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2. , et al. Tetrahedron Lett. 47, 7905-7909 (2006). 3. , et al. Org. Biomol. Chem. 7, 2894-2904 (2009). 14 Breaking Away: Proceedings of the 21st American Peptide Symposium Michal Lebl (Editor) American Peptide Society, 2009 Racemization of Cysteine and Histidine Residues in Automated Peptide Synthesis Krzysztof Darlak, Thomas E. A. Introduction Automated peptide synthesis allows for preparation of a large number of peptide sequences in a fairly straightforward manner. Currently, the most widely applied methodologies utilize Fmocprotection in combination with uronium/phosphonium activating agents for synthesis of peptides.
Clearly, in the HIV-1 protease molecule the two flaps do not function in an equivalent manner in the enzyme-substrate complex. Further work is being undertaken on selected flap analogues with site-specific NMR and EPR probes, in order to correlate the conformational properties of the flaps with catalytic properties in the HIV-1 protease protein molecule. 6 Fig. 7. Total chemical synthesis of HIV-1 protease covalent dimer. (A) 203 amino acid target sequence. (B) Fully convergent synthetic strategy.
Without that ingenious and powerful technique, modern chemical protein synthesis would not be feasible. I also wish to thank my colleagues and collaborators who have contributed to the development of modern chemical protein synthesis and its applications to the total synthesis of a variety of protein targets. S. Department of Energy, Grant number: DE-FG02-07ER64501. References 1. Yooseph, S. et al. PLoS. Biol. 5, e16 (2007). 2. , et al. Proc. Natl. Acad. Sci. A. 106, 6910-6915 (2009). 3. , Mebs, D.