The Daily Bulletin Archive

Please join the Chemistry and Physics departments for the seminar "Syntheses of Privileged Chemical Scaffold Containing Peptidomimetic Libraries, and Study of a Role of Metabolites Toward Sarcoma Treatment," presented by Sujit Suwal, senior research associate in the University of Miami's Miller School of Medicine, on Thursday, April 6, at 12:30 p.m. in Science and Mathematics Complex 173. All students, staff, and faculty are welcome. This seminar is partially funded by the Faculty-Student Association.

Abstract
Human genome sequencing has deconvoluted a myriad of potential therapeutic protein targets for treating different diseases. A wide variety of compounds—small molecules, oligomers, and biomimetics that are functionally diverse, potent, and highly specific against targeted biomolecules—are, therefore, in high demand to meet the current therapeutic needs. Often, small molecules bind to active sites, while oligomers bind to protein surfaces and alter their function allosterically. In either scenario, high-affinity ligands are important, which require compound rigidity that reduces entropic penalty upon binding to the target protein. To fulfill these needs, my research is focused toward diversification of privileged-chemical scaffold and syntheses of highly functionalized oligomers that resemble peptides and natural products. Using a solid-phase approach, oligomers that contain 6–12-mers (including privileged scaffolds) are synthesized and screened against targeted recombinant proteins. The hit molecules are separated manually and re-validated. Finally, the active components in the hit molecules are identified by sarcosine scanning and further pursued by medicinal chemistry toward developing high-affinity ligands. Biological relevance of the hit molecules are tested by in-vitro or in-cellulo assays.

Apart from genomic alteration and proteomic aberration, metabolomic perturbations have been identified in different types of diseases, for example, cancer. It is, therefore, important to explore the role of metabolites in drug efficacy, which governs cellular microenvironment and affects different cell processes. Also, the study of metabolomic perturbation discriminates metabolomic pattern before, after, and during treatment with drugs, and importantly it helps in discovering new drug targets and biomarkers.