Src protein

Cruz-Aguado, J.A., Chen, Y., Zhang, Z., Brook, M.A. and Brennan, J.D. (2004) Entrapment of Src protein tyrosine kinase in sugar-modified silica. Analytical Chemistry, 76, 4182— 4188. 

Geertzema, A. Hennipman, and G. Rijksen, c-Src protein expression is increased in human breast cancer. A immunohistochemical and biochemical analysis, J. Pathol. 180 383 (1996). 

An, W. G., T. W. Schulte, and L. M. Neckers. The heat shock protein 90 antagonist geldanamycin alters chaperone association with p210bcr-abl and v-src proteins before their degradation by the proteasome. Cell Growth Differ. 11 355-60.2000. 

The second type of point mutation results in the replacement of one amino acid with another. Such mutations will have more or less of an effect depending on which amino acid is changed. Obviously, if a critical amino acid is replaced by one that is unable to provide the same function, the protein will lose some or all of its activity. Mutations within that Ras and Src genes are two examples in which point mutations lead to disease. In the case of the Ras protein, substitution of a single amino acid, most commonly at either position 12 or 61, is associated with the occurrence of several human tumors. In the case of the Src protein, a point mutation that occurs in a tyrosine residue leads to the constitutive activation of the protein and is associated once again with several types of tumors. 

Halistanol sulfate (532) from Halichondria cf. moorei is a tris-sodium sulfate salt, which possesses antimicrobial, hemolytic, and ichthyotoxic activity [444]. It was later isolated from two sponges of the genus Topsentia as the free sterol and found to inhibit pp60v-src protein tyrosine kinase activity [445]. The tris(2-aminoimidazolium) salt of halistanol sulfate (533) was isolated from Topsentia sp. from Japan and is also antimicrobial [446]. 

MAP kinase kinases Src Protein tyrosine kinase encoded by... 

Melemeleones A and B (320 and 321) possess a 4,9-friedodrimane sesquiterpene array linked to a quinone bearing a taurine and they are structurally related to avarol. Compounds 320 and 321 were isolated from the sponge Dysidea sp. and identified by analysis of their spectroscopic data. Compound 321 showed a moderate inhibitory activity against the pp60v src protein Tyrosine Kinase with an IC50 of 28 pM [236]. 

Lou Q, Leftwich ME, Lam KS, Identification of GIYWHHY as a novel peptide substrate for human p60c-src protein tyrosine kinase, Bioorg. Med. Chem., 4 677-682, 1996. 

Fig. 2. A comparison of the sequences surrounding the sites of phosphorylation by protein C of the human EGF receptor and the human c-src protein. Taken from Gould et al. [13]. The single-letter amino acid code is used., serine (S) or threonine (T) at equivalent positions.

Kwon, HJ. et al. 1992. Potent and specific inhibition of p60v-src protein kinase both in vivo and in vitro by radicicol. Cancer Res. 52, 6926-6930. 

Houseman et al. prepared a peptide chip by Diels-Alder-mediated reaction of kinase-peptide substrates with a self-assembled monolayer of alkanethiolates on gold surface. Peptide phosphorylation was determined by incubating the peptide microarrays with c-src protein-tyrosine kinase followed by quantitation with a phos-phoryl imager. In the presence of soluble inhibitors at a range of concentrations, dose-dependent inhibition of phosphorylation against a number of peptide substrates could be determined on a single chip. ... 

Luttrell LM, Ferguson SS, Daaka Y, et al. P-Arrestin-dependent formation of P2 adrenergic receptor-Src protein kinase complexes. Science 1999 283 655-661. 

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