biological Chemistry.The article was published on 2007-03-02 and is currently open access. It has received 107 citations till now. The article focuses on the topics: Cyclin-dependent kinase 9 & Kinase activity.read more
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A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases
Oleg Fedorov,Brian D. Marsden,Vanda Pogacic,P. Rellos,Susanne Müller,Alex N. Bullock,Juerg Schwaller,Michael Sundström,Stefan Knapp +8 more
TL;DR: This analysis evaluated the specificity of 156 validated kinase inhibitors, including inhibitors used in clinical trials, against 60 human Ser/Thr kinases using a thermal stability shift assay and revealed many unexpected cross-reactivities for inhibitors thought to be specific for certain targets.
Journal ArticleDOI
Targeting Mitosis in Cancer: Emerging Strategies
Carmen Dominguez-Brauer,Kelsie L. Thu,Jacqueline M. Mason,Heiko Blaser,Mark R. Bray,Tak W. Mak +5 more
TL;DR: The concept of exploiting the genomic instability of tumor cells through therapeutic inhibition of mitotic checkpoints is discussed, and it is believed this strategy has a high likelihood of success given its potential to enhance therapeutic index by targeting tumor-specific vulnerabilities.
Journal ArticleDOI
Cell cycle regulation by the NEK family of protein kinases
TL;DR: The functions of the human NEKs are reviewed, with particular emphasis on those family members that are involved in cell cycle control, and their potential as therapeutic targets in cancer is considered.
Journal ArticleDOI
Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms
Natalia Jura,Xuewu Zhang,Nicholas F. Endres,Nicholas F. Endres,Markus A. Seeliger,Thomas Schindler,John Kuriyan +6 more
TL;DR: This mechanism, which involves the stabilization of the active conformation of an α helix, has features in common with mechanisms operative in several other kinases and is central to understanding of how kinase domain of the EGF receptor is activated.
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Mitotic regulation by NIMA-related kinases.
TL;DR: The evidence that NIMA-related kinases make a significant contribution to the orchestration of mitotic progression and thereby protect cells from chromosome instability is discussed and their potential as novel chemotherapeutic targets are highlighted.
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An Allosteric Mechanism for Activation of the Kinase Domain of Epidermal Growth Factor Receptor
TL;DR: It is found that the EGFR kinase domain can be activated by increasing its local concentration or by mutating a leucine in the activation loop, which suggests that the Kinase domain is intrinsically autoinhibited, and an intermolecular interaction promotes its activation.
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Active and Inactive Protein Kinases: Structural Basis for Regulation
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