|Name||Mr. Reed Roberts|
|Organization or Institution||Southeastern University|
Applications of the Cesium Effect: Synthesis of de Novo Peptidomimetics as Potential Anticancer Agents.
Reed W. Roberts, Aaron J. Todman, Quintan T. Rossow, Mark E. Steury, Nathaniel J. Jordan, Lucas Kline and Ralph N. Salvatore*
Numerous physiological and pathological stimuli induced programmed cell death (apoptosis), and the Bcl-2 family of oncoproteins plays a central role in this regulation. Proteins such as Bcl-2 are known to inhibit apoptosis, and uncontrolled cell survival due to Bcl-2 overexpression has been proven to make a significant contribution to tumor formation. With this in mind, we have directed our attention toward the synthesis of a variety of non-peptide inhibitors of oncoprotein Bcl-2. Thus, we disclose herein efficient protocols leading to the synthesis of carbazate, dithiocarbazate, dithiocarbamate, a "carbamatoid" and amine peptidomimetics, respectively. This study is now being extended to the synthesis of other de novo analogs (diselenocarbamate) with similar structural features to natural proteins, that may interrupt protein-protein interactions. Utilizing our aforementioned protocols, various scaffoldings are being employed for the development of novel artificial biomolecules, which may result in interesting biological behaviors regarding the disruption of protein-protein interactions and furthermore, may serve as potential therapeutics in clinical chemotherapy.