a screen for peptide agonists of the g-csf receptor屏幕上的肽受体激动剂g - csf受体.pdfVIP

Conzelmann and Schneider BMC Research Notes 2011, 4:194 /1756-0500/4/194 PROJECT NOTE Open Access A screen for peptide agonists of the G-CSF receptor * Nadine Conzelmann and Armin Schneider Abstract Background: Granulocyte-colony stimulating factor (G-CSF) is one of the most important pharmacologically used proteins. Potential uses beyond the stimulation of neutrophilic granulocytes are the treatment of CNS disorders. Disadvantages of the G-CSF protein as a drug are its moderate plasma half-life time and considerable production costs. We therefore conducted a screen for peptide agonists derived from the sequence of human G-CSF. Findings: Despite of the high sensitivity of our screening system we could not detect any positive hits in a single peptide approach. In a multiplex approach using a permutation of any combination of 10 different peptides we could also not detect a positive block. Conclusions: We conclude that larger coherent parts of the protein or dimerising peptides may be needed to achieve activation of the receptor. Background half-life time (~4 h), the relatively high costs, and Granulocyte-colony stimulating factor (G-CSF) is one chronic effects on the hematopoietic system. Pegylated the most widely employed protein drugs. It is mostly forms of G-CSF are available that have a much extended used for counteracting neutropenia in patients receiving half-life, however, it is unclear at present if those modi- chemotherapy [1], but also for stem cell harvesting [2,3], fications hinder passage of the blood-brain-barrier and as add-on to anti-infectious therapy. G-CSF is a gly- (BBB). coprotein that binds in 2:2