SEP 16, 2015 08:00 AM PDT

Diversity-Oriented Synthesis for Discovery of Novel Therapeutics

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  • Vice President, Discovery Chemistry, H3 Biomedicine
      Dr. Lisa Marcaurelle joined H3 Biomedicine as Vice President of Discovery Chemistry in April 2011, from the Broad Institute, where she was Director of Synthetic Chemistry in the Chemical Biology Platform.

      During her four years at the Broad Institute, Lisa established a synthetic platform for the large-scale production of diversity-oriented synthesis (DOS) libraries, generating a collection of more than 100,000 small molecules for use in high-throughput screening. While at the Broad, Lisa also served as a Project Leader for the Harvard/Broad Center for Chemical Methodology and Library Development (CMLD). Prior to joining the Broad, she worked at Infinity Pharmaceuticals from 2002 to 2007, where she was engaged in the synthesis of numerous DOS libraries and participated in oncology-focused medicinal chemistry efforts.

      Lisa completed her post-doctoral research at the Massachusetts Institute of Technology, working with Professor Peter Seeberger. She obtained a Ph.D. in chemistry from the University of California, Berkeley, working under the guidance of Professor Carolyn Bertozzi. Lisa earned a B.A. in chemistry from the College of the Holy Cross in Worcester, MA.

    Recent evidence demonstrating the importance of structural complexity in advancing compounds to the clinic points to the need for enhancing small molecule screening collections with sp3-rich compounds. The development of diversity-oriented synthesis (DOS) strategies for accessing libraries of sp3-rich compounds containing one or more stereogenic centers will be presented, focusing on library synthesis efforts at H3 Biomedicine as well as previous work at the Broad Institute. The DOS libraries which have been created, span a broad range of molecular frameworks, including macrocycles and medium-sized rings, as well as fused-, bridged- and spirocyclic- ring systems. Preliminary results of high-throughput screening of the H3 compound collection will be discussed, with an emphasis on the identification of novel modulators of pre-mRNA splicing.

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