Other Protein Targets

248 nM (right), (b) Farnesyltransferase inhibitor, IC50 25 iM. (c) COX-2 inhibitors with 60% (left) and 48% (right) inhibition at 1 pM 

Perola et al. successfully applied a stmcture-based virtual screening protocol to a database of 220000 commercially available compounds to identify farnesyltransferase (FT) inhibitors [98]. First, they applied a number of consecutive filters to 

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Other Targets Protein-Protein and Protein-RNA Interactions... 

OTHER TARGETS PROTEIN-PROTEIN AND PROTEIN-RNA INTERACTIONS... 

Notwithstanding the aforementioned difficulty in detecting specific target proteins other than the types normally observed in the taxonomic fingerprints from whole bacteria MALDI spectra (i.e., ribosomal proteins), some other target proteins and protein-like materials have been studied directly from whole cells. For example, Lantibiotics, antimicrobial peptides secreted by Gram-positive bacteria have been detected directly from whole bacteria by MALDI-TOF MS.51 The lantibiotics nisin and lacticin 481 were detected from whole cells and crude supernatants. Surprisingly, better results were reported from whole cells than the supernatants. In this study the presence of variants... 

The Ca -calmodulin complex stimulates a wide array of enzymes, pumps, and other target proteins. Two targets are... 

The interest in the present pharmaceutical industry is very wide spanning the overall drug discovery sphere encompassing data related to small molecules, structure activity relationships, pre-clinical candidates, clinical candidates, launched drugs, biomarkers, toxic molecules, and other target protein inhibitors. While no single database could address all these areas, attempts were made to at least address them individually. We have developed databases... 

G proteins get their name because they bind GTP as part of their effect An example is the G protein that is linked to the epinephrine receptor and leads to the production of cAMP as a second messenger. Receptor tyrosine kinases have a different mode of action. When they bind their hormone, they phos-phorylate tyrosine residues on themselves and other target proteins, which then act as a second messenger. Insulin is an example of a hormone that binds to a receptor tyrosine kinase. 

Fig. 5.1. (Opposite page) Possible mechanisms of actions of the eicosanoids in cell signaling. The eicosanoids are synthesized within cells, where they can exert their effects by modulating the activity of ion channels, protein kinases and other target proteins. They can also be extruded into the extracellular medium by selective membrane transporters. Once outside, they can bind to and activate C protein-linked membrane receptors on neighboring cells.

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