Inhibitors of cyclin-dependent kinases as cancer therapeutics.
TLDR
The advent of potent isoform‐selective inhibitors with accompanying biomarkers has re‐ignited interest in the development of inhibitors of the cyclin‐dependent kinases and resistance mechanism are beginning to be identified for CDK inhibitors.About:
This article is published in Pharmacology & Therapeutics.The article was published on 2017-05-01 and is currently open access. It has received 233 citations till now. The article focuses on the topics: Cyclin-dependent kinase & Palbociclib.read more
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Mechanisms of Cellular Senescence: Cell Cycle Arrest and Senescence Associated Secretory Phenotype
Ruchi Kumari,Parmjit S Jat +1 more
TL;DR: In this article, the molecular mechanisms that underlie cellular senescence and the senescent associated growth arrest with a particular focus on why cells stop dividing, the stability of the growth arrest, the hypersecretory phenotype and how the different pathways are all integrated.
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The broken cycle: E2F dysfunction in cancer.
Lindsey N. Kent,Gustavo Leone +1 more
TL;DR: The activities of E1F proteins in cancer and therapeutic strategies to target this oncogenic pathway are discussed, with an emphasis on the newest atypical E2F family members.
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Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials
Ann Lin,Ann Lin,Christopher J. Giuliano,Christopher J. Giuliano,Ann C. Palladino,Kristen M. John,Kristen M. John,Connor Abramowicz,Connor Abramowicz,Monet Lou Yuan,Erin L. Sausville,Devon A. Lukow,Devon A. Lukow,Luwei Liu,Luwei Liu,Alexander R. Chait,Zachary C. Galluzzo,Clara Tucker,Clara Tucker,Jason M. Sheltzer +19 more
TL;DR: It is suggested that stringent genetic validation of the mechanism of action of cancer drugs in the preclinical setting may decrease the number of therapies tested in human patients that fail to provide any clinical benefit.
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Cell cycle control in cancer.
TL;DR: A detailed analysis of cell cycle control mechanisms and their role in cancer can be found in this article, where the authors reveal how these dependencies can be best exploited in cancer treatment and how to best exploit these dependencies.
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Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs.
TL;DR: A crucial mechanism in controlling cell cycle progression is the precise timing of more than 32,000 phosphorylation and dephosphorylation reactions catalyzed by a network of protein kinases and phosphoprotein phosphatases as determined by mass spectrometry.
References
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Hallmarks of cancer: the next generation.
TL;DR: Recognition of the widespread applicability of these concepts will increasingly affect the development of new means to treat human cancer.
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CDK inhibitors: positive and negative regulators of G1-phase progression
TL;DR: This work challenges previous assumptions about how the G1/S transition of the mammalian cell cycle is governed, helps explain some enigmatic features of cell cycle control that also involve the functions of the retinoblastoma protein (Rb) and the INK4 proteins, and changes the thinking about how either p16 loss or overexpression of cyclin D-dependent kinases contribute to cancer.
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Cancer Cell Cycles
TL;DR: Genetic alterations affecting p16INK4a and cyclin D1, proteins that govern phosphorylation of the retinoblastoma protein and control exit from the G1 phase of the cell cycle, are so frequent in human cancers that inactivation of this pathway may well be necessary for tumor development.
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Wnt/β-catenin signaling and disease.
Hans Clevers,Roel Nusse +1 more
TL;DR: An update of the core Wnt/β-catenin signaling pathway is provided, how its various components contribute to disease, and outstanding questions to be addressed in the future are discussed.