The site design process

Proteinkinases are targets for therapeutic agents designed to intervene in signaling processes in the diseased state. Most kinase inhibitors are directed towards the conserved ATP binding site. Because the essential features of this site are conserved in all eukaryotic protein kinases, it is generally assumed that the same compound will bind in a similar manner to different protein kinases.

8p tumor12 20-04-2013 36 3   Download

We report here the first crystal structure of a stable isosteric analogue of 1,3-bisphospho-D-glyceric acid (1,3-BPGA) bound to the catalytic domain of Trypanosoma cruzi glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH)in which the two phosphoryl moieties interact with Arg249. This complex possibly illustrates a step of the catalytic process by which Arg249 may induce compression of the product formed, allowing its expulsion fromthe active site.

13p fptmusic 12-04-2013 70 3   Download

X-prolyl dipeptidyl aminopeptidases (X-PDAP) are enzymes catalysing the release of dipeptides from the amino termini of polypeptides containing a proline or an alanine at the penultimate position. Involved in various mam-malian regulation processes, as well as in chronic human diseases, they have been proposed to play a role in pathogenicity forStreptococci.

10p awards 06-04-2013 34 4   Download