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Protein tyrosine kinases (PTKs) play a key role in cell signaling and regulate biological processes such as proliferation, differentiation, and apoptosis. The malfunctioning of these proteins is the root of many diseases. Over 60% of all oncoproteins and proto-oncoproteins, which play a key role in cancers, are PTKs. Malfunctioning of PTKs is also the hallmark of other diseases such as psoriasis,...
Within the last few years, therapeutic intervention into signal transduction cascades attracted the interest of pharmaceutical research. Apart from selective inhibition of phosphorylating and dephosphorylating enzymes, medicinal chemistry has focused on an SH2 domain-targeted drug design approach. This review will briefly summarize the role of adaptor proteins in signaling networks, followed by an...
Ras is a central switch in regulation of cell proliferation and differentiation. It becomes activated by extracellular stimuli like growth factors and relays the signal into diverse cellular pathways. A balanced action of regulatory proteins is required to maintain the desired level of Ras activity. Oncogenic mutations in Ras lead to uncontrollable over-function, resulting in transformation of the...
The protein Ras, an important intracellular signal transducer, is crucially involved in the development of tumor growth. The farnesylation of Ras, catalyzed by the enzyme Ras-farnesyltransferase, is essential to its proper functioning in the normal and in the transformed state. Therefore, the inhibition of Ras lipidation has become a promising target for the development of new classes of anti-tumor...
The PLC class of enzymes has been studied extensively over the past 15–20 years because of their involvement in signaling pathways in which extracellular messages are delivered to the cell to induce a response. Of the PLC isoenzymes, the PI-PLCs have perhaps been examined in the greatest detail because of their key role in initiating cellular response by hydrolyzing the phosphodiester bond of phosphatidylinositols...
Biological signal transduction pathways control the essential functions in all cells and tissues. Understanding the mechanisms at the molecular level accelerates the development of new selective medicines. The determination of the disease related molecular targets is also essential in these efforts. Photoaffinity labeling provides a well-established technique for identification, localization of binding...
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