00:00:01 1999 American Peptide Symposium, chaired by Bruce Merrifield. I'm Arno F. Spatola

00:00:08 from the Department of Chemistry and the Institute for Molecular Diversity and Drug Design at the University of Louisville.

00:00:14 This is an exciting time to be engaged in organic peptide synthesis. There were many presentations and posters of this meeting

00:00:21 that illustrate the incredible diversity of reactions, products, and matrices used in modern peptide science.

00:00:28 And these products are highly sought after for drug lead discovery and in proteomics.

00:00:34 In fact, a colleague interested in discovering new proteins and modified proteins suggested to me that

00:00:40 we've got the targets and you have the bullets. While I'm not sure that in this era of gun control I can endorse his analogy,

00:00:48 it is clear that those of us engaged in synthesis will be very busy at the start of this new millennium.

00:00:54 One of the clearest themes of this meeting was the broad use of organic reactions to create new modified amino acids,

00:01:01 peptidomimetics, and protein derivatives. Many of these are attempts to expand structural diversity with glycopeptides,

00:01:10 lipopeptides, and even nucleopeptides. But there is increasing emphasis on replicating phosphorylated peptides

00:01:19 in their analogs, as well as farnesylated derivatives, or peptides with various branched carbohydrates,

00:01:26 in an effort to duplicate the wide range of post-translational modifications being cataloged in humans and other organisms.

00:01:34 Another trend evident at this pivotal conference was the emphasis on improved methods of synthesis.

00:01:40 These range from increased use of solid phase reactions, new and improved coupling reagents,

00:01:45 including perhaps the rediscovery of Fischer's amino acid chlorides, and further investigation of novel multifaceted solid supports

00:01:53 that could prove equally useful for synthesis and analysis. To this admittedly biased observer,

00:02:00 there seemed to be even more interest and examples of the use of cyclization for constrained peptide analog synthesis.

00:02:08 Finally, we also learned of the need to consider the synthesis of structures that could survive the many different types of traps

00:02:16 that hinder bioavailability as peptide analogs meander to their ultimate sites of action.

00:02:23 The aforementioned glycopeptides can help, as can various pegylated derivatives.

00:02:28 But synthetic chemists need to consider not only new strategies of prodrugs,

00:02:33 but must also be well informed about alternate delivery methods and the special requirements that accompany these modes.

00:02:41 Thank you and happy birthday, Bruce, for all that you have meant to us as both a scientist and as a friend.

00:02:48 Those who remind us that if we can see further, it is because we are standing on the shoulders of giants, must surely have had you in mind.