Protein Kinase Inhibitor History

Protein kinases catalyze the phosphorylation of proteins, peptides, lipids, and sugars by using ATP, the energy store of the cell, as a phosphate donor  

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Trask, O.J., Jr. et al. 2006. Assay development and case history of a 32K-biased library high-content MK2-EGFP translocation screen to identify p38 mitogen-activated protein kinase inhibitors on the Array Scan 3.1 imaging platform. Meth. Enzymol. 414, 419-439. 

Anthraquinones The Oj Pile). Alizarin (1,2-dihydroxyanthraquinone) is the orange-red compound of Rubia tinctorum (madder) (Rubiaceae), a longstanding dyestuff in human history. A range of anthraquinones are variously cathartic, antimicrobial and cytotoxic. A variety of anthraquinones are protein kinase inhibitors including alizarin, chrysazin, damnacanthal, emodin and purpurin. 

The majority of indolocarbazole alkaloids, isolated so far from nature, are derivatives of the indolo[2,3-fl]pyrrolo[3,4-c]carbazole ring system 292. They have been isolated from soil organisms, slime molds, and marine sources (3,7,8,252-255), and have shown a broad range of potent biological activities, such as antifungal, antimicrobial, antitumor, and antihypertensive activity (3,7,256-260,267-270). Their activity as potent inhibitors of protein kinase C (PKC) has received special attention, and was the focus of several investigations (8,257,258,271-280). The history of these natural products dates back about 30 years (Scheme 2.73). 

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