Protein Kinase C Protocols
Protein Kinase C Protocols

Author: Alexandra C. Newton

Publisher: Springer Science & Business Media

Published: 2008-02-03

Total Pages: 565

ISBN-13: 1592593976

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Since the discovery that protein kinase C (PKC) transduces the ab- dance of signals that result in phospholipid hydrolysis, this enzyme has been at the forefront of research in signal transduction. Protein Kinase C Protocols covers fundamental methods for studying the structure, function, regulation, subcellular localization, and macromolecular interactions of PKC. Protein Kinase C Protocols is divided into 11 sections representing the major aspects of PKC regulation and function. Part I contains an introduction and a historical perspective on the discovery of PKC by Drs. Yasutomi Nishizuka and Ushio Kikkawa. Part II describes methods to purify PKC. Part III describes the standard methods for measuring PKC activity: its enzymatic activity and its stimulus-dependent translocation from the cytosol to the membrane. Part IV describes methods for measuring the membrane interaction of PKC in vivo and in vitro. Part V provides methodologies and techniques for measuring the ph- phorylation state of PKC, including a protocol for measuring the activity of PKC’s upstream kinase, PDK-1. Novel methods for identifying substrates are described in Part VI. Part VII presents protocols for expressing and analyzing the membrane targeting domains of PKC. Part VIII provides a comprehensive c- pilation of methods used to identify binding partners for PKC. Part IX describes pharmacological probes used to study PKC. The book ends with a presentation of genetic approaches to study PKC (Part X) and a discussion of approaches used to study PKC in disease (Part XI).

Protein Kinase D Signaling Through Substrate Phosphorylation
Protein Kinase D Signaling Through Substrate Phosphorylation

Author: Sokha Nhek

Publisher:

Published: 2009

Total Pages: 370

ISBN-13:

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By combining in vitro biochemical and in silico screening approaches with the substrate-directed PKD pMOTIF antibody, we were able to identify oxysterol-binding protein (OSBP) and signal-induced proliferation-associated 1-like protein 1 (SIPA1L1) as novel PKD substrates. PKD phosphorylation of OSBP inhibits its 25-hydroxycholesterol-induced Golgi localization. These findings reveal PKD as the first identified upstream kinase to regulate OSBP localization. 25OH- mediated OSBP localization regulates sphingomyelin synthesis, demonstrating an additional mechanism in which PKD regulates Golgi lipid homeostasis. PKD phosphorylation of SIPA1L1 and binding through a PDZ domain-interaction regulates SIPA1L1 proteasomal degradation. The cellular abundance of SIPA1L1 protein is critical to its function in E6-induced mammary epithelial cell transformation and neuronal cell morphology, thus implicating PKD in regulation of these biological processes.

Next Generation Kinase Inhibitors
Next Generation Kinase Inhibitors

Author: Paul Shapiro

Publisher: Springer Nature

Published: 2020-07-14

Total Pages: 224

ISBN-13: 3030482839

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Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease.

Cyclin Dependent Kinase 5 (Cdk5)
Cyclin Dependent Kinase 5 (Cdk5)

Author: Nancy Y. Ip

Publisher: Springer Science & Business Media

Published: 2009-02-28

Total Pages: 326

ISBN-13: 0387788875

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Cyclin Dependent Kinase 5 provides a comprehensive and up-to-date collection of reviews on the discovery, signaling mechanisms and functions of Cdk5, as well as the potential implication of Cdk5 in the treatment of neurodegenerative diseases. Since the identification of this unique member of the Cdk family, Cdk5 has emerged as one of the most important signal transduction mediators in the development, maintenance and fine-tuning of neuronal functions and networking. Further studies have revealed that Cdk5 is also associated with the regulation of neuronal survival during both developmental stages and in neurodegenerative diseases. These observations indicate that precise control of Cdk5 is essential for the regulation of neuronal survival. The pivotal role Cdk5 appears to play in both the regulation of neuronal survival and synaptic functions thus raises the interesting possibility that Cdk5 inhibitors may serve as therapeutic treatment for a number of neurodegenerative diseases.