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Purity profiling and the associated functional effects of a new peptide

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Abstract
Peptides show great pharmaceutical potential as active drugs and diagnostics in several clinical areas such as endocrinology, obstetrics or oncology. The search towards novel lead-peptides with a biological function has thus attracted renewed interest. Within a collaborative, multidisciplinary approach investigating the mouse peptidomics [1], new peptides were identified with the potential of serving as a basis towards new peptidic drugs. Tissue organ bath tests were used for functional screening of these newly identified peptides, obtained in sufficient quantity by chemical synthesis. One of these new peptides, SBO215_7, was identified to induce baseline contractions in longitudinal smooth muscle preparations of the guinea pig ileum (GPI). However, unlike the initially tested crude peptide, the pure peptide (> 95% purity) could not induce the previously observed baseline contractions. Peptide purity (crude vs. > 95% purity) will thus influence the final outcome of the functionality testing. Nevertheless, this quality aspect is generally neglected in this phase of investigation, leading to wrong fail/pass decisions. The crude peptide was synthesized by three different world-wide suppliers and characterized in comparison with the high-purity (> 95%) peptide. Their purity profile was investigated using HPLC-UV/DAD-ESI/MSn allowing purity quantification as well as identification of the related impurities. Each of the three suppliers had a different major impurity, with only a few impurities in common. Moreover, differences in GPI-contraction behaviour was observed between the different peptide suppliers and qualities. We thus demonstrated that the quality of peptides is an important aspect in their functional screening using tissue organ bath experiments.
Keywords
Peptides, Functionality conclusions, Impurity profiling

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Chicago
Verbeken, Mathieu, Romain Lefebvre, Goossens Els, Luyten Walter, Schoofs Liliane, and Bart De Spiegeleer. 2011. “Purity Profiling and the Associated Functional Effects of a New Peptide.” In Abstract Book 15th Forum of Pharmaceutical Sciences.
APA
Verbeken, M., Lefebvre, R., Els, G., Walter, L., Liliane, S., & De Spiegeleer, B. (2011). Purity profiling and the associated functional effects of a new peptide. Abstract book 15th forum of pharmaceutical sciences. Presented at the 15th Forum of Pharmaceutical Sciences.
Vancouver
1.
Verbeken M, Lefebvre R, Els G, Walter L, Liliane S, De Spiegeleer B. Purity profiling and the associated functional effects of a new peptide. Abstract book 15th forum of pharmaceutical sciences. 2011.
MLA
Verbeken, Mathieu, Romain Lefebvre, Goossens Els, et al. “Purity Profiling and the Associated Functional Effects of a New Peptide.” Abstract Book 15th Forum of Pharmaceutical Sciences. 2011. Print.
@inproceedings{1234114,
  abstract     = {Peptides show great pharmaceutical potential as active drugs and diagnostics in several clinical areas such as endocrinology, obstetrics or oncology. The search towards novel lead-peptides with a biological function has thus attracted renewed interest. Within a collaborative, multidisciplinary approach investigating the mouse peptidomics [1], new peptides were identified with the potential of serving as a basis towards new peptidic drugs. Tissue organ bath tests were used for functional screening of these newly identified peptides, obtained in sufficient quantity by chemical synthesis. One of these new peptides, SBO215\_7, was identified to induce baseline contractions in longitudinal smooth muscle preparations of the guinea pig ileum (GPI). However, unlike the initially tested crude peptide, the pure peptide ({\textrangle} 95\% purity) could not induce the previously observed baseline contractions. Peptide purity (crude vs. {\textrangle} 95\% purity) will thus influence the final outcome of the functionality testing. Nevertheless, this quality aspect is generally neglected in this phase of investigation, leading to wrong fail/pass decisions. The crude peptide was synthesized by three different world-wide suppliers and characterized in comparison with the high-purity ({\textrangle} 95\%) peptide. Their purity profile was investigated using HPLC-UV/DAD-ESI/MSn allowing purity quantification as well as identification of the related impurities. Each of the three suppliers had a different major impurity, with only a few impurities in common. Moreover, differences in GPI-contraction behaviour was observed between the different peptide suppliers and qualities. We thus demonstrated that the quality of peptides is an important aspect in their functional screening using tissue organ bath experiments.},
  author       = {Verbeken, Mathieu and Lefebvre, Romain and Els, Goossens  and Walter, Luyten and Liliane, Schoofs and De Spiegeleer, Bart},
  booktitle    = {Abstract book 15th forum of pharmaceutical sciences},
  keyword      = {Peptides,Functionality conclusions,Impurity profiling},
  language     = {eng},
  location     = {Spa, Belgium},
  title        = {Purity profiling and the associated functional effects of a new peptide},
  year         = {2011},
}