A Carbohydrate-Derived Splice Modulator

  • J Am Chem Soc. 2016 Apr 20;138(15):5063-8. doi: 10.1021/jacs.5b13427.
Sachin Dhar  1 ,  James J La Clair  1 ,  Brian León  1 ,  Justin C Hammons  1 ,  Zhe Yu  2 ,  Manoj K Kashyap  2 ,  Januario E Castro  2 ,  Michael D Burkart  1
Affiliations
  • 1. Department of Chemistry and Biochemistry, University of California-San Diego , 9500 Gilman Drive, La Jolla, California 92093-0358, United States.
  • 2. Moores Cancer Center, University of California-San Diego , La Jolla, California 92093-0358, United States.
PMID: 27058259 DOI: 10.1021/jacs.5b13427
Abstract

Small-molecule splice modulators have recently been recognized for their clinical potential for diverse cancers. This, combined with their use as tools to study the importance of splice-regulated events and their association with disease, continues to fuel the discovery of new splice modulators. One of the key challenges found in the current class of Materials arises from their instability, where rapid metabolic degradation can lead to off-target responses. We now describe the preparation of bench-stable splice modulators by adapting carbohydrate motifs as a central scaffold to provide rapid access to potent splice modulators.

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