Professor Zhao Changgui's Research Group from the College of Chemistry Published a Paper in Science
Recently, the research group led by Professor Zhao Changgui from the College of Chemistry at 91传媒 published a paper entitled "Two Free Ends Make a Match" in Science. The paper reviews recent progress in the organocatalytic construction of chiral macrocycles and highlights an approach in which peptide-based catalysts guide precise head-to-tail cyclization, allowing the predictable formation of 12- to 18-membered macrocycles.
The abstract of this paper is as follows:
Macrocycles—ring-shaped molecules with 12 or more atoms—can bind to large, flat, or flexible protein surfaces that are inaccessible to traditionally small-molecule drugs. Their three-dimensional (3D) cyclic structures serve as preorganized keys that fit specific bioactive sites. A macrocycle is often prepared through cyclization in which two ends of a linear precursor join to form a circle. However, existing cyclization methods require multiple synthesis steps. It is also difficult to control the resulting 3D structure because of the high energy barrier for a linear molecule to form a ring structure. On page 931 of this issue, Rackl et al. report a peptide-based organocatalyst that guides the ends of a linear precursor to form 12- to 18-membered rings with predictable 3D structure. This approach avoids arduous multistep processes of synthesis and could accelerate new drug discovery.
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