Bert Gevaert

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Bert Gevaert

Drug Quality and Registration (DruQuaR) group
Ottergemsesteenweg 460, 9000 Ghent (Belgium)

Phone: + 32 (0)9 264.80.94 (secr. 81.01)
Fax: + 32 (0)9 264.81.93
E-mail: Bert.Gevaert@UGent.be

 

 

Ph.D. research

 

Title: Chemical-functional characterization of prepro-neuroproteins derived peptides.

Summary:

Limited proteolysis involves the cleavage of a target protein by many proteases with different specificity, releasing several distinct peptides, by virtue of its structure of tissue, with possibly different physiological activities. A striking example is the pituitary multihormone precursor prepro-opiomelanocortin (POMC), which contains sequences for lipotropins, MSHs, β-endorphin, enkephalin and ACTH (corticotropin). The unraveling of such cryptic peptide systems will not only significantly increase our fundamental understanding, but also aid the development of novel therapeutic strategies for a wide diversity of human illnesses.

The general goal of this project is to find and chemical-functionally characterize new bioactive peptides originating from selected prepro-proteins. The hypotheses of a hitherto unknown cryptic system looks confirmed as our group discovered a new cryptic octapeptide, coded NMG, that shows activity in the guinea ileum tissue bath and antinociceptive properties in the mouse. In a first phase, NMG will be characterized: after the development of a selective and sensitive bioanalytical LC/MS method, the endogenous distribution, the influence of exogen factors on its production and the metabolization of NMG will be determined. Further, the distribution of injected NMG will be examined with special interest for the ADME and BBB characteristics and the functionality of this peptide will be investigated. Finally, the structure-activity relationship will be determined and the activity of NMG will be explored by modeling and docking. In a second part of this project, we intend to find more bioactive peptides derived from the investigated prepro-neuropreoteins. These peptides will be generated in 2 ways: by enzymatic digestion and by SPOT synthesis. After screening impedance measurements, more specific functional test will be performed investigation general receptor and immunomodulating activity.

Keywords: cryptic peptides, neuropeptidesystem

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