Paul Shapiro's research while affiliated with University of Maryland, Baltimore and other places

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Publications (1)


Next Generation Kinase Inhibitors Moving Beyond the ATP Binding/Catalytic Sites: Moving Beyond the ATP Binding/Catalytic Sites
  • Book

January 2020

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17 Reads

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11 Citations

Paul Shapiro

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.

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Citations (1)


... In the last few decades, many new therapies emerged by targeting cancer-relevant kinases using small molecules. [96][97][98][99] Consequently, kinases are now the second most common drug target, 87 and the rapidly increasing number of kinase-targeting small molecules in the clinical practice affirms the efficacy of modulating the phosphoproteome as an effective disease treatment. This rise in kinase binders has also provided a large number of compounds against diverse kinases that have been leveraged to develop bifunctional compounds, such as phosphorylation-inducing chimeric small molecules (PHICS) (Fig. 4). ...

Reference:

Proximity-inducing modalities: the past, present, and future
Next Generation Kinase Inhibitors Moving Beyond the ATP Binding/Catalytic Sites: Moving Beyond the ATP Binding/Catalytic Sites
  • Citing Book
  • January 2020